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1. Traboulsi H, Guerrina N, Iu M, Maysinger D, Ariya P, Baglole CJ: Inhaled Pollutants: The Molecular Scene behind Respiratory and Systemic Diseases Associated with Ultrafine Particulate Matter. Int J Mol Sci; 2017 Jan 24;18(2)
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  • Air pollution is a complex mixture that varies in space and time, and contains hundreds of compounds including volatile organic compounds (e.g., benzene), metals, sulphur and nitrogen oxides, ozone and particulate matter (PM).
  • Some of the pathogenic mechanisms through which PM<sub>0.1</sub> may contribute to chronic disease is their ability to induce inflammation, oxidative stress and cell death by molecular mechanisms that include transcription factors such as nuclear factor κB (NF-κB) and nuclear factor (erythroid-derived 2)-like 2 (Nrf2).

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  • (PMID = 28125025.001).
  • [ISSN] 1422-0067
  • [Journal-full-title] International journal of molecular sciences
  • [ISO-abbreviation] Int J Mol Sci
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; air pollution / aryl hydrocarbon receptor / chronic obstructive pulmonary disease / epigenetics / nuclear factor-κB / particulate matter
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2. Guixà-González R, Albasanz JL, Rodriguez-Espigares I, Pastor M, Sanz F, Martí-Solano M, Manna M, Martinez-Seara H, Hildebrand PW, Martín M, Selent J: Membrane cholesterol access into a G-protein-coupled receptor. Nat Commun; 2017 Feb 21;8:14505
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  • [Title] Membrane cholesterol access into a G-protein-coupled receptor.
  • Cholesterol is a key component of cell membranes with a proven modulatory role on the function and ligand-binding properties of G-protein-coupled receptors (GPCRs).
  • Crystal structures of prototypical GPCRs such as the adenosine A<sub>2A</sub> receptor (A<sub>2A</sub>R) have confirmed that cholesterol finds stable binding sites at the receptor surface suggesting an allosteric role of this lipid.
  • We confirm the presence of cholesterol inside the receptor by chemical modification of the A<sub>2A</sub>R interior in a biotinylation assay.

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  • (PMID = 28220900.001).
  • [ISSN] 2041-1723
  • [Journal-full-title] Nature communications
  • [ISO-abbreviation] Nat Commun
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
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3. Matalonga J, Glaria E, Bresque M, Escande C, Carbó JM, Kiefer K, Vicente R, León TE, Beceiro S, Pascual-García M, Serret J, Sanjurjo L, Morón-Ros S, Riera A, Paytubi S, Juarez A, Sotillo F, Lindbom L, Caelles C, Sarrias MR, Sancho J, Castrillo A, Chini EN, Valledor AF: The Nuclear Receptor LXR Limits Bacterial Infection of Host Macrophages through a Mechanism that Impacts Cellular NAD Metabolism. Cell Rep; 2017 Jan 31;18(5):1241-1255
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] The Nuclear Receptor LXR Limits Bacterial Infection of Host Macrophages through a Mechanism that Impacts Cellular NAD Metabolism.
  • Using a model of infection by Salmonella Typhimurium, we have identified a molecular mechanism regulated by the nuclear receptor LXR that limits infection of host macrophages through transcriptional activation of the multifunctional enzyme CD38.
  • Altogether, this work reveals an unappreciated role for CD38 in bacterial-host cell interaction that can be pharmacologically exploited by activation of the LXR pathway.

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  • [Copyright] Copyright © 2017 The Author(s). Published by Elsevier Inc. All rights reserved.
  • (PMID = 28147278.001).
  • [ISSN] 2211-1247
  • [Journal-full-title] Cell reports
  • [ISO-abbreviation] Cell Rep
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; CD38 / LXR / NAD / bacterial infection / cytoskeleton / macrophage / nuclear receptor
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4. Sato Y, Kinoshita M, Takemura S, Tanaka S, Hamano G, Nakamori S, Fujikawa M, Sugawara Y, Yamamoto T, Arimoto A, Yamamura M, Sasaki M, Harada K, Nakanuma Y, Kubo S: The PD-1/PD-L1 axis may be aberrantly activated in occupational cholangiocarcinoma. Pathol Int; 2017 Mar;67(3):163-170
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [MeSH-major] Antigens, CD274 / biosynthesis. Bile Duct Neoplasms / pathology. Cholangiocarcinoma / pathology. Occupational Diseases / pathology. Programmed Cell Death 1 Receptor / biosynthesis

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  • [Copyright] © 2017 Japanese Society of Pathology and John Wiley & Sons Australia, Ltd.
  • (PMID = 28139862.001).
  • [ISSN] 1440-1827
  • [Journal-full-title] Pathology international
  • [ISO-abbreviation] Pathol. Int.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Australia
  • [Chemical-registry-number] 0 / Antigens, CD274; 0 / CD274 protein, human; 0 / PDCD1 protein, human; 0 / Programmed Cell Death 1 Receptor; 0 / Solvents
  • [Keywords] NOTNLM ; immune escape / multistep carcinogenesis / occupational cholangiocarcinoma / organic solvent exposure
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5. Dócs K, Mészár Z, Gonda S, Kiss-Szikszai A, Holló K, Antal M, Hegyi Z: The Ratio of 2-AG to Its Isomer 1-AG as an Intrinsic Fine Tuning Mechanism of CB1 Receptor Activation. Front Cell Neurosci; 2017;11:39
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  • [Title] The Ratio of 2-AG to Its Isomer 1-AG as an Intrinsic Fine Tuning Mechanism of CB1 Receptor Activation.

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  • (PMID = 28265242.001).
  • [Journal-full-title] Frontiers in cellular neuroscience
  • [ISO-abbreviation] Front Cell Neurosci
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; 1-AG / 2-AG / CB1 / calcium signaling / cannabinoid / modulation
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6. Elmeligie S, Ahmed EM, Abuel-Maaty SM, Zaitone SA, Mikhail DS: Design and Synthesis of Pyridazine Containing Compounds with Promising Anticancer Activity. Chem Pharm Bull (Tokyo); 2017;65(3):236-247
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  • All the synthesized compounds were screened for their cytotoxic activity in vitro on colon cancer cell line (HCT-116) and breast cancer cell line (MCF-7).
  • The in vitro vascular endothelial growth factor receptor (VEGFR) enzyme inhibition assay was carried out for the most active compounds at a single dose of 10 µM.

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  • (PMID = 28250345.001).
  • [ISSN] 1347-5223
  • [Journal-full-title] Chemical & pharmaceutical bulletin
  • [ISO-abbreviation] Chem. Pharm. Bull.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Japan
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7. Di Giglio MG, Muttenthaler M, Harpsøe K, Liutkeviciute Z, Keov P, Eder T, Rattei T, Arrowsmith S, Wray S, Marek A, Elbert T, Alewood PF, Gloriam DE, Gruber CW: Development of a human vasopressin V&lt;sub&gt;1a&lt;/sub&gt;-receptor antagonist from an evolutionary-related insect neuropeptide. Sci Rep; 2017 Feb 01;7:41002
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  • [Title] Development of a human vasopressin V<sub>1a</sub>-receptor antagonist from an evolutionary-related insect neuropeptide.
  • We isolated the insect oxytocin/vasopressin orthologue inotocin from the black garden ant (Lasius niger), identified and cloned its cognate receptor and determined its pharmacological properties on the insect and human oxytocin/vasopressin receptors.
  • The Arg8/D-Arg8 ligand-pair was further investigated to gain novel insights into the oxytocin/vasopressin peptide-receptor interaction, which led to the identification of key residues of the receptors that are important for ligand functionality and selectivity.
  • These observations could play an important role for development of oxytocin/vasopressin receptor modulators that would enable clear distinction of the physiological and pathological responses of the individual receptor subtypes.

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  • (PMID = 28145450.001).
  • [ISSN] 2045-2322
  • [Journal-full-title] Scientific reports
  • [ISO-abbreviation] Sci Rep
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
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8. Keller AN, Eckle SB, Xu W, Liu L, Hughes VA, Mak JY, Meehan BS, Pediongco T, Birkinshaw RW, Chen Z, Wang H, D'Souza C, Kjer-Nielsen L, Gherardin NA, Godfrey DI, Kostenko L, Corbett AJ, Purcell AW, Fairlie DP, McCluskey J, Rossjohn J: Drugs and drug-like molecules can modulate the function of mucosal-associated invariant T cells. Nat Immunol; 2017 Apr;18(4):402-411
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  • Here we identified a range of small organic molecules, drugs, drug metabolites and drug-like molecules, including salicylates and diclofenac, as MR1-binding ligands.
  • Crystal structures of a T cell antigen receptor (TCR) from a MAIT cell in complex with MR1 bound to the non-stimulatory and stimulatory compounds showed distinct ligand orientations and contacts within MR1, which highlighted the versatility of the MR1 binding pocket.
  • This indicated that drugs and drug-like molecules can modulate MAIT cell function in mammals.

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  • (PMID = 28166217.001).
  • [ISSN] 1529-2916
  • [Journal-full-title] Nature immunology
  • [ISO-abbreviation] Nat. Immunol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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9. Huo X, Wang C, Yu Z, Peng Y, Wang S, Feng S, Zhang S, Tian X, Sun C, Liu K, Deng S, Ma X: Human transporters, PEPT1/2, facilitate melatonin transportation into mitochondria of cancer cells: an implication of the therapeutic potential. J Pineal Res; 2017 Jan 18;
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Several functions of melatonin are mediated by its membrane receptors but others are receptor-independent.
  • In the current study, it was identified that melatonin and its sulfation metabolites were the substrates of oligopeptide transporter (PEPT) 1/2 and organic anion transporter (OAT) 3, respectively.
  • For the first time, PEPT1/2 were identified to localize in the mitochondrial membrane of human cancer cell lines of PC3 and U118.
  • Thus, PEPT1/2 can potentially be used as a cancer cell-targeted melatonin delivery system to improve the therapeutic effects of melatonin in cancer treatment.

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  • [Copyright] This article is protected by copyright. All rights reserved.
  • (PMID = 28099762.001).
  • [ISSN] 1600-079X
  • [Journal-full-title] Journal of pineal research
  • [ISO-abbreviation] J. Pineal Res.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; PEPT1/2 / apoptosis / cancer / melatonin / mitochondria / transporters
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10. Van den Bossche L, Borsboom D, Devriese S, Van Welden S, Holvoet T, Devisscher L, Hindryckx P, De Vos M, Laukens D: Tauroursodeoxycholic acid protects bile acid homeostasis under inflammatory conditions and dampens Crohn's disease-like ileitis. Lab Invest; 2017 Feb 06;
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  • We investigated whether tauroursodeoxycholic acid (TUDCA), a secondary bile acid with cytoprotective properties, regulates ileal nuclear receptor and bile acid transporter expression and assessed its therapeutic potential in an experimental model of Crohn's disease (CD).
  • Gene expression of the nuclear receptors farnesoid X receptor, pregnane X receptor and vitamin D receptor and the bile acid transporters apical sodium-dependent bile acid transporter and organic solute transporter α and β was analyzed in Caco-2 cell monolayers exposed to tumor necrosis factor (TNF)α, in ileal tissue of TNF<sup>ΔARE/WT</sup> mice and in inflamed ileal biopsies from CD patients by quantitative real-time polymerase chain reaction.
  • Exposing Caco-2 cell monolayers to TNFα impaired the mRNA expression of nuclear receptors and bile acid transporters, whereas co-incubation with TUDCA antagonized their downregulation.

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  • (PMID = 28165466.001).
  • [ISSN] 1530-0307
  • [Journal-full-title] Laboratory investigation; a journal of technical methods and pathology
  • [ISO-abbreviation] Lab. Invest.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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11. Huang L, Wang Y, Ling X, Chaurasiya B, Yang C, Du Y, Tu J, Xiong Y, Sun C: Efficient delivery of paclitaxel into ASGPR over-expressed cancer cells using reversibly stabilized multifunctional pullulan nanoparticles. Carbohydr Polym; 2017 Mar 01;159:178-187
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  • Pull-LA-CLNPs showed high stability against extensive dilution, high salt concentration and organic solvent.
  • Asialoglycoprotein receptor (ASGPR) competitive inhibition and intracellular distribution studies performed by flow cytometer, fluorescence microscope and confocal laser scanning microscopy (CLSM) showed that Pull-LA-NPs could be efficiently taken up by the cells via ASGPR-mediated endocytosis and mainly distributed in cytoplasm.
  • In conclusion, Pull-LA-CLNPs is a promisingly safe, biodegradable and cell-specific nano-carrier to deliver lipophilic anticancer drugs.

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  • [Copyright] Copyright © 2016 Elsevier Ltd. All rights reserved.
  • (PMID = 28038747.001).
  • [ISSN] 1879-1344
  • [Journal-full-title] Carbohydrate polymers
  • [ISO-abbreviation] Carbohydr Polym
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; Disulfide bonds / Pullulan / Reducing sensitivity / Reversible core-crosslinking / Self-targeting
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12. Elshenawy OH, Abdelhamid G, Soshilov AA, Denison MS, El-Kadi AO: Down-regulation of cytochrome P450 1A1 by monomethylarsonous acid in human HepG2 cells. Toxicol Lett; 2017 Mar 15;270:34-50
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  • Arsenic is capable of modulating the expression of aryl hydrocarbon receptor (AhR)-regulated genes, nevertheless, whether its trivalent organic metabolites have similar effects or not need to be investigated.
  • [MeSH-minor] Arsenites / toxicity. Basic Helix-Loop-Helix Transcription Factors / genetics. Basic Helix-Loop-Helix Transcription Factors / metabolism. Cell Survival / drug effects. Heme Oxygenase-1 / genetics. Heme Oxygenase-1 / metabolism. Hep G2 Cells. Humans. Oxidative Stress / drug effects. Polychlorinated Dibenzodioxins / toxicity. Protein Processing, Post-Translational. Protein Stability / drug effects. RNA, Messenger / genetics. RNA, Messenger / metabolism. Reactive Oxygen Species / metabolism. Receptors, Aryl Hydrocarbon / genetics. Receptors, Aryl Hydrocarbon / metabolism. Signal Transduction. Sodium Compounds / toxicity

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28189647.001).
  • [ISSN] 1879-3169
  • [Journal-full-title] Toxicology letters
  • [ISO-abbreviation] Toxicol. Lett.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / AHR protein, human; 0 / Arsenites; 0 / Basic Helix-Loop-Helix Transcription Factors; 0 / Organometallic Compounds; 0 / Polychlorinated Dibenzodioxins; 0 / RNA, Messenger; 0 / Reactive Oxygen Species; 0 / Receptors, Aryl Hydrocarbon; 0 / Sodium Compounds; 0 / monomethylarsonous acid; 48OVY2OC72 / sodium arsenite; EC 1.14.14.1 / CYP1A1 protein, human; EC 1.14.14.1 / Cytochrome P-450 CYP1A1; EC 1.14.14.18 / HMOX1 protein, human; EC 1.14.14.18 / Heme Oxygenase-1
  • [Keywords] NOTNLM ; Arsenite / Aryl hydrocarbon receptor / CYP1A1 / Free radicals / Monomethylarsonous acid / ROS / XRE
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13. Mitchell RF, Hall LP, Reagel PF, McKenna DD, Baker TC, Hildebrand JG: Odorant receptors and antennal lobe morphology offer a new approach to understanding olfaction in the Asian longhorned beetle. J Comp Physiol A Neuroethol Sens Neural Behav Physiol; 2017 Feb;203(2):99-109
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  • Traps baited with an attractive mixture of volatile organic compounds from hosts have been of limited success in monitoring invasion sites.

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  • (PMID = 28078425.001).
  • [ISSN] 1432-1351
  • [Journal-full-title] Journal of comparative physiology. A, Neuroethology, sensory, neural, and behavioral physiology
  • [ISO-abbreviation] J. Comp. Physiol. A Neuroethol. Sens. Neural. Behav. Physiol.
  • [Language] eng
  • [Grant] United States / NIGMS NIH HHS / GM / K12 GM000708
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; Anoplophora glabripennis / Antennal lobe morphology / Cerambycidae / Olfactory receptor / Pheromone
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14. Řezníčková E, Tenora L, Pospíšilová P, Galeta J, Jorda R, Berka K, Majer P, Potáček M, Kryštof V: ALK5 kinase inhibitory activity and synthesis of 2,3,4-substituted 5,5-dimethyl-5,6-dihydro-4H-pyrrolo[1,2-b]pyrazoles. Eur J Med Chem; 2017 Feb 15;127:632-642
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [MeSH-minor] Cell Line, Tumor. Chemistry Techniques, Synthetic. Humans. Structure-Activity Relationship

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  • [Copyright] Copyright © 2017 Elsevier Masson SAS. All rights reserved.
  • (PMID = 28135685.001).
  • [ISSN] 1768-3254
  • [Journal-full-title] European journal of medicinal chemistry
  • [ISO-abbreviation] Eur J Med Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] France
  • [Chemical-registry-number] 0 / Protein Kinase Inhibitors; 0 / Pyrazoles; 0 / Receptors, Transforming Growth Factor beta; EC 2.7.1.11 / TGF-beta type I receptor; EC 2.7.11.1 / Protein-Serine-Threonine Kinases
  • [Keywords] NOTNLM ; Inhibitor / Protein kinase / Substituted pyrrolo[1,2-b]pyrazoles / Transforming growth factor beta receptor I
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15. LeVan TD, Smith LM, Heires AJ, Mikuls TR, Meza JL, Weissenburger-Moser LA, Romberger DJ: Interaction of CD14 haplotypes and soluble CD14 on pulmonary function in agricultural workers. Respir Res; 2017 Mar 16;18(1):49
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • BACKGROUND: Agricultural environments are contaminated with organic dusts containing bacterial components.
  • Chronic inhalation of organic dusts is implicated in respiratory diseases.
  • CD14 is a critical receptor for gram-negative lipopolysaccharide; however, its association with respiratory disease among agricultural workers is unknown.

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  • (PMID = 28302109.001).
  • [ISSN] 1465-993X
  • [Journal-full-title] Respiratory research
  • [ISO-abbreviation] Respir. Res.
  • [Language] eng
  • [Grant] United States / CSRD VA / CX / I01 CX000434
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; Agriculture / CD14 / COPD / Lung function / Polymorphism
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16. Deng T, Peng Y, Zhang R, Wang J, Zhang J, Gu Y, Huang D, Deng D: Water-Solubilizing Hydrophobic ZnAgInSe/ZnS QDs with Tumor-Targeted cRGD-Sulfobetaine-PIMA-Histamine Ligands via a Self-Assembly Strategy for Bioimaging. ACS Appl Mater Interfaces; 2017 Mar 23;
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  • Exploring the organic-to-aqueous phase transfer of quantum dots (QDs) is significant for achieving their versatile applications in biomedical fields.
  • Herein, the new highly fluorescent tumor-targeted QDs-clusters consisting of ZnAgInSe/ZnS (ZAISe/ZnS) QDs and sulfobetaine-PIMA-histamine (SPH) polymer with the α<sub>ν</sub>β<sub>3</sub> integrin receptor cyclic RGD (c-RGD) were developed via ligand exchange and an accompanying self-assembly process.
  • In the meantime, those clusters also recognized and enriched the cell surface when cocultured with the α<sub>ν</sub>β<sub>3</sub> integrin receptor overexpressed malignant cells (U87MG tumor).

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  • (PMID = 28293947.001).
  • [ISSN] 1944-8252
  • [Journal-full-title] ACS applied materials & interfaces
  • [ISO-abbreviation] ACS Appl Mater Interfaces
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; QDs-clusters / optical imaging / quaternary quantum dots / self-assembly / tumor targeting polymer
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17. Gilligan LC, Gondal A, Tang V, Hussain MT, Arvaniti A, Hewitt AM, Foster PA: Estrone Sulfate Transport and Steroid Sulfatase Activity in Colorectal Cancer: Implications for Hormone Replacement Therapy. Front Pharmacol; 2017;8:103
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Here, we show that a panel of CRC cell lines (Colo205, Caco2, HCT116, HT-29) have steroid sulfatase (STS) activity, and thus can hydrolyze E<sub>1</sub>S.
  • STS activity is significantly higher in CRC cell lysate, suggesting the importance of E<sub>1</sub>S transport in intracellular STS substrate availability.
  • As E<sub>1</sub>S transport is regulated by the expression pattern of certain solute carrier organic anion transporter polypeptides, we show that in CRC OATP4A1 is the most abundantly expressed transporter.
  • All four CRC cell lines rapidly transported E<sub>1</sub>S into cells, with this effect significantly inhibited by the competitive OATP inhibitor BSP.
  • Examination of estrogen receptor status showed ERα was present in Colo205 and Caco2 cells.
  • Intriguingly, HCT116 and HT29 cells strongly expressed the G protein coupled estrogen receptor (GPER), and that stimulation of this receptor with estradiol (E<sub>2</sub>) and G1, a GPER agonist, significantly (<i>p</i> < 0.01) increased STS activity.

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  • (PMID = 28326039.001).
  • [Journal-full-title] Frontiers in pharmacology
  • [ISO-abbreviation] Front Pharmacol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; GPER / OATP / SLCO / colorectal cancer / estrogen / steroid sulfatase / tamoxifen
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18. Dai Y, Huo X, Zhang Y, Yang T, Li M, Xu X: Elevated lead levels and changes in blood morphology and erythrocyte CR1 in preschool children from an e-waste area. Sci Total Environ; 2017 Mar 13;592:51-59
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Improper dismantling and combustion of electronic waste (e-waste) may release persistent organic pollutants and heavy metals that possess potential risk for human health.
  • The aim of the study was to investigate the effect of Pb exposure on blood morphology and erythrocyte complement receptor 1 (CR1) levels as related to immunologic function in preschool children.

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28301822.001).
  • [ISSN] 1879-1026
  • [Journal-full-title] The Science of the total environment
  • [ISO-abbreviation] Sci. Total Environ.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Electronic waste / Erythrocyte complement receptor type 1 / Erythrocyte immunity / Lead / Preschool children
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19. Ziarek JJ, Kleist AB, London N, Raveh B, Montpas N, Bonneterre J, St-Onge G, DiCosmo-Ponticello CJ, Koplinski CA, Roy I, Stephens B, Thelen S, Veldkamp CT, Coffman FD, Cohen MC, Dwinell MB, Thelen M, Peterson FC, Heveker N, Volkman BF: Structural basis for chemokine recognition by a G protein-coupled receptor and implications for receptor activation. Sci Signal; 2017 Mar 21;10(471)
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Structural basis for chemokine recognition by a G protein-coupled receptor and implications for receptor activation.
  • Chemokines orchestrate cell migration for development, immune surveillance, and disease by binding to cell surface heterotrimeric guanine nucleotide-binding protein (G protein)-coupled receptors (GPCRs).
  • The receptor CXCR4 recognizes both monomeric and dimeric forms of the chemokine CXCL12, which is a distinct example of ligand bias in the chemokine family.
  • We demonstrated that a constitutively monomeric CXCL12 variant reproduced the G protein-dependent and β-arrestin-dependent responses that are associated with normal CXCR4 signaling and lead to cell migration.
  • In addition, monomeric CXCL12 made specific contacts with CXCR4 that are not present in the structure of the receptor in complex with a dimeric form of CXCL12, a biased agonist that stimulates only G protein-dependent signaling.
  • We produced an experimentally validated model of an agonist-bound chemokine receptor that merged a nuclear magnetic resonance-based structure of monomeric CXCL12 bound to the amino terminus of CXCR4 with a crystal structure of the transmembrane domains of CXCR4.
  • The large CXCL12:CXCR4 protein-protein interface revealed by this structure identified previously uncharacterized functional interactions that fall outside of the classical "two-site model" for chemokine-receptor recognition.
  • Our model suggests a mechanistic hypothesis for how interactions on the extracellular face of the receptor may stimulate the conformational changes required for chemokine receptor-mediated signal transduction.

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  • [Copyright] Copyright © 2017, American Association for the Advancement of Science.
  • (PMID = 28325822.001).
  • [ISSN] 1937-9145
  • [Journal-full-title] Science signaling
  • [ISO-abbreviation] Sci Signal
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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20. Kostarnoy AV, Gancheva PG, Lepenies B, Tukhvatulin AI, Dzharullaeva AS, Polyakov NB, Grumov DA, Egorova DA, Kulibin AY, Bobrov MA, Malolina EA, Zykin PA, Soloviev AI, Riabenko E, Maltseva DV, Sakharov DA, Tonevitsky AG, Verkhovskaya LV, Logunov DY, Naroditsky BS, Gintsburg AL: Receptor Mincle promotes skin allergies and is capable of recognizing cholesterol sulfate. Proc Natl Acad Sci U S A; 2017 Mar 14;
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Receptor Mincle promotes skin allergies and is capable of recognizing cholesterol sulfate.
  • Here, we show that cholesterol sulfate, a molecule present in relatively high concentrations in the epithelial layer of barrier tissues, is selectively recognized by Mincle (Clec4e), a C-type lectin receptor of the innate immune system that is strongly up-regulated in response to skin damage.
  • In a well-established model of allergic contact dermatitis, the absence of Mincle leads to a significant suppression of the magnitude of the skin inflammatory response as assessed by changes in ear thickness, myeloid cell infiltration, and cytokine and chemokine secretion.

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  • (PMID = 28292894.001).
  • [ISSN] 1091-6490
  • [Journal-full-title] Proceedings of the National Academy of Sciences of the United States of America
  • [ISO-abbreviation] Proc. Natl. Acad. Sci. U.S.A.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Mincle / allergy / cholesterol sulfate / innate immunity / sterile inflammation
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21. Kobayashi T, Koizumi T, Kobayashi M, Ogura J, Horiuchi Y, Kimura Y, Kondo A, Furugen A, Narumi K, Takahashi N, Iseki K: Insulin stimulates transport of organic anion compounds mediated by organic anion transporting polypeptide 2B1 in the human intestinal cell line Caco-2. Drug Metab Pharmacokinet; 2016 Dec 27;
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Insulin stimulates transport of organic anion compounds mediated by organic anion transporting polypeptide 2B1 in the human intestinal cell line Caco-2.
  • Organic anion transporting polypeptide 2B1 (OATP2B1) is the major uptake transporter in the intestine, and transports various clinically used therapeutic agents.
  • Insulin acts through the insulin receptor in targeted cells, and Rab8A is one of the insulin signaling pathways.
  • The small intestine in humans also expresses insulin receptor and Rab8A.
  • Caco-2 cells treated with insulin showed increased OATP2B1 expression at the cell surface.

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  • [Copyright] Copyright © 2016 The Japanese Society for the Study of Xenobiotics. Published by Elsevier Ltd. All rights reserved.
  • (PMID = 28318878.001).
  • [ISSN] 1880-0920
  • [Journal-full-title] Drug metabolism and pharmacokinetics
  • [ISO-abbreviation] Drug Metab. Pharmacokinet.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; Caco-2 cell / Estrone-3-sulfate / Insulin / Intestinal absorption / OATP2B1
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22. Hanauer T, Hopkinson RJ, Patel K, Li Y, Correddu D, Kawamura A, Sarojini V, Leung IK, Gruber T: Selective recognition of the di/trimethylammonium motif by an artificial carboxycalixarene receptor. Org Biomol Chem; 2017 Feb 01;15(5):1100-1105
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Selective recognition of the di/trimethylammonium motif by an artificial carboxycalixarene receptor.
  • We report a simple carboxycalixarene that selectively binds molecules containing di/trimethylammonium moieties in isolation, in cell lysates and when incorporated in histone peptides.

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  • (PMID = 28091667.001).
  • [ISSN] 1477-0539
  • [Journal-full-title] Organic & biomolecular chemistry
  • [ISO-abbreviation] Org. Biomol. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
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23. Mitra S, Sasmal HS, Kundu T, Kandambeth S, Illath K, Díaz Díaz D, Banerjee R: Targeted Drug Delivery in Covalent Organic Nanosheets (CONs) via Sequential Postsynthetic Modification. J Am Chem Soc; 2017 Mar 16;
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Targeted Drug Delivery in Covalent Organic Nanosheets (CONs) via Sequential Postsynthetic Modification.
  • Covalent organic nanosheets (CONs) have emerged as a new class of functional two-dimensional (2D) porous organic polymeric materials with a high accessible surface, diverse functionality, and chemical stability.
  • In order to meet this requirement, we have developed a facile, salt-mediated synthesis of covalent organic frameworks (COFs) in the presence of p-toluenesulfonic acid (PTSA).
  • Targeted CONs showed sustained release of the drug to the cancer cells through receptor-mediated endocytosis, which led to cancer cell death via apoptosis.

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  • (PMID = 28256830.001).
  • [ISSN] 1520-5126
  • [Journal-full-title] Journal of the American Chemical Society
  • [ISO-abbreviation] J. Am. Chem. Soc.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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24. Rosa M, Gonzalez-Nunez V, Barreto-Valer K, Marcelo F, Sánchez-Sánchez J, Calle LP, Arévalo JC, Rodríguez RE, Jiménez-Barbero J, Arsequell G, Valencia G: Role of the sugar moiety on the opioid receptor binding and conformation of a series of enkephalin neoglycopeptides. Bioorg Med Chem; 2017 Apr 01;25(7):2260-2265
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Role of the sugar moiety on the opioid receptor binding and conformation of a series of enkephalin neoglycopeptides.

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  • [Copyright] Copyright © 2017 Elsevier Ltd. All rights reserved.
  • (PMID = 28284867.001).
  • [ISSN] 1464-3391
  • [Journal-full-title] Bioorganic & medicinal chemistry
  • [ISO-abbreviation] Bioorg. Med. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; Enkephalin-related / Glycosylation / Neoglycopeptides / Neuropeptide / Opioid receptors / Pharmacology
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25. Zhang Y, Guo X, Zheng M, Yang R, Yang H, Jia L, Yang M: A 4,5-quinolimide-based fluorescent sensor for the turn-on detection of Cd&lt;sup&gt;2+&lt;/sup&gt; with live-cell imaging. Org Biomol Chem; 2017 Feb 21;
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] A 4,5-quinolimide-based fluorescent sensor for the turn-on detection of Cd<sup>2+</sup> with live-cell imaging.
  • : A 4,5-quinolimide derivative, BNA, bearing the amide-DPA receptor, was synthesized as a turn-on fluorescent sensor for Cd<sup>2+</sup>.

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  • (PMID = 28221392.001).
  • [ISSN] 1477-0539
  • [Journal-full-title] Organic & biomolecular chemistry
  • [ISO-abbreviation] Org. Biomol. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
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26. Morales P, Hurst DP, Reggio PH: Molecular Targets of the Phytocannabinoids: A Complex Picture. Prog Chem Org Nat Prod; 2017;103:103-131
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  • [Title] Molecular Targets of the Phytocannabinoids: A Complex Picture.
  • : For centuries, hashish and marihuana, both derived from the Indian hemp Cannabis sativa L., have been used for their medicinal, as well as, their psychotropic effects.
  • These effects are associated with the phytocannabinoids which are oxygen containing C<sub>21</sub> aromatic hydrocarbons found in Cannabis sativa L.
  • To date, over 120 phytocannabinoids have been isolated from Cannabis.
  • For many years, it was assumed that the beneficial effects of the phytocannabinoids were mediated by the cannabinoid receptors, CB<sub>1</sub> and CB<sub>2</sub>.
  • However, today we know that the picture is much more complex, with the same phytocannabinoid acting at multiple targets.
  • This contribution focuses on the molecular pharmacology of the phytocannabinoids, including Δ<sup>9</sup>-THC and CBD, from the prospective of the targets at which these important compounds act.

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  • (PMID = 28120232.001).
  • [ISSN] 2191-7043
  • [Journal-full-title] Progress in the chemistry of organic natural products
  • [ISO-abbreviation] Prog Chem Org Nat Prod
  • [Language] eng
  • [Grant] United States / NIDA NIH HHS / DA / K05 DA021358; United States / NIDA NIH HHS / DA / R01 DA003934
  • [Publication-type] Journal Article
  • [Publication-country] Austria
  • [Keywords] NOTNLM ; CB1 receptor / CB2 receptor / CBC / CBD / CBDV / CBE / CBG / CBL / CBN / CBND / CBT / CBV / GPCR / Glycine receptor / PPARγ / Phytocannabinoid / THCV / TRPA1 channel / TRPM8 channel / TRPV1 channel / Δ8-THC / Δ9-THC
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27. Sapudom J, Ullm F, Martin S, Kalbitzer L, Naab J, Möller S, Schnabelrauch M, Anderegg U, Schmidt S, Pompe T: Molecular weight specific impact of soluble and immobilized hyaluronan on CD44 expressing melanoma cells in 3D collagen matrices. Acta Biomater; 2017 Mar 01;50:259-270
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  • : Hyaluronan (HA) and its principal receptor CD44 are known to be involved in regulating tumor cell dissemination and metastasis.
  • To elucidate HA dependent tumor cell behavior, BRO melanoma cell lines with and without CD44 receptor expression were used for in vitro cell experiments.
  • We demonstrated that only soluble LMW-HA promoted cell proliferation in a CD44 dependent manner, while HMW-HA and immobilized LMW-HA did not.
  • Furthermore, an enhanced cell invasion was found only for immobilized LMW-HA.
  • Both findings correlated with a very strong and specific adhesive interaction of LMW-HA and CD44+ cells quantified in single cell adhesion measurements using soft colloidal force spectroscopy.
  • Mimicking in that way important in vivo features of tumor microenvironments, we found that only low molecular weight HA (LMW-HA) in soluble form promoted proliferation of a melanoma cell line (BRO), while it enhanced cell invasion in bound form.
  • The molecular weight specificity of LMW-HA was verified to be CD44 receptor dependent and was correlated to adhesive ligand-receptor interactions in quantitative colloidal force spectroscopy at single cell level.

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  • [Copyright] Copyright © 2016 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.
  • (PMID = 27965172.001).
  • [ISSN] 1878-7568
  • [Journal-full-title] Acta biomaterialia
  • [ISO-abbreviation] Acta Biomater
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; CD44 receptor / Collagen / Extracellular matrix / Hyaluronan / Melanoma cells
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28. Zhang L, Dai F, Cui L, Zhou B, Guo Y: Up-regulation of the active form of small GTPase Rab13 promotes macroautophagy in vascular endothelial cells. Biochim Biophys Acta; 2017 Apr;1864(4):613-624
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  • The importance of macroautophagy (hereafter referred to as autophagy) in vascular endothelial cell (VEC) biology and dysfunction is increasingly recognized, but the molecular mechanisms of autophagy in VECs in the presence of serum are still poorly understood.
  • Using a combination of immunofluorescence and co-immunoprecipitation (co-IP) assays, we demonstrated that pterostilbene or up-regulation of the active form of Rab13 promoted the interaction between Rab13 and growth factor receptor-bound protein 2 (Grb2).

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28087344.001).
  • [ISSN] 0006-3002
  • [Journal-full-title] Biochimica et biophysica acta
  • [ISO-abbreviation] Biochim. Biophys. Acta
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; AMP-activated protein kinase / Growth factor receptor-bound protein 2 / Macroautophagy / Pterostilbene / Small GTPase Rab13 / Vascular endothelial cell
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29. Sharma N, Bhagat S, Chundawat TS: Recent Advances in Development of GPR40 Modulators (FFA1/ FFAR1): An Emerging Target for Type 2 diabetes. Mini Rev Med Chem; 2017 Jan 20;
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  • : GPR40, an orphan G-protein coupled receptor that is activated by medium and long-chain fatty acids and is highly expressed in pancreatic islets, adipose depots and the gastrointestinal tract are involved in energy source recognition, absorption, storage and/or metabolism.
  • Since its deorphanization in 2003, G-protein-coupled receptor GPR40 have emerged as potential target for type II diabetes because they have been hypothesized to participate in the adverse effects of chronic fatty acid exposure on function of β-cell.

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  • (PMID = 28117025.001).
  • [ISSN] 1875-5607
  • [Journal-full-title] Mini reviews in medicinal chemistry
  • [ISO-abbreviation] Mini Rev Med Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
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30. Zahajská L, Nisler J, Voller J, Gucký T, Pospíšil T, Spíchal L, Strnad M: Preparation, characterization and biological activity of C8-substituted cytokinins. Phytochemistry; 2017 Mar;135:115-127
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  • The latter were further tested for their ability to activate the Arabidopsis cytokinin receptors AHK3 and CRE1/AHK4 in bacterial receptor activation assays.
  • Therefore, we also present and discuss the cytotoxicity of all the compounds against three normal human cell lines.

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  • [Copyright] Copyright © 2016 Elsevier Ltd. All rights reserved.
  • (PMID = 27986278.001).
  • [ISSN] 1873-3700
  • [Journal-full-title] Phytochemistry
  • [ISO-abbreviation] Phytochemistry
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Cytokinins; 0 / Plant Growth Regulators; EC 2.7.- / Protein Kinases; JAC85A2161 / Adenine
  • [Keywords] NOTNLM ; AHK3 and CRE1/AHK4 bacterial receptor assay / C8-substituted cytokinin / Cytokinin bioassay / Organic synthesis
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31. Bolhassani A, Talebi S, Anvar A: Endogenous and exogenous natural adjuvants for vaccine development. Mini Rev Med Chem; 2017 Feb 28;
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  • c) induction of potent cell-mediated immunity;.
  • Up to now, different exogenous adjuvants have been identified to boost immune responses including inorganic compounds (e.g., alum, calcium phosphate hydroxide), mineral oil, bacterial products (e.g., killed bacteria or toxoids), non-bacterial organics (e.g., squalene), detergents or Quil A, plant saponins, Freund's complete or incomplete adjuvants, and delivery systems.
  • Several main endogenous adjuvants contain cytokines (e.g., IL-1, IL-2, IL-12), chemokines, alarmins (e.g., HSPs, HMGB1), dendritic cells (DCs), toll like receptor (TLR) ligands or agonists, CpG motif, and antibodies.

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  • [Copyright] Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
  • (PMID = 28245781.001).
  • [ISSN] 1875-5607
  • [Journal-full-title] Mini reviews in medicinal chemistry
  • [ISO-abbreviation] Mini Rev Med Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Immune response / Natural Adjuvant / Vaccine
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32. Motoyama K, Nishiyama R, Maeda Y, Higashi T, Ishitsuka Y, Kondo Y, Irie T, Era T, Arima H: Synthesis of multi-lactose-appended β-cyclodextrin and its cholesterol-lowering effects in Niemann-Pick type C disease-like HepG2 cells. Beilstein J Org Chem; 2017;13:10-18
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  • These results indicate that multi-Lac-β-CD (DSL5.6) diminished intracellular cholesterol levels in NPC-like HepG2 cells via asialoglycoprotein receptor (ASGPR)-mediated endocytosis.

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  • (PMID = 28179943.001).
  • [Journal-full-title] Beilstein journal of organic chemistry
  • [ISO-abbreviation] Beilstein J Org Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; Niemann–Pick type C disease / asialoglycoprotein receptor / cholesterol / cyclodextrin / lactose
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33. Abdellatif K, Bakr R, Mehany A: Synthesis, EGFR inhibition and anti-cancer activity of new 3,6-dimethyl-1-phenyl-4-(substituted-methoxy)pyrazolo[3,4-d] pyrimidine derivatives. Anticancer Agents Med Chem; 2017 Feb 12;
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  • A new series of hybrid pyrazolo[3,4-d]pyrimidine scaffold with a heteroaryl moiety as pyrazole, oxadiazole, triazole or phthalimide moiety (14a-f, 16, 17, 19, 20) was synthesized and biologically evaluated for the cytotoxicity against human liver cancer cell line (HEPG-2), human breast cancer cell line (MCF-7) and human colon cancer cell line (HCT-116).
  • While the pyrazolo hybrid compounds (14a-f) showed good activity against HEPG-2, MCF-7 and HCT-116 cell lines (IC50 = 3.65 - 39.98, 1.45 - 54.19 and 2.00 - 50.6 µM respectively) in comparison with doxorubicin (IC50 = 5.66, 2.60 and 8.48 µM respectively), the triazolo derivatives (17, 19) showed considerable potency (IC50 = 22.20 - 54.61, 14.98 - 88.78, and 10.79 - 53.40 µM respectively), the oxadiazolo hybrid compound (16, IC50 = 149.91, 115.89 and 110.07 µM respectively) and phthalimido hybrid compound (20, IC50 = 96.02, 131.19 and 120.36 µM respectively) showed low potency.
  • The pyrazolo derivative (14d, IC50 = 3.65, 1.45 and 2.00 µM) was the most potent among all compounds against HEPG-2, MCF-7 and HCT-116 cell lines respectively.
  • Also, the hybrid pyrazolo[3,4-d]pyrimidine derivatives were evaluated for their inhibitory activity to epidermal growth factor receptor tyrosine kinase (EGFR-TK) and they showed a good inhibitory activity (IC50 = 8.27 - 19.03 µM).
  • With the exception of the pyrazolo derivative (14c, IC50 = 18.82 µM), the inhibitory activity against EGFR-TK was consistent with the in vitro cytotoxic activity against HEPG-2, MCF-7 and HCT-116 cell lines.

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  • [Copyright] Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
  • (PMID = 28270084.001).
  • [ISSN] 1875-5992
  • [Journal-full-title] Anti-cancer agents in medicinal chemistry
  • [ISO-abbreviation] Anticancer Agents Med Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; 4-d]pyrimidine / Anti-cancer activity; EGFR inhibition; pyrazolo[3
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34. Hamark C, Berntsson RP, Masuyer G, Henriksson LM, Gustafsson R, Stenmark P, Widmalm G: Glycans Confer Specificity to the Recognition of Ganglioside Receptors by Botulinum Neurotoxin A. J Am Chem Soc; 2017 Jan 11;139(1):218-230
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  • : The highly poisonous botulinum neurotoxins, produced by the bacterium Clostridium botulinum, act on their hosts by a high-affinity association to two receptors on neuronal cell surfaces as the first step of invasion.
  • The glycan motifs of gangliosides serve as initial coreceptors for these protein complexes, whereby a membrane protein receptor is bound.
  • We here propose that the glycan part of the ganglioside receptors mainly provides abundance and specificity, whereas the interaction with the membrane itself and protein receptor brings about the strong total binding of the toxin to the neuronal membrane.

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  • (PMID = 27958736.001).
  • [ISSN] 1520-5126
  • [Journal-full-title] Journal of the American Chemical Society
  • [ISO-abbreviation] J. Am. Chem. Soc.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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35. Giordano C, Rovito D, Barone I, Mancuso R, Bonofiglio D, Giordano F, Catalano S, Gabriele B, Andò S: Benzofuran-2-acetic ester derivatives induce apoptosis in breast cancer cells by upregulating p21&lt;sup&gt;Cip/WAF1&lt;/sup&gt; gene expression in p53-independent manner. DNA Repair (Amst); 2017 Mar;51:20-30
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  • We observed that benzofuran compounds bearing a phenyl or tert-butyl substituent α to the methoxycarbonyl group significantly inhibited anchorage-dependent and -independent cell growth, and induced G0/G1 cell cycle arrest in human estrogen receptor alpha positive (MCF-7 and T47D) and in triple negative MDA-MB-231 breast cancer cells, without affecting growth of MCF-10A normal breast epithelial cells.
  • Overall, we provide evidence that the newly tested benzofuran derivatives showed antiproliferative and pro-apoptotic activities against breast cancer cells regardless estrogen receptor status, suggesting their possible clinical development as anticancer agents.

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28108275.001).
  • [ISSN] 1568-7856
  • [Journal-full-title] DNA repair
  • [ISO-abbreviation] DNA Repair (Amst.)
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Anticancer activity / Benzofurans / Breast cancer / p21Cip/WAF1
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36. Meng W, Wang S, Yao L, Zhang N, Li D: Muscarinic Receptors Are Responsible for the Cholinergic Modulation of Projection Neurons in the Song Production Brain Nucleus RA of Zebra Finches. Front Cell Neurosci; 2017;11:51
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  • Our previous study showed that carbachol, a non-selective cholinergic receptor agonist, modulates the electrophysiology of RA projection neurons (PNs), indicating that cholinergic modulation of RA may play an important role in song production.
  • However, the receptor mechanisms underlying these effects are poorly understood.
  • In the present study, we investigated the electrophysiological properties of two acetylcholine receptors on the RA PNs of adult male zebra finches using <i>in vitro</i> whole-cell current clamp.

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  • (PMID = 28293176.001).
  • [Journal-full-title] Frontiers in cellular neuroscience
  • [ISO-abbreviation] Front Cell Neurosci
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; RA / cholinergic modulation / mAChR / nAChR / projection neuron / song premotor nucleus / zebra finch
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37. Vasaturo M, Fiengo L, De Tommasi N, Sabatino L, Ziccardi P, Colantuoni V, Bruno M, Cerchia C, Novellino E, Lupo A, Lavecchia A, Piaz FD: A compound-based proteomic approach discloses 15-ketoatractyligenin methyl ester as a new PPARγ partial agonist with anti-proliferative ability. Sci Rep; 2017 Jan 24;7:41273
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  • Here, we applied a chemical proteomic strategy to identify the peroxisome proliferator-activated receptor γ (PPARγ) as a molecular target of the pro-apoptotic agent 15-ketoatractyligenin methyl ester (compound 1).
  • We demonstrated that compound 1 interacts with PPARγ, forms a covalent bond with the thiol group of C285 and occupies the sub-pocket between helix H3 and the β-sheet of the ligand-binding domain (LBD) of the receptor by Surface Plasmon Resonance (SPR), mass spectrometry-based studies and docking experiments.
  • 1 displayed partial agonism of PPARγ in cell-based transactivation assays and was found to inhibit the AKT pathway, as well as its downstream targets.

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  • (PMID = 28117438.001).
  • [ISSN] 2045-2322
  • [Journal-full-title] Scientific reports
  • [ISO-abbreviation] Sci Rep
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
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38. Stevens MY, Chow SY, Estrada S, Eriksson J, Asplund V, Orlova A, Mitran B, Antoni G, Larhed M, Åberg O, Odell LR: Synthesis of &lt;sup&gt;11&lt;/sup&gt;C-labeled Sulfonyl Carbamates through a Multicomponent Reaction Employing Sulfonyl Azides, Alcohols, and [&lt;sup&gt;11&lt;/sup&gt;C]CO. ChemistryOpen; 2016 Dec;5(6):566-573
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  • The target compound was obtained in 24±10 % isolated radiochemical yield and was evaluated for binding properties in a tumor cell assay; in vivo biodistribution and imaging studies were also performed.
  • This represents the first successful radiolabeling of a non-peptide angiotensin II receptor subtype 2 agonist, C21, currently in clinical trials for the treatment of idiopathic pulmonary fibrosis.

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  • (PMID = 28032026.001).
  • [Journal-full-title] ChemistryOpen
  • [ISO-abbreviation] ChemistryOpen
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; AT2R agonists / multicomponent reactions / radiochemistry / sulfonyl azides / sulfonyl carbamates
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39. Pille J, van Lith SA, van Hest JC, Leenders WP: Self-Assembling VHH-Elastin-Like Peptides for Photodynamic Nanomedicine. Biomacromolecules; 2017 Mar 16;
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  • 7D12, a VHH against the epidermal growth factor receptor (EGFR) that is overexpressed in various cancers, has been evaluated as an effective cancer-targeting VHH in multiple studies.
  • We present proof of concept of the usability of such particles by controlled incorporation of a photosensitizer and show that the resulting nanoparticles induce EGFR-specific light-induced cell killing.

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  • (PMID = 28269985.001).
  • [ISSN] 1526-4602
  • [Journal-full-title] Biomacromolecules
  • [ISO-abbreviation] Biomacromolecules
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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40. Khatra H, Bose C, Sinha S: Discovery of hedgehog antagonists for cancer therapy. Curr Med Chem; 2017 Mar 16;
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  • Most of the reported small molecules primarily antagonize the Smoothened receptor although agents targeting Gli1 transcription factor and Shh ligand have also been discovered.
  • FDA) for the treatment of basal cell carcinoma.

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  • [Copyright] Copyright© Bentham Science Publishers; For any queries, please email at epub@benthamscience.org.
  • (PMID = 28302010.001).
  • [ISSN] 1875-533X
  • [Journal-full-title] Current medicinal chemistry
  • [ISO-abbreviation] Curr. Med. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; GLI / Hedgehog pathway / anticancer / inhibitors / small molecule / smoothened
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41. Daśko M, Przybyłowska M, Rachon J, Masłyk M, Kubiński K, Misiak M, Składanowski A, Demkowicz S: Synthesis and biological evaluation of fluorinated N-benzoyl and N-phenylacetoyl derivatives of 3-(4-aminophenyl)-coumarin-7-O-sulfamate as steroid sulfatase inhibitors. Eur J Med Chem; 2017 Mar 10;128:79-87
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  • The inhibitory effects of the synthesized compounds were tested on STS isolated from human placenta and against estrogen receptor-(ER)-positive MCF-7 and T47D cells, as well as ER-negative MDA-MB-231 and SkBr3 cancer cell lines.
  • Compound 6j exhibited the highest potency against the MCF-7 and T47D cell lines (15.9 μM and 8.7 μM, respectively).
  • The GI<sub>50</sub> values of tamoxifen (used as a reference) were 6.8; 10.6; 15.1; 12.5 μM against MCF-7, T47D, MDA-MB-231 and SkBr3 cancer cell lines, respectively.
  • Despite the slightly lower activity of compounds 1 and 2 (both in enzymatic and cell-based experiments) compared to 6g and 6j, analogues 1 and 2 proved to selectively inhibit the growth of ER- and PR-positive cell lines.

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  • [Copyright] Copyright © 2017 Elsevier Masson SAS. All rights reserved.
  • (PMID = 28152429.001).
  • [ISSN] 1768-3254
  • [Journal-full-title] European journal of medicinal chemistry
  • [ISO-abbreviation] Eur J Med Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] France
  • [Keywords] NOTNLM ; Breast cancer / Coumarin / STS inhibitors / Steroid sulfatase / Sulfamates
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42. Ramos E, Patiño P, Reiter RJ, Gil-Martín E, Marco-Contelles J, Parada E, Los Rios C, Romero A, Egea J: Ischemic brain injury: New insights on the protective role of melatonin. Free Radic Biol Med; 2017 Mar;104:32-53
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  • The plethora of physiopathological events associated with brain ischemia are regulate through multiple signaling pathways leading to the activation of oxidative stress process, Ca<sup>2+</sup> dyshomeostasis, mitochondrial dysfunction, proinflammatory mediators, excitotoxicity and/or programmed neuronal cell death.
  • Additionally, experimental evidence supports its actions to ameliorate ischemic long-term behavioural and neuronal deficits, preserving the functional integrity of the blood-brain barrier, inducing neurogenesis and cell proliferation through receptor-dependent mechanism, as well as improving synaptic transmission.

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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
  • (PMID = 28065781.001).
  • [ISSN] 1873-4596
  • [Journal-full-title] Free radical biology & medicine
  • [ISO-abbreviation] Free Radic. Biol. Med.
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Brain ischemia / Free radicals / Melatonin / Neuroprotection
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43. Kandhasamy S, Ramanathan G, Muthukumar T, Thyagarajan S, Umamaheshwari N, Santhanakrishnan VP, Sivagnanam UT, Perumal PT: Nanofibrous matrixes with biologically active hydroxybenzophenazine pyrazolone compound for cancer theranostics. Mater Sci Eng C Mater Biol Appl; 2017 May 01;74:70-85
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  • Among the compounds 5i exhibited the highest levels of inhibitory activity against both MCF-7, Hep-2 cell lines.
  • Furthermore, the compound 5i (BPP) was evaluated for DNA fragmentation, flow cytometry studies and cytotoxicity against MCF-7, Hep-2 and NIH 3T3 fibroblast cell lines.
  • In addition, molecular docking (PDB ID: 1T46) studies were performed to predict the binding affinity of ligand with receptor.
  • Moreover, the synthesized BPP compound was loaded in to the PHB-PCL nanofibrous scaffold to check the cytotoxicity against the MCF-7, Hep-2 and NIH 3T3 fibroblast cell lines.

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28254336.001).
  • [ISSN] 1873-0191
  • [Journal-full-title] Materials science & engineering. C, Materials for biological applications
  • [ISO-abbreviation] Mater Sci Eng C Mater Biol Appl
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Electrospinning / Hep-2 / MCF-7 / Nanofibrous scaffold / Nanomaterial / Tissue engineering
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44. Morita A, Ushikubo H, Mori A, Arima S, Sakamoto K, Nagamitsu T, Ishii K, Nakahara T: A delay in vascularization induces abnormal astrocyte proliferation and migration in the mouse retina. Dev Dyn; 2017 Mar;246(3):186-200
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  • RESULTS: A dose-dependent delay in retinal vascularization was observed in mice that had been treated with KRN633 (1-10 mg/kg), a VEGF receptor inhibitor, on the day of birth and on the following day.
  • CONCLUSIONS: These findings suggest that a delay in normal vascularization leads to abnormal astrocyte behavior, which results in the formation of abnormal astrocyte and endothelial cell networks in the mouse retina.

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  • [Copyright] © 2016 Wiley Periodicals, Inc.
  • (PMID = 28033674.001).
  • [ISSN] 1097-0177
  • [Journal-full-title] Developmental dynamics : an official publication of the American Association of Anatomists
  • [ISO-abbreviation] Dev. Dyn.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; astrocytes / endothelial cells / retina / vascular development / vascular endothelial growth factor
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45. Shevelev AY, Kostiukevich MV, Efremov EE, Vlasik TN, Mironova NA, Zykov KA, Kashirina NM, Kuznetsova IB, Sharf TV, Mamochkina EN, Lipatova LN, Peklo MM, Rutkevich PN, Yanushevskaya EV, Rybalkin IN, Stukalova OV, Malkina TA, Belyaeva MM, Kuznetsova TV, Tkachev GA, Zinchenko LV, Gupalo EM, Agapova OY, Yureneva-Tkhorzhevskaya TV, Rvacheva AV, Sidorova MV, Sadgyan AS, Tereshchenko SN, Golitsyn SP: [Detection of Autoantibodies Against the 1-Adrenergic Receptor in the Sera of Patients via the Competitive cell-Based Enzyme Linked Immunosorbent Assay]. Kardiologiia; 2016 Dec;56(11):61-70
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  • [Title] [Detection of Autoantibodies Against the 1-Adrenergic Receptor in the Sera of Patients via the Competitive cell-Based Enzyme Linked Immunosorbent Assay].
  • OBJECTIVE: This study aimed to assess the level of anti-1-adrenergic receptor autoantibodies in patients with ventricular arrhythmias with no signs of organic heart disease and with presence of cardiovascular pathology in comparison with a group of healthy volunteers.
  • MATERIAL AND METHODS: The study included 44 patients with ventricular arrhythmias with no signs of organic heart disease ("idiopathic"), 34 patients with diagnosed dilated cardiomyopathy (DCM) of inflammatory origin, 35 patients with coronary heart disease and ventricular arrhythmias, 12patients with coronary heart disease with no ventricular arrhythmias, and 19 healthy volunteers (control group).
  • The level of autoantibodies against the 1-adrenergic receptor was determined by the developed competitive cell-based enzyme-linked immunosorbent assay (ELISA) and by the standard ELISA using peptides corresponding to the second extracellular loop of the 1-adrenergic receptor.
  • RESULTS: Elevated level of autoantibodies detected by a competitive cell-based ELISA was observed in 62% of patients with DCM compared to 21% of healthy volunteers (p=0.0006).
  • In patients with "idiopathic" ventricular arrhythmias, the level of 1-adrenergic receptor autoantibodies was lower than in healthy subjects (p=0.003).
  • No correlation between the data from competitive cell-based ELISA and peptide-based ELISA was found.
  • CONCLUSIONS: This study demonstrated that competitive cell-based ELISA technique can be applied for detection of 1-adrenergic receptor autoantibodies.

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  • (PMID = 28290821.001).
  • [ISSN] 0022-9040
  • [Journal-full-title] Kardiologiia
  • [ISO-abbreviation] Kardiologiia
  • [Language] rus
  • [Publication-type] English Abstract; Journal Article
  • [Publication-country] Russia (Federation)
  • [Keywords] NOTNLM ; 1-adrenergic receptor / autoantibodies / competitive cell-based ELISA / dilated cardiomyopathy / ventricular arrhythmias
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46. Estrela GR, Wasinski F, Felizardo RJ, Souza LL, Câmara NO, Bader M, Araujo RC: MATE-1 modulation by kinin B1 receptor enhances cisplatin efflux from renal cells. Mol Cell Biochem; 2017 Feb 04;
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  • [Title] MATE-1 modulation by kinin B1 receptor enhances cisplatin efflux from renal cells.
  • Organic transporters have an important role to control the absorption and excretion of cisplatin in renal cells.
  • Deletion and blockage of kinin B1 receptor has already been show to protect against cisplatin-induced acute kidney injury.
  • To test whether it exerts its protective function by modulating the organic transporters in kidney, we studied kinin B1 receptor knockout mice and treatment with a receptor antagonist at basal state and in presence of cisplatin.
  • Cisplatin administration caused downregulation of renal organic transporters; in B1 receptor knockout mice, this downregulation of organic transporters in kidney was absent; and treatment by a B1 receptor antagonist attenuated the downregulation of the transporter MATE-1.
  • Moreover, kinin B1 receptor deletion and blockage at basal state resulted in higher renal expression of MATE-1.
  • Moreover we observed that kinin B1 receptor deletion and blockage result in less accumulation of platinum in renal tissue.
  • Thus, we propose that B1 receptor deletion and blockage protect the kidney from cisplatin-induced acute kidney injury by upregulating the expression of MATE-1, thereby increasing the efflux of cisplatin from renal cells.

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  • (PMID = 28161805.001).
  • [ISSN] 1573-4919
  • [Journal-full-title] Molecular and cellular biochemistry
  • [ISO-abbreviation] Mol. Cell. Biochem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Cisplatin nephrotoxicity / Kinins / Organic transporters
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47. Ferroni C, Pepe A, Kim YS, Lee S, Guerrini A, Parenti MD, Tesei A, Zamagni A, Cortesi M, Zaffaroni N, De Cesare M, Beretta GL, Trepel JB, Malhotra SV, Varchi G: 1,4-Substituted Triazoles as Nonsteroidal Anti-Androgens for Prostate Cancer Treatment. J Med Chem; 2017 Mar 20;
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  • Prostate cancer (PC) is the fifth leading cause of cancer death in men, and the androgen receptor (AR) represents the primary target for PC treatment, even though the disease frequently progresses toward androgen-independent forms.
  • In fact, compound 14d displayed promising in vitro antitumor activity toward three different prostate cancer cell lines and was able to induce 60% tumor growth inhibition of the CW22Rv1 in vivo xenograft model.

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  • (PMID = 28272894.001).
  • [ISSN] 1520-4804
  • [Journal-full-title] Journal of medicinal chemistry
  • [ISO-abbreviation] J. Med. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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48. Elkamhawy A, Park JE, Hassan AH, Ra H, Pae AN, Lee J, Park BG, Moon B, Park HM, Roh EJ: Discovery of 1-(3-(benzyloxy)pyridin-2-yl)-3-(2-(piperazin-1-yl)ethyl)urea: A new modulator for amyloid beta-induced mitochondrial dysfunction. Eur J Med Chem; 2017 Mar 10;128:56-69
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  • Among them, 1-(3-(benzyloxy)pyridin-2-yl)-3-(2-(piperazin-1-yl)ethyl)urea (5x) effectively maintained mitochondrial function and cell viabilities on ATP assay, MTT assay, and ROS assay.
  • Using CDocker algorithm, a molecular docking model presented a plausible binding mode for 5x with cyclophilin D (CypD) receptor as a major component of mPTP.

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  • [Copyright] Copyright © 2016. Published by Elsevier Masson SAS.
  • (PMID = 28152427.001).
  • [ISSN] 1768-3254
  • [Journal-full-title] European journal of medicinal chemistry
  • [ISO-abbreviation] Eur J Med Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] France
  • [Keywords] NOTNLM ; Alzheimer's disease (AD) / Mitochondrial permeability transition pore (mPTP) / Molecular docking / Pyridyl-urea / β-amyloid peptide (Aβ)
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49. Hirota Y, Nakagawa K, Mimatsu S, Sawada N, Sakaki T, Kubodera N, Kamao M, Tsugawa N, Suhara Y, Okano T: Nongenomic effects of 1α,25-dihydroxyvitamin D&lt;sub&gt;3&lt;/sub&gt; on cartilage formation deduced from comparisons between Cyp27b1 and Vdr knockout mice. Biochem Biophys Res Commun; 2017 Jan 29;483(1):359-365
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  • : The active form of vitamin D, 1α,25-dihydroxyvitamin D<sub>3</sub> (1α,25D<sub>3</sub>), plays an important role in the maintenance of calcium (Ca) homeostasis, bone formation, and cell proliferation and differentiation via nuclear vitamin D receptor (VDR).

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  • [Copyright] Copyright © 2016 The Authors. Published by Elsevier Inc. All rights reserved.
  • (PMID = 28025137.001).
  • [ISSN] 1090-2104
  • [Journal-full-title] Biochemical and biophysical research communications
  • [ISO-abbreviation] Biochem. Biophys. Res. Commun.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Bone remodeling / CYP27B1 / Genomic action / Knockout mice / VDR / Vitamin D
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50. Singh G, Singh G, Bhatti R, Gupta V, Mahajan A, Singh P, Singh Ishar MP: Rationally designed benzopyran fused isoxazolidines and derived β&lt;sup&gt;2,3,3&lt;/sup&gt;-amino alcohols as potent analgesics: Synthesis, biological evaluation and molecular docking analysis. Eur J Med Chem; 2017 Feb 15;127:210-222
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  • Further, molecular docking analysis reveals that compound 2a binds to δ-opioid receptor (DOR) with comparatively better D-score than to μ (MOR) and κ (KOR) receptors.
  • [MeSH-minor] Animals. Cell Line. Chemistry Techniques, Synthetic. Drug Design. Female. Humans. Male. Mice. Pain / drug therapy. Prostaglandin-Endoperoxide Synthases / metabolism. Protein Conformation. Receptors, Opioid / chemistry. Receptors, Opioid / metabolism

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  • [Copyright] Copyright © 2016 Elsevier Masson SAS. All rights reserved.
  • (PMID = 28063353.001).
  • [ISSN] 1768-3254
  • [Journal-full-title] European journal of medicinal chemistry
  • [ISO-abbreviation] Eur J Med Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] France
  • [Chemical-registry-number] 0 / Amino Alcohols; 0 / Analgesics; 0 / Benzopyrans; 0 / Isoxazoles; 0 / Receptors, Opioid; EC 1.14.99.1 / Prostaglandin-Endoperoxide Synthases
  • [Keywords] NOTNLM ; Antinociceptive activity / Benzopyran fused isoxazolidines / Intramolecular 1,3-dipolar cycloaddition / Opioid receptor / Reductive cleavage
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51. Tokizane K, Konishi H, Makide K, Kawana H, Nakamuta S, Kaibuchi K, Ohwada T, Aoki J, Kiyama H: Phospholipid localization implies microglial morphology and function via Cdc42 in vitro. Glia; 2017 May;65(5):740-755
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  • We demonstrate that lysophosphatidylserine (LysoPS), a kind of lysophospholipids, rapidly and substantially alters the morphology of primary cultured microglia to an in vivo-like ramified shape in a receptor independent manner.

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  • [Copyright] © 2017 Wiley Periodicals, Inc.
  • (PMID = 28181299.001).
  • [ISSN] 1098-1136
  • [Journal-full-title] Glia
  • [ISO-abbreviation] Glia
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; NF-kB / lysophospholipid / phosphatidylserine / pro-inflammatory cytokines / ramified microglia
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52. Qin HL, Leng J, Youssif BG, Amjad MW, Raja MA, Hussain MA, Hussain Z, Kazmi SN, Bukhari SN: Synthesis and mechanistic studies of curcumin analogs based oximes as potential anticancer agents. Chem Biol Drug Des; 2017 Feb 10;
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  • The findings from the antiproliferative assay using seven different human cancer cell lines provided a clear picture of structure-activity relationship.
  • The oxime analogs namely 7a and 8a showed strong antiproliferative activity against the cell lines.
  • The compounds 5a and 6a displayed potent activity on various targets such as BRAF<sup>V</sup><sup>600E</sup> and EGFR TK kinases and also exhibited strong antiproliferative activity against different cell lines hence showing potential of multifunctional anticancer agents.

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  • [Copyright] This article is protected by copyright. All rights reserved.
  • (PMID = 28186369.001).
  • [ISSN] 1747-0285
  • [Journal-full-title] Chemical biology & drug design
  • [ISO-abbreviation] Chem Biol Drug Des
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; tubulin polymerization / Natural compounds / epidermal growth factor receptor (EGFR) / multidrug resistance (MDR) / α, β-unsaturated carbonyl
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53. Koprivanacz K, Tőke O, Besztercei B, Juhász T, Radnai L, Merő B, Mihály J, Péter M, Balogh G, Vígh L, Buday L, Liliom K: The SH3 domain of Caskin1 binds to lysophosphatidic acid suggesting a direct role for the lipid in intracellular signaling. Cell Signal; 2017 Apr;32:66-75
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  • They also exert several G protein-coupled receptor-independent functions but their intracellular target proteins are mostly unknown.

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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
  • (PMID = 28104445.001).
  • [ISSN] 1873-3913
  • [Journal-full-title] Cellular signalling
  • [ISO-abbreviation] Cell. Signal.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; Caskin1 / SH3 domain / lipid signaling / lysophosphatidic acid / proline-rich motif / protein-lipid interaction
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54. Haruta M, Sussman MR: Ligand Receptor-Mediated Regulation of Growth in Plants. Curr Top Dev Biol; 2017;123:331-363
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  • [Title] Ligand Receptor-Mediated Regulation of Growth in Plants.
  • In plants, hormones include small organic molecules, as well as larger peptides and small proteins, which, as in animals, act as ligands and interact with receptor proteins to trigger rapid biochemical changes and induce the intracellular transcriptional and long-term physiological responses.
  • For example, auxins stimulate cell elongation by bringing negatively acting transcriptional repressor proteins to the proteasome to be degraded, thus unleashing the gene expression program required for increasing cell size.
  • The "dormancy" inducing hormone, ABA, binds to soluble receptor proteins and inhibits a specific class of protein phosphatases (PP2C), which activates phosphorylation signaling leading to transcriptional changes needed for the desiccation of the seeds prior to entering dormancy.
  • Recent comparative genomics studies have revealed that parasitic nematodes and pathogenic microbes produce plant peptide hormone mimics that target specific plant plasma membrane receptor-like protein kinases, thus usurping endogenous signaling pathways for their own pathogenic purposes.
  • With biochemical, genetic, and physiological analyses of the regulation of hormone receptor signal pathways, we are thus just now beginning to understand how plants optimize the development of their body shape and cope with constantly changing environmental conditions.

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  • [Copyright] © 2017 Elsevier Inc. All rights reserved.
  • (PMID = 28236971.001).
  • [ISSN] 1557-8933
  • [Journal-full-title] Current topics in developmental biology
  • [ISO-abbreviation] Curr. Top. Dev. Biol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Arabidopsis / Cell expansion / Peptide hormone / Phosphorylation / Protein kinase / Receptor-like kinase
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55. Rush MD, Walker EM, Prehna G, Burton T, van Breemen RB: Development of a Magnetic Microbead Affinity Selection Screen (MagMASS) Using Mass Spectrometry for Ligands to the Retinoid X Receptor-α. J Am Soc Mass Spectrom; 2017 Mar;28(3):479-485
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  • [Title] Development of a Magnetic Microbead Affinity Selection Screen (MagMASS) Using Mass Spectrometry for Ligands to the Retinoid X Receptor-α.
  • The screening process involves immobilization of a target protein on a magnetic microbead using a variety of possible chemistries, incubation with mixtures of molecules containing possible ligands, a washing step that removes non-bound compounds while a magnetic field retains the beads in the microtiter well, and an organic solvent release step followed by LC-MS analysis.
  • Using retinoid X receptor-α (RXRα) as an example, which is a nuclear receptor and target for anti-inflammation therapy as well as cancer treatment and prevention, a MagMASS assay was developed and compared with an existing screening assay, pulsed ultrafiltration (PUF)-MS.

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  • (PMID = 27966173.001).
  • [ISSN] 1879-1123
  • [Journal-full-title] Journal of the American Society for Mass Spectrometry
  • [ISO-abbreviation] J. Am. Soc. Mass Spectrom.
  • [Language] eng
  • [Grant] United States / NCCIH NIH HHS / AT / P50 AT000155; United States / NCCIH NIH HHS / AT / R01 AT007659; United States / NCCIH NIH HHS / AT / T32 AT007533
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Affinity selection screening / MS-based screening / Magnetic microbeads / Natural products / Pulsed ultrafiltration / Retinoid X receptor-α (RXRα)
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56. Jeong SC, Cho Y, Song MK, Lee E, Ryu JC: Epidermal growth factor receptor (EGFR)-MAPK-nuclear factor(NF)-κB-IL8: A possible mechanism of particulate matter(PM) 2.5-induced lung toxicity. Environ Toxicol; 2017 Jan 19;
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  • [Title] Epidermal growth factor receptor (EGFR)-MAPK-nuclear factor(NF)-κB-IL8: A possible mechanism of particulate matter(PM) 2.5-induced lung toxicity.
  • In this study, we investigated whether exposure to particulate matter (PM) 2.5, a PM with an aerodynamic diameter of less than 2.5 µm, enhances inflammation-related toxicity in the human respiratory system through activation of the epidermal growth factor receptor (EGFR) signaling pathway.
  • Through cytokine antibody array analysis of two extracts of PM<sub>2.5</sub> [water (W-PM<sub>2.5</sub> ) and organic (O-PM<sub>2.5</sub> ) soluble extracts] exposed to A549 (human alveolar epithelial cell), we identified eight cytokines changed their expression with W-PM<sub>2.5</sub> and three cytokines with O-PM<sub>2.5</sub> .
  • Then, in both groups, we can identify the increase in EGF receptor protein levels.

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  • [Copyright] © 2017 Wiley Periodicals, Inc.
  • (PMID = 28101945.001).
  • [ISSN] 1522-7278
  • [Journal-full-title] Environmental toxicology
  • [ISO-abbreviation] Environ. Toxicol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Cytokine / epidermal growth factor receptor (EGFR) / erlotinib / mitogen-activated protein kinase (MAPK) / particulate matter2.5(PM2.5)
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57. Helle J, Keiler AM, Zierau O, Dörfelt P, Vollmer G, Lehmann L, Chittur SV, Tenniswood M, Welsh J, Kretzschmar G: Effects of the aryl hydrocarbon receptor agonist 3-methylcholanthrene on the 17β-estradiol regulated mRNA transcriptome of the rat uterus. J Steroid Biochem Mol Biol; 2017 Mar 08;
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  • [Title] Effects of the aryl hydrocarbon receptor agonist 3-methylcholanthrene on the 17β-estradiol regulated mRNA transcriptome of the rat uterus.
  • Polycyclic aromatic hydrocarbons (PAHs) are products of incomplete combustion of organic compounds, abundant in exhaust fumes and cigarette smoke.
  • They act by binding to the aryl hydrocarbon receptor (AHR) which induces expression of phase 1 and phase 2 enzymes in the liver.
  • PAH induced AHR activation may also lead to adverse effects by modulating other pathways, for example estrogen receptor (ER) signaling in the female reproductive tract.

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  • [Copyright] Copyright © 2017 Elsevier Ltd. All rights reserved.
  • (PMID = 28285017.001).
  • [ISSN] 1879-1220
  • [Journal-full-title] The Journal of steroid biochemistry and molecular biology
  • [ISO-abbreviation] J. Steroid Biochem. Mol. Biol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; 17β-estradiol / Aryl hydrocarbon receptor / Polycyclic aromatic hydrocarbons / Uterotrophic assay / Uterus
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58. Giambartolomei GH, Arriola Benitez PC, Delpino MV: &lt;i&gt;Brucella&lt;/i&gt; and Osteoarticular Cell Activation: Partners in Crime. Front Microbiol; 2017;8:256
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  • [Title] <i>Brucella</i> and Osteoarticular Cell Activation: Partners in Crime.
  • The molecular mechanisms implicated in bone damage have been recently elucidated. <i>B. abortus</i> induces bone damage through diverse mechanisms in which TNF-α and the receptor activator of nuclear factor kappa-B ligand (RANKL)-the natural modulator of bone homeostasis are involved.
  • These bacteria inhibit bone matrix deposition by osteoblasts (the only bone cells involved in bone deposition), and modify the phenotype of these cells to produce matrix metalloproteinases (MMPs) and cytokine secretion, contributing to bone matrix degradation. <i>B. abortus</i> also affects osteoclasts (cells naturally involved in bone resorption) by inducing an increase in osteoclastogenesis and osteoclast activation; thus, increasing mineral and organic bone matrix resorption, contributing to bone damage.
  • The analysis of <i>B. abortus</i>-infected synoviocytes indicated that bacteria also replicate in their reticulum suggesting that they could use this cell type for intracellular replication during the osteoarticular localization of the disease.

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  • (PMID = 28265268.001).
  • [Journal-full-title] Frontiers in microbiology
  • [ISO-abbreviation] Front Microbiol
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; B and T cells and Brucella / osteoarticular brucellosis / osteoblast / osteoclastogenesis / synoviocyte
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59. Cardozo T, Shmelkov E, Felsovalyi K, Swetnam J, Butler T, Malaspina D, Shmelkov SV: Chemistry-based molecular signature underlying the atypia of clozapine. Transl Psychiatry; 2017 Feb 21;7(2):e1036
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  • The only organic molecular entities objectively associated with psychiatric phenotypes in humans are drugs that induce psychiatric phenotypes and drugs used for treatment of specific psychiatric conditions.
  • Here, we identified candidate biomolecules contributing to the organic basis for psychosis by deriving an in vivo biomolecule-tissue signature for the atypical pharmacologic action of the antipsychotic drug clozapine.
  • Our results suggest that D4 and CHRM1 receptor activity in specific tissues may represent underappreciated drug targets to advance the pharmacologic treatment of schizophrenia.
  • These findings may enhance our understanding of the organic basis of psychiatric disorders and help developing effective therapies.

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  • (PMID = 28221369.001).
  • [ISSN] 2158-3188
  • [Journal-full-title] Translational psychiatry
  • [ISO-abbreviation] Transl Psychiatry
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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60. Korbecki J, Baranowska-Bosiacka I, Gutowska I, Chlubek D: [Insulin-mimetic property of vanadium compounds]. Postepy Biochem; 2016;62(1):60-65
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  • : Vanadium is a transition metal which creates a number of inorganic and organic derivatives with various organic substances.
  • They have anti-tumor properties, capable of inhibiting cell proliferation at the concentrations of several micromoles.
  • As they can increase the activity of the insulin-like growth factor I receptor, they stimulate glycogen synthesis, increase the number of GLUT-4 transporters in the cell membrane and impair gluconeogenesis.
  • Thanks to their mitotic properties, low concentrations of vanadium compounds are also able to induce β cell regeneration.
  • However, the range of therapeutic concentrations is very narrow; at concentrations as low a several micromoles vanadium compounds inhibit cell proliferation and cause apoptosis, necrosis and inflammation.

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  • (PMID = 28132446.001).
  • [ISSN] 0032-5422
  • [Journal-full-title] Postepy biochemii
  • [ISO-abbreviation] Postepy Biochem.
  • [Language] pol
  • [Publication-type] English Abstract; Journal Article; Review
  • [Publication-country] Poland
  • [Keywords] NOTNLM ; diabetes mellitus / insulin / vanadium
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61. Baatrup E, Døving KB: Histochemical demonstration of mercury in the olfactory system of salmon (Salmo salar L.) following treatments with dietary methylmercuric chloride and dissolved mercuric chloride. Ecotoxicol Environ Saf; 1990 Dec;20(3):277-89
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  • The deposition of organic and inorganic mercury compounds was studied histochemically in the salmon (Salmo salar L.) olfactory system.
  • The silver grains evoked by methylmercury were localized predominantly in lysosome-like inclusions within the receptor cells, while those produced by HgCl2 exposure were situated mainly along the borders of neighboring cells.
  • The present findings that organic and inorganic mercury compounds were deposited in the olfactory system along its whole length, from the receptor cell apices to the brain, support the electrophysiological results presented elsewhere (Baatrup et al., 1990, Ecotoxicol. Environ.

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  • (PMID = 2090443.001).
  • [ISSN] 0147-6513
  • [Journal-full-title] Ecotoxicology and environmental safety
  • [ISO-abbreviation] Ecotoxicol. Environ. Saf.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] UNITED STATES
  • [Chemical-registry-number] 0 / Mercury Radioisotopes; 0 / Methylmercury Compounds; 53GH7MZT1R / Mercuric Chloride; RWZ4L3O1X0 / methylmercuric chloride
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62. Simon DT, Larsson KC, Nilsson D, Burström G, Galter D, Berggren M, Richter-Dahlfors A: An organic electronic biomimetic neuron enables auto-regulated neuromodulation. Biosens Bioelectron; 2015 Sep 15;71:359-64
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] An organic electronic biomimetic neuron enables auto-regulated neuromodulation.
  • Here, we present an organic electronic biomimetic neuron, with the capacity to precisely intervene with the underlying malfunctioning signalling pathway using endogenous substances.
  • The fundamental function of neurons, defined as chemical-to-electrical-to-chemical signal transduction, is achieved by connecting enzyme-based amperometric biosensors and organic electronic ion pumps.
  • When exceeding defined threshold concentrations, biosensor output signals, connected via custom hardware/software, activated local or distant neurotransmitter delivery from the organic electronic ion pump.
  • Changes of 20 µM glutamate or acetylcholine triggered diffusive delivery of acetylcholine, which activated cells via receptor-mediated signalling.
  • This was observed in real-time by single-cell ratiometric Ca(2+) imaging.
  • The results demonstrate the potential of the organic electronic biomimetic neuron in therapies involving long-range neuronal signalling by mimicking the function of projection neurons.

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  • [Copyright] Copyright © 2015 Elsevier B.V. All rights reserved.
  • (PMID = 25932795.001).
  • [ISSN] 1873-4235
  • [Journal-full-title] Biosensors & bioelectronics
  • [ISO-abbreviation] Biosens Bioelectron
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Ion Pumps; IY9XDZ35W2 / Glucose
  • [Keywords] NOTNLM ; Controlled drug release / Neural prosthesis / Neuromodulation / Organic electronic material
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63. Takayama H: [Creation of functional organic compounds and their applications]. Yakugaku Zasshi; 2002 Feb;122(2):127-55
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  • [Title] [Creation of functional organic compounds and their applications].
  • Our studies on creation of functional organic compounds and their applications, have focused on three areas, namely, (A) organic chemical studies on VD (vitamin D) analogues, (B) studies on solitary wasp venoms, and (C) studies on functional building blocks for organic synthesis.
  • In the first area, several novel and important vitamin D analogues were synthesized and biologically evaluated, and their high VDR (vitamin D receptor) binding affinities were discussed on the basis of conformational analysis and docking study by Molecular Mechanics Calculation to the LBD (ligand binding domain) of VDR: These compounds include 24,24-difluoro-1 alpha,25-dihydroxy-VD3 (2) (an antimetabolism agent, the first VD analogue having higher potency than the natural hormone (1)), 2 alpha-methyl-1 alpha,25-dihydroxy-VD3 (42b) (the first A-ring-modified VD analogue exhibiting stronger VDR affinity than 1) and its 20-epimer (43b) (a VD analogue having a highest HL-60 cell differentiation inducing activity with a relatively low calcemic effect), and 2 alpha-(omega-hydroxypropyl)-1 alpha,25-dihydroxy-VD3 (exceptionally high calcemic effect).
  • [MeSH-minor] Animals. Chemistry, Organic. Organic Chemistry Phenomena. Receptors, Calcitriol / metabolism. Structure-Activity Relationship

  • MedlinePlus Health Information. consumer health - Vitamin D.
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  • [ErratumIn] Yakugaku Zasshi. 2003 Jun;123(6):475-6
  • (PMID = 11857955.001).
  • [ISSN] 0031-6903
  • [Journal-full-title] Yakugaku zasshi : Journal of the Pharmaceutical Society of Japan
  • [ISO-abbreviation] Yakugaku Zasshi
  • [Language] jpn
  • [Publication-type] English Abstract; Journal Article; Review
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Bicyclo Compounds, Heterocyclic; 0 / Cyclic S-Oxides; 0 / Neurotoxins; 0 / Receptors, Calcitriol; 0 / Wasp Venoms; 1406-16-2 / Vitamin D
  • [Number-of-references] 63
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64. Ballatori N: Pleiotropic functions of the organic solute transporter Ostα-Ostβ. Dig Dis; 2011;29(1):13-7
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  • [Title] Pleiotropic functions of the organic solute transporter Ostα-Ostβ.
  • The heteromeric organic solute transporter alpha-beta (Ostα-Ostβ) is expressed at relatively high levels on the basolateral membrane of enterocytes, where it plays a critical role in the intestinal absorption of bile acids and the enterohepatic circulation.
  • Bile acids activate nuclear receptors such as the farnesoid X receptor (FXR/NR1H4), the pregnane X receptor and the vitamin D receptor, are ligands for a G-protein-coupled bile acid receptor (GPBAR1/TGR5), and can also activate protein kinases A and C as well as mitogen-activated protein kinase pathways.
  • Note that although FXR and TGR5 are thought to function primarily as bile acid receptors, they are modulated by some other sterols and select lipid metabolites, and are also widely expressed in tissues, indicating a complex interplay among diverse regulatory networks that impact critical cell and organ functions.

  • Guide to Pharmacology. gene/protein/disease-specific - SLC51 family of steroid-derived molecule transporters - overview and references .
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  • [Copyright] Copyright © 2011 S. Karger AG, Basel.
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  • (PMID = 21691099.001).
  • [ISSN] 1421-9875
  • [Journal-full-title] Digestive diseases (Basel, Switzerland)
  • [ISO-abbreviation] Dig Dis
  • [Language] ENG
  • [Grant] United States / NIEHS NIH HHS / ES / ES01247; United States / NIEHS NIH HHS / ES / P30 ES001247; United States / NIEHS NIH HHS / ES / ES07026; United States / NIEHS NIH HHS / ES / R01 ES007026; United States / NIDDK NIH HHS / DK / DK067214; United States / NIDDK NIH HHS / DK / R01 DK067214; United States / NIEHS NIH HHS / ES / T32 ES007026
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural; Review
  • [Publication-country] Switzerland
  • [Chemical-registry-number] 0 / Bile Acids and Salts; 0 / Membrane Transport Proteins; 0 / Receptors, Cytoplasmic and Nuclear; 0 / Sterols
  • [Other-IDs] NLM/ PMC3128137
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65. Liljefors T, Thelin B, Van Der Pers JN: Structure-activity relationships between stimulus molecule and response of a pheromone receptor cell in turnip moth,Agrotis segetum : Modifications of the acetate group. J Chem Ecol; 1984 Dec;10(12):1661-75
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  • [Title] Structure-activity relationships between stimulus molecule and response of a pheromone receptor cell in turnip moth,Agrotis segetum : Modifications of the acetate group.
  • The response of an antennal receptor cell of the turnip moth,Agrotis segetum, was recorded during stimulation with a series of (Z)-7-dodecenyl acetate analogs with structural variations of the acetate group.
  • The investigated receptor cell is known to be highly selective to (Z)-7-dodecenyl acetate.
  • The results indicate very strict requirements on the shape of the polar functional group, as well as on its electron distribution for a successful interaction with the antennal receptor cell.

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  • (PMID = 24318425.001).
  • [ISSN] 0098-0331
  • [Journal-full-title] Journal of chemical ecology
  • [ISO-abbreviation] J. Chem. Ecol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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66. Poole JA, Romberger DJ: Immunological and inflammatory responses to organic dust in agriculture. Curr Opin Allergy Clin Immunol; 2012 Apr;12(2):126-32
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Immunological and inflammatory responses to organic dust in agriculture.
  • PURPOSE OF REVIEW: Agriculture represents a major industry worldwide, and despite protection against the development of IgE-mediated diseases, chronic exposure to agriculture-related organic dusts is associated with an increased risk of developing respiratory disease.
  • This article will review the literature regarding new knowledge of important etiologic agents in the dusts and focus on the immunologic responses following acute and repetitive organic dust exposures.
  • Pattern recognition receptors including Toll-like receptor 4 (TLR4), TLR2 and intracellular nucleotide oligomerization domain-like receptors are partially responsible for mediating the inflammatory consequences.
  • Repeated organic dust exposures modulate innate and adaptive immune function with a resultant adaptation-like response.
  • SUMMARY: The immunological consequences of organic dust exposure in the farming industry are likely explained by the diversity of microbial motifs in dust that can elicit differing innate immune receptor signaling pathways.

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  • (PMID = 22306554.001).
  • [ISSN] 1473-6322
  • [Journal-full-title] Current opinion in allergy and clinical immunology
  • [ISO-abbreviation] Curr Opin Allergy Clin Immunol
  • [Language] ENG
  • [Grant] United States / NIEHS NIH HHS / ES / R01 ES019325-02; United States / NIOSH CDC HHS / OH / R01 OH008539-01; United States / NIEHS NIH HHS / ES / ES015522-03S1; United States / NIEHS NIH HHS / ES / K08 ES015522-05; United States / NIOSH CDC HHS / OH / R01 OH008539; United States / NIOSH CDC HHS / OH / 1 U54 OH010162-01; United States / NIEHS NIH HHS / ES / K08 ES015522-01; United States / NIEHS NIH HHS / ES / R01 ES019325; United States / NIEHS NIH HHS / ES / K08 ES015522; United States / NIOSH CDC HHS / OH / U54 OH010162
  • [Publication-type] Journal Article; Research Support, American Recovery and Reinvestment Act; Research Support, N.I.H., Extramural; Review
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Dust; 0 / Endotoxins; 0 / Receptors, Pattern Recognition; 37341-29-0 / Immunoglobulin E
  • [Other-IDs] NLM/ NIHMS355362; NLM/ PMC3292674
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67. Costa C, García-Lestón J, Costa S, Coelho P, Silva S, Pingarilho M, Valdiglesias V, Mattei F, Dall'Armi V, Bonassi S, Laffon B, Snawder J, Teixeira JP: Is organic farming safer to farmers' health? A comparison between organic and traditional farming. Toxicol Lett; 2014 Oct 15;230(2):166-76
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  • [Title] Is organic farming safer to farmers' health? A comparison between organic and traditional farming.
  • Recently, organic farming has been introduced as a consumer and environmental friendly agricultural system, although little is known about the effects on workers' health.
  • The aim of this work was to evaluate genetic damage and immunological alterations in workers of both traditional and organic farming.
  • Eighty-five farmers exposed to several pesticides, thirty-six organic farmers and sixty-one controls took part in the study.
  • Biomarkers of exposure (pyrethroids, organophosphates, carbamates, and thioethers in urine and butyrylcholinesterase activity in plasma), early effect (micronuclei in lymphocytes and reticulocytes, T-cell receptor mutation assay, chromosomal aberrations, comet assay and lymphocytes subpopulations) and susceptibility (genetic polymorphisms related to metabolism - EPHX1, GSTM1, GSTT1 and GSTP1 - and DNA repair-XRCC1 and XRCC2) were evaluated.
  • When compared to controls and organic farmers, pesticide farmers presented a significant increase of micronuclei in lymphocytes (frequency ratio, FR=2.80) and reticulocytes (FR=1.89), chromosomal aberrations (FR=2.19), DNA damage assessed by comet assay (mean ratio, MR=1.71), and a significant decrease in the proportion of B lymphocytes (MR=0.88).
  • Results were not consistent for organic farmers when compared to controls, with a 48% increase of micronuclei in lumphocytes frequency (p=0.016) contrasted by the significant decreases of TCR-Mf (p=0.001) and %T (p=0.001).
  • [MeSH-major] Occupational Exposure / adverse effects. Organic Agriculture. Pesticides / toxicity

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  • [Copyright] Copyright © 2014 Elsevier Ireland Ltd. All rights reserved.
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  • (PMID = 24576785.001).
  • [ISSN] 1879-3169
  • [Journal-full-title] Toxicology letters
  • [ISO-abbreviation] Toxicol. Lett.
  • [Language] eng
  • [Grant] United States / Intramural CDC HHS / / CC999999
  • [Publication-type] Comparative Study; Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Biomarkers; 0 / Pesticides; EC 2.5.1.- / glutathione S-transferase T1; EC 2.5.1.18 / Glutathione Transferase; EC 2.5.1.18 / glutathione S-transferase M1
  • [Other-IDs] NLM/ HHSPA713526; NLM/ PMC4532340
  • [Keywords] NOTNLM ; Biomarkers / Genotoxicity / Immunotoxicity / Organic farming / Pesticides
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68. Katow H, Yaguchi S, Kyozuka K: Serotonin stimulates [Ca2+]i elevation in ciliary ectodermal cells of echinoplutei through a serotonin receptor cell network in the blastocoel. J Exp Biol; 2007 Feb;210(Pt 3):403-12
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  • [Title] Serotonin stimulates [Ca2+]i elevation in ciliary ectodermal cells of echinoplutei through a serotonin receptor cell network in the blastocoel.
  • A full-length serotonin receptor mRNA from the 5Hthpr gene was sequenced from larvae of the sea urchin, Hemicentrotus pulcherrimus.
  • Immunohistochemistry with anti-5HThpr antibodies indicated that the protein was expressed on blastocoelar cells that comprised the major blastocoelar network (serotonin receptor cell network).
  • The calcium transient propagated as a wave at about 175 microm s(-1), but was not detectable in the serotonin receptor-positive cell network.
  • In larvae treated with p-chlorophenylalanine, a potent and irreversible serotonin synthesis inhibitor, serotonin application did not stimulate [Ca(2+)](i), the serotonin receptor cell network did not develop properly, and the swimming behavior of the larvae was abnormal.
  • These results imply that serotonin secreted from the apical ganglion into the blastocoel stimulates the elevation of [Ca(2+)](i) in the larval ectodermal cells through the serotonin receptor cell network.
  • [MeSH-minor] Amino Acid Sequence. Animals. Base Sequence. Cilia / metabolism. Embryo, Nonmammalian / cytology. Embryo, Nonmammalian / drug effects. Embryo, Nonmammalian / metabolism. Fenclonine / pharmacology. Larva / drug effects. Larva / genetics. Larva / metabolism. Molecular Sequence Data. Neurites / drug effects. Neurites / metabolism. Organic Chemicals / analysis. Protein Structure, Tertiary. RNA, Messenger / chemistry. RNA, Messenger / metabolism. Sequence Analysis, DNA. Sequence Analysis, Protein. Serotonin Antagonists / pharmacology. Swimming / physiology

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  • (PMID = 17234609.001).
  • [ISSN] 0022-0949
  • [Journal-full-title] The Journal of experimental biology
  • [ISO-abbreviation] J. Exp. Biol.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Oregon Green BAPTA-dextran; 0 / Organic Chemicals; 0 / RNA, Messenger; 0 / Receptors, Serotonin; 0 / Serotonin Antagonists; 333DO1RDJY / Serotonin; R5J7E3L9SP / Fenclonine; SY7Q814VUP / Calcium
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69. Grung M, Lichtenthaler R, Ahel M, Tollefsen KE, Langford K, Thomas KV: Effects-directed analysis of organic toxicants in wastewater effluent from Zagreb, Croatia. Chemosphere; 2007 Feb;67(1):108-20
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  • [Title] Effects-directed analysis of organic toxicants in wastewater effluent from Zagreb, Croatia.
  • The organic toxicants present in the effluent of the main sewer of the city of Zagreb, Croatia were isolated and identified through the use of effects-directed characterisation techniques.
  • The organic load of the wastewater was isolated by solid phase extraction and toxicity profiles obtained using reverse-phase HPLC.
  • The steroid estrogens 17 beta-estradiol and estriol were identified by LC-MS/MS as estrogen receptor agonists in two of the estrogenic fractions.
  • [MeSH-minor] Animals. Cell Survival / drug effects. Cells, Cultured. Chromatography, High Pressure Liquid. Chromatography, Liquid. Croatia. Cytochrome P-450 CYP1A1 / metabolism. Environmental Monitoring / methods. Gas Chromatography-Mass Spectrometry. Mass Spectrometry. Molecular Structure. Trout / metabolism. Vitellogenins / metabolism

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  • (PMID = 17166550.001).
  • [ISSN] 0045-6535
  • [Journal-full-title] Chemosphere
  • [ISO-abbreviation] Chemosphere
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Sewage; 0 / Vitellogenins; 0 / Water Pollutants, Chemical; EC 1.14.14.1 / Cytochrome P-450 CYP1A1
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70. Anzai N, Jutabha P, Kanai Y, Endou H: Integrated physiology of proximal tubular organic anion transport. Curr Opin Nephrol Hypertens; 2005 Sep;14(5):472-9
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  • [Title] Integrated physiology of proximal tubular organic anion transport.
  • PURPOSE OF REVIEW: Renal organic anion transport proteins play important roles in the reabsorption and the secretion of endogenous and exogenous compounds.
  • RECENT FINDINGS: To date, molecular identification of organic anion transport proteins is still continuing: rodent organic anion transporter 5, organic anion-transporting polypeptide 4C1, voltage-driven organic anion transporter 1, multidrug resistance-associated protein 4, and sodium-coupled monocarboxylate transporter have yielded additional information in this field.
  • This novel aspect of renal organic anion transport, the potential modulation of signaling via dicarboxylate receptors, may be of significant relevance to renovascular hypertension and other renal diseases.
  • SUMMARY: Comprehensive understanding of the multimolecular complex, which is composed of transporters and their related signaling elements and is supported by the scaffold proteins underneath the plasma membrane, may be useful in clarifying complex transport phenomena such as renal apical organic anion handling.
  • [MeSH-minor] Animals. Carrier Proteins / metabolism. Cell Membrane / metabolism. Dicarboxylic Acids / metabolism. Humans. Ion Transport. Models, Biological. Multiprotein Complexes. Organic Anion Transporters / metabolism. Organic Cation Transport Proteins. Receptors, Cytoplasmic and Nuclear / metabolism. Signal Transduction. Sodium-Phosphate Cotransporter Proteins / metabolism

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  • (PMID = 16046907.001).
  • [ISSN] 1062-4821
  • [Journal-full-title] Current opinion in nephrology and hypertension
  • [ISO-abbreviation] Curr. Opin. Nephrol. Hypertens.
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Carrier Proteins; 0 / Dicarboxylic Acids; 0 / Multiprotein Complexes; 0 / Organic Anion Transporters; 0 / Organic Cation Transport Proteins; 0 / Receptors, Cytoplasmic and Nuclear; 0 / SLC22A12 protein, human; 0 / Sodium-Phosphate Cotransporter Proteins; 0 / diazepam-binding inhibitor receptor
  • [Number-of-references] 57
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71. Pophof B, Stange G, Abrell L: Volatile organic compounds as signals in a plant-herbivore system: electrophysiological responses in olfactory sensilla of the moth Cactoblastis cactorum. Chem Senses; 2005 Jan;30(1):51-68
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  • [Title] Volatile organic compounds as signals in a plant-herbivore system: electrophysiological responses in olfactory sensilla of the moth Cactoblastis cactorum.
  • The male sensilla trichodea house a receptor cell responding to the putative pheromone component (9Z,12E)-tetradecadienyl acetate.
  • The sensilla trichodea of the females were much shorter than those of the males and contained specialized receptor cells responding to certain terpenoids, the most frequent being the nerolidol-sensitive cell.
  • Eight volatile organic compounds emitted by Opuntia stricta, a host plant of C. cactorum, were identified using gas chromatography-mass spectrometry, beta-caryophyllene being the major compound.
  • Five compounds identified by gas chromatography in the headspace of O. stricta elicited responses in olfactory receptor cells of C. cactorum, nonanal being the most active compound and therefore a candidate attractant of C. cactorum.
  • [MeSH-major] Moths / physiology. Organic Chemicals / analysis. Pheromones / analysis. Pheromones / physiology. Plant Oils / analysis. Receptors, Odorant / metabolism. Sense Organs / physiology

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  • [ErratumIn] Chem Senses. 2005 Mar;30(3):279
  • (PMID = 15647464.001).
  • [ISSN] 0379-864X
  • [Journal-full-title] Chemical senses
  • [ISO-abbreviation] Chem. Senses
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Organic Chemicals; 0 / Pheromones; 0 / Plant Oils; 0 / Receptors, Odorant
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72. Balasubramanian S, Lynch JW, Barry PH: The permeation of organic cations through cAMP-gated channels in mammalian olfactory receptor neurons. J Membr Biol; 1995 Jul;146(2):177-91
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  • [Title] The permeation of organic cations through cAMP-gated channels in mammalian olfactory receptor neurons.
  • The permeation of monovalent organic cations through adenosine 3',5'-cyclic monophosphate-(cAMP) activated channels was studied by recording macroscopic currents in excised inside-out membrane patches from the dendritic knobs of isolated mammalian olfactory receptor neurons (ORNs).
  • Current-voltage relations were measured when bathing solution Na+ was replaced by monovalent organic cations.
  • Some of the small organic cations tested included ammonium (NH4+), hydroxylammonium and formamidinium, with relative permeability ratios of 1.41, 2.3 and 1.01 respectively.
  • (ii) the pore dimension must be at least 6.5 x 6.5 A, in order to allow TEA and Tris to permeate and (iii) molecular sieving must be an important mechanism for the permeation of large organic ions through the channels with specific ion binding playing a smaller role than in other structurally similar channels.
  • In addition, the results clearly indicate that cyclic nucleotide-gated (CNG) channels in different cells are not the same, the olfactory CNG channel being different from that of the photoreceptors, particularly with respect to the permeation of large organic cations, which the ORN channels allow to permeate readily.
  • [MeSH-major] Ion Channels / metabolism. Olfactory Receptor Neurons / metabolism
  • [MeSH-minor] Amidines / metabolism. Animals. Arginine / metabolism. Cations. Cell Membrane Permeability. Choline / metabolism. Cyclic AMP / metabolism. Cyclic Nucleotide-Gated Cation Channels. Electric Conductivity. Female. Methylation. Quaternary Ammonium Compounds / metabolism. Rats. Rats, Wistar. Tromethamine / metabolism

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  • (PMID = 7473687.001).
  • [ISSN] 0022-2631
  • [Journal-full-title] The Journal of membrane biology
  • [ISO-abbreviation] J. Membr. Biol.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] UNITED STATES
  • [Chemical-registry-number] 0 / Amidines; 0 / Cations; 0 / Cyclic Nucleotide-Gated Cation Channels; 0 / Ion Channels; 0 / Quaternary Ammonium Compounds; 0 / olfactory cyclic-nucleotide-gated channel 2; 023C2WHX2V / Tromethamine; 463-52-5 / formamidine; 94ZLA3W45F / Arginine; E0399OZS9N / Cyclic AMP; N91BDP6H0X / Choline
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73. Bhattacharya S, Labutti JN, Seiner DR, Gates KS: Oxidative inactivation of protein tyrosine phosphatase 1B by organic hydroperoxides. Bioorg Med Chem Lett; 2008 Nov 15;18(22):5856-9
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  • [Title] Oxidative inactivation of protein tyrosine phosphatase 1B by organic hydroperoxides.
  • Protein tyrosine phosphatases (PTPs) are cysteine-dependent enzymes that play a central role in cell signaling.
  • Organic hydroperoxides cause thiol-reversible, oxidative inactivation of PTP1B in a manner that mirrors the endogenous signaling agent hydrogen peroxide.

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  • (PMID = 18595691.001).
  • [ISSN] 1464-3405
  • [Journal-full-title] Bioorganic & medicinal chemistry letters
  • [ISO-abbreviation] Bioorg. Med. Chem. Lett.
  • [Language] ENG
  • [Grant] United States / NCI NIH HHS / CA / R01 CA119131; United States / NCI NIH HHS / CA / CA119131-01; United States / NCI NIH HHS / CA / CA083925-01; United States / NCI NIH HHS / CA / CA 119131; United States / NCI NIH HHS / CA / R01 CA083925; United States / NCI NIH HHS / CA / R01 CA083925-01; United States / NCI NIH HHS / CA / R01 CA119131-01; United States / NCI NIH HHS / CA / CA 83925
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Sulfhydryl Compounds; BBX060AN9V / Hydrogen Peroxide; EC 3.1.3.48 / Protein Tyrosine Phosphatase, Non-Receptor Type 1; GAN16C9B8O / Glutathione; I6KPI2E1HD / Peracetic Acid; K848JZ4886 / Cysteine
  • [Other-IDs] NLM/ NIHMS170682; NLM/ PMC2819122
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74. Delfino RJ, Staimer N, Tjoa T, Arhami M, Polidori A, Gillen DL, Kleinman MT, Schauer JJ, Sioutas C: Association of biomarkers of systemic inflammation with organic components and source tracers in quasi-ultrafine particles. Environ Health Perspect; 2010 Jun;118(6):756-62
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  • [Title] Association of biomarkers of systemic inflammation with organic components and source tracers in quasi-ultrafine particles.
  • METHODS: Weekly biomarkers of inflammation were plasma interleukin-6 (IL-6) and soluble tumor necrosis factor-alpha receptor II (sTNF-RII) (n = 578).
  • Exposures included indoor and outdoor community organic PM0.25 constituents [polycyclic aromatic hydrocarbons (PAHs), hopanes, n-alkanes, organic acids, water-soluble organic carbon, and transition metals].
  • RESULTS: Indoor and outdoor PAHs (low-, medium-, and high-molecular-weight PAHs), followed by hopanes (vehicle emissions tracer), were positively associated with biomarkers, but other organic components and transition metals were not. sTNF-RII increased by 135 pg/mL [95% confidence interval (CI), 45-225 pg/mL], and IL-6 increased by 0.27 pg/mL (95% CI, 0.10-0.44 pg/mL) per interquartile range increase of 0.56 ng/m3 outdoor total PAHs.
  • CONCLUSIONS: Traffic emission sources of organic chemicals represented by PAHs are associated with increased systemic inflammation and explain associations with quasi-ultrafine particle mass.

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  • (PMID = 20123637.001).
  • [ISSN] 1552-9924
  • [Journal-full-title] Environmental health perspectives
  • [ISO-abbreviation] Environ. Health Perspect.
  • [Language] ENG
  • [Grant] United States / NCRR NIH HHS / RR / M01 RR000827; United States / NIEHS NIH HHS / ES / R01 ES012243; United States / NIEHS NIH HHS / ES / ES12243; United States / NCRR NIH HHS / RR / M01 RR00827
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, Non-P.H.S.
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Biomarkers; 0 / Interleukin-6; 0 / Particulate Matter; 0 / Polycyclic Hydrocarbons, Aromatic; 0 / Receptors, Tumor Necrosis Factor, Type II; 0 / Triterpenes; 0 / Vehicle Emissions; 471-62-5 / hopane
  • [Other-IDs] NLM/ PMC2898850
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75. Aubert L, Motais R: Molecular features of organic anion permeablity in ox red blood cell. J Physiol; 1975 Mar;246(1):159-79
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  • [Title] Molecular features of organic anion permeablity in ox red blood cell.
  • 1. The penetration of organic anions into bovine red blood cells has been studied under experimental conditions where it could be distinguished from the penetration of undissociated acids which proceeds by diffusion through lipid zones of the membrane.
  • 2. Several lines of evidence suggest that the entry of organic anions cannot be ascribed to simple diffusion across aqueous channels limited by positive charges but needs a specific interaction of the penetrating anion with a component of the membrane.
  • Interaction between substrate and receptor requires at least a three point attachment involving three oxygen atoms in the substrate which react with complementary loci on the receptor to form ionic and hydrogen bonds.
  • 4. As suggested by the behaviour of the formate anion, in such a transport system any carboxylic acid could interact transiently with the receptor and therefore interfere with the transport of an organic anion even though such ionic interaction with the receptor were insufficient to produce transport of the acid itself.
  • [MeSH-major] Cell Membrane Permeability. Erythrocytes / metabolism

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  • [Cites] Eur J Biochem. 1970 May 1;14(1):120-6 [5447428.001]
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  • (PMID = 237121.001).
  • [ISSN] 0022-3751
  • [Journal-full-title] The Journal of physiology
  • [ISO-abbreviation] J. Physiol. (Lond.)
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] ENGLAND
  • [Chemical-registry-number] 0 / Anions; 0 / Carboxylic Acids; 0 / Dicarboxylic Acids; 0 / Sulfonic Acids
  • [Other-IDs] NLM/ PMC1309408
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76. Campbell CG, Spray DC, Wolkoff AW: Extracellular ATP4- modulates organic anion transport by rat hepatocytes. J Biol Chem; 1993 Jul 25;268(21):15399-404
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  • [Title] Extracellular ATP4- modulates organic anion transport by rat hepatocytes.
  • The hepatocyte has an organic anion transport system that recognizes compounds such as bilirubin and sulfobromophthalein.
  • In this study, the influence of extracellular ATP on the hepatocyte organic anion transport mechanism has been characterized.
  • Decreased transport activity was rapidly reversible, was non-competitive with respect to ATP, did not require ATP hydrolysis, and did not correlate with P2y purinergic receptor activity.
  • Although an ATP4- receptor in macrophages mediates increased cellular permeability, reduced organic anion permeability is seen in hepatocytes.
  • This effect is not seen in the hepatoma cell line HepG2.
  • Modulation of activity of the organic anion transporter by extracellular ATP may have important pathophysiological consequences in conditions resulting in liver cell injury.

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  • (PMID = 8340370.001).
  • [ISSN] 0021-9258
  • [Journal-full-title] The Journal of biological chemistry
  • [ISO-abbreviation] J. Biol. Chem.
  • [Language] eng
  • [Grant] United States / NIDDK NIH HHS / DK / DK-23026; United States / NIDDK NIH HHS / DK / DK-41296
  • [Publication-type] Journal Article; Research Support, U.S. Gov't, P.H.S.
  • [Publication-country] UNITED STATES
  • [Chemical-registry-number] 0 / Anions; 0 / Culture Media; 0C2P5QKL36 / Sulfobromophthalein; 8L70Q75FXE / Adenosine Triphosphate
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77. Anyatonwu GI, Ehrlich BE: Organic cation permeation through the channel formed by polycystin-2. J Biol Chem; 2005 Aug 19;280(33):29488-93
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  • [Title] Organic cation permeation through the channel formed by polycystin-2.
  • Polycystin-2 (PC2), a member of the transient receptor potential family of ion channels (TRPP2), forms a calcium-permeable cation channel.
  • Organic cations of increasing size were used as current carriers through the PC2 channel after PC2 was incorporated into lipid bilayers.
  • The slope conductance of the PC2 channel decreased as the ionic diameter of the organic cation increased.
  • For each organic cation tested, the currents were inhibited by gadolinium and anti-PC2 antibody.
  • [MeSH-minor] Animals. Cations / metabolism. Cell Line. Gadolinium / pharmacology. Organic Chemicals / metabolism. Permeability. Protein Conformation. Swine. TRPP Cation Channels

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  • (PMID = 15961385.001).
  • [ISSN] 0021-9258
  • [Journal-full-title] The Journal of biological chemistry
  • [ISO-abbreviation] J. Biol. Chem.
  • [Language] eng
  • [Grant] United States / NIDDK NIH HHS / DK / 5F31DK062635; United States / NIGMS NIH HHS / GM / T32-GM07324
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, P.H.S.
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Calcium Channels; 0 / Cations; 0 / Membrane Proteins; 0 / Organic Chemicals; 0 / TRPP Cation Channels; 0 / polycystic kidney disease 2 protein; AU0V1LM3JT / Gadolinium
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78. Parales RE, Luu RA, Chen GY, Liu X, Wu V, Lin P, Hughes JG, Nesteryuk V, Parales JV, Ditty JL: Pseudomonas putida F1 has multiple chemoreceptors with overlapping specificity for organic acids. Microbiology; 2013 Jun;159(Pt 6):1086-96
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  • [Title] Pseudomonas putida F1 has multiple chemoreceptors with overlapping specificity for organic acids.
  • Previous studies have demonstrated that Pseudomonas putida strains are not only capable of growth on a wide range of organic substrates, but also chemotactic towards many of these compounds.
  • However, deletion of the gene encoding the P. putida F1 orthologue (locus tag Pput_4520, designated mcfS) of McpS, a known receptor for organic acids in P. putida KT2440, did not result in an obvious chemotaxis phenotype.
  • This screen resulted in the identification of a receptor, McfQ (locus tag Pput_4894), which responds to citrate and fumarate.
  • An additional receptor, McfR (locus tag Pput_0339), which detects succinate, malate and fumarate, was found by individually expressing each of the 18 genes encoding canonical MCPs from strain F1 in a KT2440 mcpS-deletion mutant.
  • Therefore, at least three receptors, McfR, McfS, and McfQ, work in concert to detect organic acids in P. putida F1.

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  • (PMID = 23618999.001).
  • [ISSN] 1465-2080
  • [Journal-full-title] Microbiology (Reading, England)
  • [ISO-abbreviation] Microbiology (Reading, Engl.)
  • [Language] eng
  • [Grant] United States / NIGMS NIH HHS / GM / T32 GM007377; United States / NIGMS NIH HHS / GM / T32 GM007377
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural; Research Support, U.S. Gov't, Non-P.H.S.
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Bacterial Proteins; 0 / Carboxylic Acids; 0 / Membrane Proteins; 0 / methyl-accepting chemotaxis proteins
  • [Other-IDs] NLM/ PMC4085986
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79. Tanimoto S, Takahashi D, Toshima K: Chemical methods for degradation of target proteins using designed light-activatable organic molecules. Chem Commun (Camb); 2012 Aug 11;48(62):7659-71
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  • [Title] Chemical methods for degradation of target proteins using designed light-activatable organic molecules.
  • Molecular design, chemical synthesis, and biological evaluation of several designed organic molecules, which target-selectively degrade proteins upon photo-irradiation, are introduced.
  • The designed molecules for protein photo-degradation include 2-phenylquinoline-steroid hormone hybrids and porphyrin derivatives, both of which selectively photo-degrade estrogen receptor-α, and fullerene-sugar and -sulfonic acid hybrids, which selectively photo-degrade HIV-1 protease and amyloid β, respectively.
  • [MeSH-minor] Amyloid beta-Peptides / chemistry. Animals. Cell Line. Estrogen Receptor alpha / chemistry. Fullerenes / chemistry. HIV Protease / chemistry. Humans. Monosaccharides / chemistry. Porphyrins / chemistry. Quinolines / chemistry. Rats. Steroids / chemistry. Sulfonic Acids / chemistry. Ultraviolet Rays

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  • (PMID = 22739361.001).
  • [ISSN] 1364-548X
  • [Journal-full-title] Chemical communications (Cambridge, England)
  • [ISO-abbreviation] Chem. Commun. (Camb.)
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / 2-phenylquinoline; 0 / Amyloid beta-Peptides; 0 / Estrogen Receptor alpha; 0 / Fullerenes; 0 / Monosaccharides; 0 / Photosensitizing Agents; 0 / Porphyrins; 0 / Quinolines; 0 / Steroids; 0 / Sulfonic Acids; 0 / estrogen receptor alpha, human; EC 3.4.23.- / HIV Protease; EC 3.4.23.- / p16 protease, Human immunodeficiency virus 1
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80. Myre M, Imbeault P: Persistent organic pollutants meet adipose tissue hypoxia: does cross-talk contribute to inflammation during obesity? Obes Rev; 2014 Jan;15(1):19-28
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  • [Title] Persistent organic pollutants meet adipose tissue hypoxia: does cross-talk contribute to inflammation during obesity?
  • Lipophilic persistent organic pollutants (POPs) accumulate in lipid-rich tissues such as human adipose tissue.
  • The aryl hydrocarbon receptor (AhR) mediates the cellular response to some pollutants, while hypoxia responses occur through the oxygen-sensitive transcription factor hypoxia-inducible factor (HIF)-1.
  • [MeSH-major] Adipose Tissue / metabolism. Cell Hypoxia / immunology. Environmental Pollutants / metabolism. Hypoxia-Inducible Factor 1, alpha Subunit / metabolism. Inflammation Mediators / metabolism. Obesity / metabolism. Polychlorinated Biphenyls / metabolism. Receptors, Aryl Hydrocarbon / metabolism
  • [MeSH-minor] Adiposity. Animals. Female. Humans. Inflammation / immunology. Male. Rats. Receptor Cross-Talk / immunology. Signal Transduction

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  • [Copyright] © 2013 The Authors. obesity reviews © 2013 International Association for the Study of Obesity.
  • (PMID = 23998203.001).
  • [ISSN] 1467-789X
  • [Journal-full-title] Obesity reviews : an official journal of the International Association for the Study of Obesity
  • [ISO-abbreviation] Obes Rev
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't; Review
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Environmental Pollutants; 0 / HIF1A protein, human; 0 / Hypoxia-Inducible Factor 1, alpha Subunit; 0 / Inflammation Mediators; 0 / Receptors, Aryl Hydrocarbon; DFC2HB4I0K / Polychlorinated Biphenyls
  • [Keywords] NOTNLM ; Aryl hydrocarbon receptor / hypoxia-inducible factor / oxygen deficit / xenobiotics
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81. Burckhardt G: Drug transport by Organic Anion Transporters (OATs). Pharmacol Ther; 2012 Oct;136(1):106-30
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Drug transport by Organic Anion Transporters (OATs).
  • Common to all so far functionally characterized Organic Anion Transporters (OATs) is their broad substrate specificity and their ability to exchange extracellular against intracellular organic anions.
  • In human kidneys, OAT1, OAT2, and OAT3 are localized in the basolateral membrane, and OAT4, OAT10, and URAT1 in the apical cell membrane of proximal tubule cells, respectively.
  • Several classes of drugs interact with human OAT1-3, including ACE inhibitors, angiotensin II receptor antagonists, diuretics, HMG CoA reductase inhibitors, β-lactam antibiotics, antineoplastic and antiviral drugs, and uricosuric drugs.
  • [MeSH-major] Organic Anion Transporters / physiology. Pharmaceutical Preparations / metabolism

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  • [Copyright] Copyright © 2012 Elsevier Inc. All rights reserved.
  • (PMID = 22841915.001).
  • [ISSN] 1879-016X
  • [Journal-full-title] Pharmacology & therapeutics
  • [ISO-abbreviation] Pharmacol. Ther.
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Organic Anion Transporters; 0 / Pharmaceutical Preparations
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82. Obara S: Effects of some organic cations on generator potential of crayfish stretch receptor. J Gen Physiol; 1968 Aug;52(2):363-86
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  • [Title] Effects of some organic cations on generator potential of crayfish stretch receptor.
  • The generator potential of both slowly and rapidly adapting crayfish stretch receptor cells can still be elicited by mechanical stimuli when all the Na of the bathing medium is replaced by various organic cations.
  • In the presence of tris(hydroxymethyl)aminomethane (Tris), the generator potential is particularly large, about 30-50 % of that in the control saline, while spike electrogenesis of the cell is abolished.
  • Thus, whereas the electrogenesis of the generator membrane must be due to an increased permeability to monovalent cations, the active receptor membrane appears to be less selective for different monovalent cations than is the receptor component of some other cells, or the conductile component of the stretch receptor neuron.
  • [MeSH-major] Sensory Receptor Cells / drug effects. Tromethamine / pharmacology
  • [MeSH-minor] Acetates / pharmacology. Amidines / pharmacology. Aminobutyrates / pharmacology. Animals. Calcium / pharmacology. Cell Membrane Permeability. Chlorides / pharmacology. Choline / pharmacology. Crustacea. Electrophysiology. Guanidines / pharmacology. Hydrazines / pharmacology. In Vitro Techniques. Quaternary Ammonium Compounds / pharmacology. Sucrose / pharmacology. Sulfonic Acids / pharmacology. Tetraethylammonium Compounds / pharmacology

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  • (PMID = 5672006.001).
  • [ISSN] 0022-1295
  • [Journal-full-title] The Journal of general physiology
  • [ISO-abbreviation] J. Gen. Physiol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] UNITED STATES
  • [Chemical-registry-number] 0 / Acetates; 0 / Amidines; 0 / Aminobutyrates; 0 / Chlorides; 0 / Guanidines; 0 / Hydrazines; 0 / Quaternary Ammonium Compounds; 0 / Sulfonic Acids; 0 / Tetraethylammonium Compounds; 023C2WHX2V / Tromethamine; 57-50-1 / Sucrose; N91BDP6H0X / Choline; SY7Q814VUP / Calcium
  • [Other-IDs] NLM/ PMC2225805
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83. Zhao X, Yang H, Yamoah EN, Lundberg YW: Gene targeting reveals the role of Oc90 as the essential organizer of the otoconial organic matrix. Dev Biol; 2007 Apr 15;304(2):508-24
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  • [Title] Gene targeting reveals the role of Oc90 as the essential organizer of the otoconial organic matrix.
  • A critical part of the functional development of our peripheral balance system is the embryonic formation of otoconia, composite crystals that overlie and provide optimal stimulus input to the sensory epithelium of the gravity receptor in the inner ear.
  • Using gene targeting and protein analysis strategies, we demonstrate that the predominant mammalian otoconin, otoconin-90/95 (Oc90), is essential for formation of the organic matrix of otoconia by specifically recruiting other matrix components, which includes otolin, a novel mammalian otoconin that we identified to be in wildtype murine otoconia.
  • During otoconia development, the organic matrix forms prior to CaCO3 deposition and provides optimal calcification efficiency.

  • KOMP Repository. gene/protein/disease-specific - KOMP Repository (subscription/membership/fee required).
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  • (PMID = 17300776.001).
  • [ISSN] 0012-1606
  • [Journal-full-title] Developmental biology
  • [ISO-abbreviation] Dev. Biol.
  • [Language] ENG
  • [Grant] United States / NCRR NIH HHS / RR / P20 RR018788; United States / NCRR NIH HHS / RR / RR018788-030004; United States / NCRR NIH HHS / RR / 1P20RR018788-01; United States / NCRR NIH HHS / RR / P20 RR018788-030004
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Extracellular Matrix Proteins; 0 / Oc90 protein, mouse
  • [Other-IDs] NLM/ NIHMS21769; NLM/ PMC1950278
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84. Huber RD, Gao B, Sidler Pfändler MA, Zhang-Fu W, Leuthold S, Hagenbuch B, Folkers G, Meier PJ, Stieger B: Characterization of two splice variants of human organic anion transporting polypeptide 3A1 isolated from human brain. Am J Physiol Cell Physiol; 2007 Feb;292(2):C795-806
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  • [Title] Characterization of two splice variants of human organic anion transporting polypeptide 3A1 isolated from human brain.
  • In the present study we isolated two splice variants of organic anion transporting polypeptide 3A1 (OATP3A1_v1 and OATP3A1_v2) from human brain.
  • Immunolocalization of OATP3A1_v2 included Sertoli cells in testis, apical and/or subapical membranes in choroid plexus epithelial cells, and neurons (cell bodies and axons) of the gray and white matter of human frontal cortex.
  • Transported substrates include prostaglandin (PG)E(1) and PGE(2), thyroxine, and the cyclic oligopeptides BQ-123 (endothelin receptor antagonist) and vasopressin.
  • [MeSH-major] Alternative Splicing. Brain / metabolism. Organic Anion Transporters / physiology
  • [MeSH-minor] Alprostadil / metabolism. Amino Acid Sequence. Animals. CHO Cells. Cricetinae. Cricetulus. Dinoprostone / metabolism. Endothelin Receptor Antagonists. Humans. Molecular Sequence Data. Organ Specificity. Rats. Vasopressins / metabolism. Xenopus laevis

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  • (PMID = 16971491.001).
  • [ISSN] 0363-6143
  • [Journal-full-title] American journal of physiology. Cell physiology
  • [ISO-abbreviation] Am. J. Physiol., Cell Physiol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Endothelin Receptor Antagonists; 0 / Organic Anion Transporters; 0 / SLCO3A1 protein, human; 11000-17-2 / Vasopressins; F5TD010360 / Alprostadil; K7Q1JQR04M / Dinoprostone
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85. Cheng X, Quintás-Cardama A, Golemovic M, Zingaro R, Gao MZ, Freireich EJ, Andreeff M, Kantarjian HM, Verstovsek S: The organic arsenic derivative GMZ27 induces PML-RARα-independent apoptosis in myeloid leukemia cells. Anticancer Res; 2012 Jul;32(7):2871-80
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  • [Title] The organic arsenic derivative GMZ27 induces PML-RARα-independent apoptosis in myeloid leukemia cells.
  • However, organic arsenic derivatives (OAD) have a more favorable toxicity profile than ATO.
  • GMZ27 had potent antiproliferative activity against human acute myeloid leukemia (AML) cell lines that was higher than that of ATO.
  • In contrast to ATO, GMZ27 only marginally induced maturation of leukemia cells and had no effect on the cell cycle.
  • [MeSH-minor] Animals. Caspase 9 / metabolism. Cell Cycle / drug effects. Cell Growth Processes / drug effects. Cell Line, Tumor. Dose-Response Relationship, Drug. Enzyme Activation / drug effects. Female. HL-60 Cells. Humans. Mice. Oxides / pharmacology. Oxygen / metabolism

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  • (PMID = 22753750.001).
  • [ISSN] 1791-7530
  • [Journal-full-title] Anticancer research
  • [ISO-abbreviation] Anticancer Res.
  • [Language] eng
  • [Grant] United States / NCI NIH HHS / CA / P30 CA016672
  • [Publication-type] Journal Article
  • [Publication-country] Greece
  • [Chemical-registry-number] 0 / Antineoplastic Agents; 0 / Arsenicals; 0 / Oncogene Proteins, Fusion; 0 / Oxides; 0 / promyelocytic leukemia-retinoic acid receptor alpha fusion oncoprotein; EC 3.4.22.- / Caspase 9; S7V92P67HO / arsenic trioxide; S88TT14065 / Oxygen
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86. Schaffner CA, Mwinyi J, Gai Z, Thasler WE, Eloranta JJ, Kullak-Ublick GA: The organic solute transporters alpha and beta are induced by hypoxia in human hepatocytes. Liver Int; 2015 Apr;35(4):1152-61
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  • [Title] The organic solute transporters alpha and beta are induced by hypoxia in human hepatocytes.
  • BACKGROUND & AIMS: The organic solute transporters alpha and beta (OSTα-OSTβ) form a heterodimeric transporter located at the basolateral membrane of intestinal epithelial cells and hepatocytes.
  • [MeSH-minor] Animals. Binding Sites. Cell Hypoxia. Cell Line. Chenodeoxycholic Acid / pharmacology. Disease Models, Animal. Humans. Hypoxia-Inducible Factor 1, alpha Subunit / genetics. Hypoxia-Inducible Factor 1, alpha Subunit / metabolism. Kidney Failure, Chronic / metabolism. RNA Interference. Rats, Sprague-Dawley. Receptors, Cytoplasmic and Nuclear / genetics. Receptors, Cytoplasmic and Nuclear / metabolism. Response Elements. Transfection. Up-Regulation

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  • [Copyright] © 2014 The Authors. Liver International Published by John Wiley & Sons Ltd.
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  • (PMID = 24703425.001).
  • [ISSN] 1478-3231
  • [Journal-full-title] Liver international : official journal of the International Association for the Study of the Liver
  • [ISO-abbreviation] Liver Int.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / HIF1A protein, human; 0 / Hypoxia-Inducible Factor 1, alpha Subunit; 0 / Membrane Transport Proteins; 0 / Ostalpha protein, rat; 0 / Ostbeta protein, rat; 0 / Receptors, Cytoplasmic and Nuclear; 0 / farnesoid X-activated receptor; 0 / organic solute transporter alpha, human; 0 / organic solute transporter beta, human; 0GEI24LG0J / Chenodeoxycholic Acid
  • [Other-IDs] NLM/ PMC4407926
  • [Keywords] NOTNLM ; bile acid transport / chronic renal failure / gene regulation / ligand / nephrectomy / nuclear receptor / organic anion transport / rat liver
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87. Yang XH, Liu SY, Xing AY: Molecular regulation of organic anion transporting polypeptide 1A2 (OATP1A2)by taurocholic acid in Bewo Cells. Cell Mol Biol (Noisy-le-grand); 2014;60(2):22-6
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  • [Title] Molecular regulation of organic anion transporting polypeptide 1A2 (OATP1A2)by taurocholic acid in Bewo Cells.
  • To characterize the mechanisms of action of taurocholic acid(TCA) and farnesoid X receptor(FXR) on organic anion transporting polypeptide 1A2(OATP1A2) expression in placental Bewo cell line.
  • TCA is one of the regulation factors for OATP1A2 in the Bewo cell line.
  • Farnesoid X receptor may act in synergy with TCA to increase the expression of OATP1A2.
  • [MeSH-major] Organic Anion Transporters / metabolism. Taurocholic Acid / chemistry
  • [MeSH-minor] Cell Line. Detergents / chemistry. Detergents / pharmacology. Gene Expression / drug effects. Humans. RNA, Messenger / metabolism. Receptors, Cytoplasmic and Nuclear / genetics. Receptors, Cytoplasmic and Nuclear / metabolism

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  • (PMID = 24970118.001).
  • [ISSN] 1165-158X
  • [Journal-full-title] Cellular and molecular biology (Noisy-le-Grand, France)
  • [ISO-abbreviation] Cell. Mol. Biol. (Noisy-le-grand)
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] France
  • [Chemical-registry-number] 0 / Detergents; 0 / Organic Anion Transporters; 0 / RNA, Messenger; 0 / Receptors, Cytoplasmic and Nuclear; 0 / SLCO1A2 protein, human; 0 / farnesoid X-activated receptor; 5E090O0G3Z / Taurocholic Acid
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88. Sears ML: Regulation of aqueous flow by the adenylate cyclase receptor complex in the ciliary epithelium. Am J Ophthalmol; 1985 Jul 15;100(1):194-8
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  • [Title] Regulation of aqueous flow by the adenylate cyclase receptor complex in the ciliary epithelium.
  • The answer to how the beta-adrenergic receptor mediates a fall in intraocular pressure has been elusive.
  • On a molecular basis, stimulation of the beta-adrenergic receptor activates intracellular adenylate cyclase to produce increased cyclic adenosine monophosphate.
  • Acting by different cell-receptor mechanisms, but nonetheless potent, nonadrenergic stimulators of adenylate cyclase in the ciliary epithelium, such as cholera toxin and organic fluorides, have been studied in experimental animals.
  • [MeSH-minor] ADP-Ribosylation Factors. Adenylyl Cyclases / physiology. Adult. Aged. Anterior Chamber / metabolism. Cell Membrane Permeability. Colforsin. Cyclic AMP / biosynthesis. Epithelium / metabolism. Humans. Middle Aged. Receptors, Adrenergic, beta / physiology. Timolol / pharmacology

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  • (PMID = 2990214.001).
  • [ISSN] 0002-9394
  • [Journal-full-title] American journal of ophthalmology
  • [ISO-abbreviation] Am. J. Ophthalmol.
  • [Language] eng
  • [Grant] United States / NEI NIH HHS / EY / EY-00237; United States / NEI NIH HHS / EY / EY-00785
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.
  • [Publication-country] UNITED STATES
  • [Chemical-registry-number] 0 / Diterpenes; 0 / Membrane Proteins; 0 / Receptors, Adrenergic, beta; 1F7A44V6OU / Colforsin; 817W3C6175 / Timolol; E0399OZS9N / Cyclic AMP; EC 3.6.5.2 / ADP-Ribosylation Factors; EC 4.6.1.1 / Adenylyl Cyclases
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89. Zhang Y, Csanaky IL, Selwyn FP, Lehman-McKeeman LD, Klaassen CD: Organic anion-transporting polypeptide 1a4 (Oatp1a4) is important for secondary bile acid metabolism. Biochem Pharmacol; 2013 Aug 1;86(3):437-45
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  • [Title] Organic anion-transporting polypeptide 1a4 (Oatp1a4) is important for secondary bile acid metabolism.
  • Organic anion transporting polypeptides (human: OATPs; rodent: Oatps) were thought to have important functions in bile acid (BA) transport.

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  • [Copyright] Copyright © 2013 Elsevier Inc. All rights reserved.
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  • (PMID = 23747753.001).
  • [ISSN] 1873-2968
  • [Journal-full-title] Biochemical pharmacology
  • [ISO-abbreviation] Biochem. Pharmacol.
  • [Language] ENG
  • [Grant] United States / NIEHS NIH HHS / ES / R01 ES009649; United States / NIEHS NIH HHS / ES / R01 ES019487; United States / NIEHS NIH HHS / ES / ES-019487; United States / NIEHS NIH HHS / ES / ES009649
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Bile Acids and Salts; 0 / Oatp2 protein, mouse; 0 / Organic Cation Transport Proteins
  • [Other-IDs] NLM/ NIHMS501152; NLM/ PMC3774164
  • [Keywords] NOTNLM ; 7-oxo-deoxycholic acid / 7-oxoDCA / ATP-binding cassette transporter a1 / Abca1 / BA / Bile acid / Bsep / CA / CDCA / Cyp / DCA / Fxr / Gapdh / HDCA / IS / LCA / Liver / MCA / MDCA / Mrp / Ntcp / Oatp/OATP / Oatp1a4 / Ost / Rpl13a / Secondary bile acid / Shp / T-12-epiDCA / TCA / UDCA / UPLC / WT / bile acid / bile salt-export pump / chenodeoxycholic acid / cholic acid / cytochrome P450 / deoxycholic acid / farnesoid X receptor / glyceraldehyde 3-phosphate dehydrogenase / hyodeoxycholic acid / internal standard / lithocholic acid / multidrug resistance-associated protein / muricholic acid / murideoxycholic acid / organic anion transporting polypeptide / organic solute transporter / ribosomal protein L13a / small heterodimer partner / sodium taurocholate cotransporting polypeptide / tauro-12-epi deoxycholic acid / tauro-cholic acid / ultra performance liquid chromatography / ursodeoxycholic acid / wild type
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90. Ma L, Lu L, Zhu M, Wang Q, Gao F, Yuan C, Wu Y, Xing S, Fu X, Mei Y, Gao X: Dinuclear copper complexes of organic claw: potent inhibition of protein tyrosine phosphatases. J Inorg Biochem; 2011 Sep;105(9):1138-47
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  • [Title] Dinuclear copper complexes of organic claw: potent inhibition of protein tyrosine phosphatases.
  • Three dinuclear copper complexes of organic claw ligands (2,2',2″,2'''-(5-R-2-hydroxy-1,3-phenylene)bis(methylene)bis(azanetriyl)tetraacetic acid, R=methyl (H(5)L1), chloro (H(5)L2) and bromo (H(5)L3)): [Cu(2)NaL1(H(2)O)(2)] (1), [Cu(2)HL2(H(2)O)(2)] (2), [Cu(2)NaL3(H(2)O)(2)] (3), have been synthesized and characterized by elemental analyses, infrared spectra, thermo-gravimetric analyses, X-ray diffraction analysis, electrospray ionization mass spectra, pH-potentiometric titration, molar conductivity.
  • Their inhibitory effects against human protein tyrosine phosphatase 1B (PTP1B), T cell protein tyrosine phosphatase (TCPTP), Megakaryocyte protein tyrosinephosphatase 2 (PTP-MEG2), srchomology phosphatase 1 (SHP-1) and srchomology phosphatase 2 (SHP-2) are evaluated in vitro.
  • [MeSH-major] Acids, Heterocyclic / pharmacology. Chelating Agents / pharmacology. Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors. Protein Tyrosine Phosphatase, Non-Receptor Type 11 / antagonists & inhibitors. Protein Tyrosine Phosphatase, Non-Receptor Type 2 / antagonists & inhibitors. Protein Tyrosine Phosphatase, Non-Receptor Type 6 / antagonists & inhibitors. Protein Tyrosine Phosphatases, Non-Receptor / antagonists & inhibitors. Recombinant Proteins / antagonists & inhibitors

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  • [Copyright] Copyright © 2011 Elsevier Inc. All rights reserved.
  • (PMID = 21708098.001).
  • [ISSN] 1873-3344
  • [Journal-full-title] Journal of inorganic biochemistry
  • [ISO-abbreviation] J. Inorg. Biochem.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Acids, Heterocyclic; 0 / Chelating Agents; 0 / Enzyme Inhibitors; 0 / Ligands; 0 / Recombinant Proteins; 789U1901C5 / Copper; EC 3.1.3.48 / PTPN11 protein, human; EC 3.1.3.48 / PTPN6 protein, human; EC 3.1.3.48 / PTPN9 protein, human; EC 3.1.3.48 / Protein Tyrosine Phosphatase, Non-Receptor Type 1; EC 3.1.3.48 / Protein Tyrosine Phosphatase, Non-Receptor Type 11; EC 3.1.3.48 / Protein Tyrosine Phosphatase, Non-Receptor Type 2; EC 3.1.3.48 / Protein Tyrosine Phosphatase, Non-Receptor Type 6; EC 3.1.3.48 / Protein Tyrosine Phosphatases, Non-Receptor
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91. Trdan Lušin T, Stieger B, Marc J, Mrhar A, Trontelj J, Zavratnik A, Ostanek B: Organic anion transporting polypeptides OATP1B1 and OATP1B3 and their genetic variants influence the pharmacokinetics and pharmacodynamics of raloxifene. J Transl Med; 2012;10:76
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  • [Title] Organic anion transporting polypeptides OATP1B1 and OATP1B3 and their genetic variants influence the pharmacokinetics and pharmacodynamics of raloxifene.
  • BACKGROUND: Raloxifene, a selective estrogen receptor modulator, exhibits quite large and unexplained interindividual variability in pharmacokinetics and pharmacodynamics.
  • The aim of this study was to determine the role of organic-anion transporting polypeptides OATP1B1 and OATP1B3 and their genetic variants in the pharmacokinetics and pharmacodynamics of raloxifene.
  • [MeSH-major] Genetic Variation. Organic Anion Transporters / physiology. Organic Anion Transporters, Sodium-Independent / physiology. Raloxifene Hydrochloride / pharmacology. Selective Estrogen Receptor Modulators / pharmacokinetics

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  • (PMID = 22533838.001).
  • [ISSN] 1479-5876
  • [Journal-full-title] Journal of translational medicine
  • [ISO-abbreviation] J Transl Med
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Organic Anion Transporters; 0 / Organic Anion Transporters, Sodium-Independent; 0 / SLCO1B1 protein, human; 0 / SLCO1B3 protein, human; 0 / Selective Estrogen Receptor Modulators; 4F86W47BR6 / Raloxifene Hydrochloride
  • [Other-IDs] NLM/ PMC3476964
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92. Lafont V, Liautard J, Sable-Teychene M, Sainte-Marie Y, Favero J: Isopentenyl pyrophosphate, a mycobacterial non-peptidic antigen, triggers delayed and highly sustained signaling in human gamma delta T lymphocytes without inducing eown-modulation of T cell antigen receptor. J Biol Chem; 2001 May 11;276(19):15961-7
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  • [Title] Isopentenyl pyrophosphate, a mycobacterial non-peptidic antigen, triggers delayed and highly sustained signaling in human gamma delta T lymphocytes without inducing eown-modulation of T cell antigen receptor.
  • The Vgamma9Vdelta2 T cell subset, which represents up to 90% of the circulating gammadelta T cells in humans, was shown to be activated, via the T cell receptor (TcR), by non-peptidic phosphorylated small organic molecules.
  • [MeSH-major] Antigens, Bacterial / pharmacology. Hemiterpenes. Mitogen-Activated Protein Kinases / metabolism. Organophosphorus Compounds / pharmacology. Receptors, Antigen, T-Cell / immunology. Receptors, Antigen, T-Cell, gamma-delta / immunology. Signal Transduction / immunology. T-Lymphocytes / immunology

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  • (PMID = 11278429.001).
  • [ISSN] 0021-9258
  • [Journal-full-title] The Journal of biological chemistry
  • [ISO-abbreviation] J. Biol. Chem.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Antigens, Bacterial; 0 / Hemiterpenes; 0 / Organophosphorus Compounds; 0 / Receptors, Antigen, T-Cell; 0 / Receptors, Antigen, T-Cell, gamma-delta; 0 / Tumor Necrosis Factor-alpha; 358-71-4 / isopentenyl pyrophosphate; EC 2.7.10.1 / Protein-Tyrosine Kinases; EC 2.7.10.2 / Lymphocyte Specific Protein Tyrosine Kinase p56(lck); EC 2.7.10.2 / ZAP-70 Protein-Tyrosine Kinase; EC 2.7.10.2 / ZAP70 protein, human; EC 2.7.11.24 / Mitogen-Activated Protein Kinase 1; EC 2.7.11.24 / Mitogen-Activated Protein Kinase 3; EC 2.7.11.24 / Mitogen-Activated Protein Kinases
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93. Hjelmborg PS, Andreassen TK, Bonefeld-Jørgensen EC: Cellular uptake of lipoproteins and persistent organic compounds--an update and new data. Environ Res; 2008 Oct;108(2):192-8
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  • [Title] Cellular uptake of lipoproteins and persistent organic compounds--an update and new data.
  • This paper will focus on the interactions between lipoproteins and persistent organic pollutants (POPs) and how these particles are taken up by cells.
  • Uptake of DDT by MEF cells was investigated using MEF1 cells carrying the receptors low-density lipoprotein receptor-related protein (LRP) and low-density lipoprotein receptor (LDLR) present and MEF4 cells with no LRP and LDLR expression.
  • The receptor function was further evaluated by adding the 40kDa receptor-associated protein (RAP) which blocks receptor activity.
  • There was no strong evidence for a receptor-mediated uptake of the [(14)C]DDT-lipoprotein complex.
  • To conclude, DDT travels in the blood stream and can cross cell membranes while being transported as a DDT-lipoprotein complex.
  • The lipoproteins do not need receptors to cross cell membranes since passive diffusion constitutes a major passageway.
  • [MeSH-major] Environmental Pollutants / pharmacokinetics. Fibroblasts / drug effects. Lipoproteins / metabolism. Organic Chemicals / pharmacokinetics
  • [MeSH-minor] Animals. Biological Transport. Cell Culture Techniques. Cell Line. Mice. Mice, Knockout. Receptors, LDL / genetics. Ultracentrifugation

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  • (PMID = 18762293.001).
  • [ISSN] 1096-0953
  • [Journal-full-title] Environmental research
  • [ISO-abbreviation] Environ. Res.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Environmental Pollutants; 0 / Lipoproteins; 0 / Organic Chemicals; 0 / Receptors, LDL
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94. Sriarj W, Aoki K, Ohya K, Takagi Y, Shimokawa H: Bovine dentine organic matrix down-regulates osteoclast activity. J Bone Miner Metab; 2009;27(3):315-23
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  • [Title] Bovine dentine organic matrix down-regulates osteoclast activity.
  • These results could be because of different susceptibilities to acid and the different organic matrices between deciduous and permanent dentine.
  • TRAP positive cell number, TRAP activity, the areas of resorption pits, and mRNA levels of TRAP, v-ATPase, calcitonin receptor, cathepsin K, and MMP-9 were examined.
  • [MeSH-minor] Acid Phosphatase / metabolism. Animals. Bone Resorption / metabolism. Cattle. Cell Count. Cell Differentiation / drug effects. Coculture Techniques. Electrophoresis, Polyacrylamide Gel. Isoenzymes / metabolism. Mice. RNA, Messenger / genetics. RNA, Messenger / metabolism. Tissue Extracts / pharmacology. src-Family Kinases / antagonists & inhibitors

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  • (PMID = 19296049.001).
  • [ISSN] 0914-8779
  • [Journal-full-title] Journal of bone and mineral metabolism
  • [ISO-abbreviation] J. Bone Miner. Metab.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Japan
  • [Chemical-registry-number] 0 / Isoenzymes; 0 / RNA, Messenger; 0 / Tissue Extracts; EC 2.7.10.2 / src-Family Kinases; EC 3.1.3.- / tartrate-resistant acid phosphatase; EC 3.1.3.2 / Acid Phosphatase
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95. Wang F, Li C, Liu W, Jin Y: Modulation of microRNA expression by volatile organic compounds in mouse lung. Environ Toxicol; 2014 Jun;29(6):679-89
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  • [Title] Modulation of microRNA expression by volatile organic compounds in mouse lung.
  • Volatile organic compounds (VOCs) are one of main pollutants indoors.
  • Functional annotation analysis of the predicted miRNA transcript targets revealed that VOCs exposure potentially alters signaling pathways associated with cancer, chemokine signaling, Wnt signaling, neuroactive ligand-receptor interaction, and cell adhesion molecules.
  • [MeSH-major] Air Pollutants / toxicity. Lung / metabolism. MicroRNAs / metabolism. Volatile Organic Compounds / toxicity

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  • [Copyright] Copyright © 2012 Wiley Periodicals, Inc.
  • (PMID = 24733833.001).
  • [ISSN] 1522-7278
  • [Journal-full-title] Environmental toxicology
  • [ISO-abbreviation] Environ. Toxicol.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Air Pollutants; 0 / Interleukin-8; 0 / MicroRNAs; 0 / Volatile Organic Compounds; 0 / Xylenes; 1HG84L3525 / Formaldehyde; 3FPU23BG52 / Toluene; J64922108F / Benzene
  • [Keywords] NOTNLM ; VOCs mixture / gene regulation / lung / miRNA / pathways
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96. Murata Y, Kataoka-Shirasugi N, Amakawa T: Electrophysiological studies of salty taste modification by organic acids in the labellar taste cell of the blowfly. Chem Senses; 2002 Jan;27(1):57-65
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  • [Title] Electrophysiological studies of salty taste modification by organic acids in the labellar taste cell of the blowfly.
  • Using the labellar salt receptor cells of the blowfly, Phormia regina, we electrophysiologically showed that the response to NaCl and KCl aqueous solutions was enhanced and depressed by acetic, succinic and citric acids.
  • The organic acid concentrations at which the most enhanced salt response (MESR) was obtained were found to be different: 0.05-1 mM citric acid, 0.5-2 mM succinic acid and 5-50 mM acetic acid.
  • Another explanation for the enhancement is that the salty taste may also be enhanced by undissociated molecules of the organic acids, because the MESRs were obtained at the pH values lower than the pKa(1) or pKa(2) values of these organic acids.
  • On the other hand, the salty taste could be depressed by both the lower pH range (pH 2.5-2.0) and the dissociated organic anions from organic acid molecules with at least two carboxyl groups.

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  • (PMID = 11751469.001).
  • [ISSN] 0379-864X
  • [Journal-full-title] Chemical senses
  • [ISO-abbreviation] Chem. Senses
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Carboxylic Acids; 451W47IQ8X / Sodium Chloride; 660YQ98I10 / Potassium Chloride
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97. Cohen BN, Labarca C, Davidson N, Lester HA: Mutations in M2 alter the selectivity of the mouse nicotinic acetylcholine receptor for organic and alkali metal cations. J Gen Physiol; 1992 Sep;100(3):373-400
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  • [Title] Mutations in M2 alter the selectivity of the mouse nicotinic acetylcholine receptor for organic and alkali metal cations.
  • We measured the permeability ratios (PX/PNa) of 3 wild-type, 1 hybrid, 2 subunit-deficient, and 22 mutant nicotinic receptors expressed in Xenopus oocytes for alkali metal and organic cations using shifts in the bi-ionic reversal potential of the macroscopic current.
  • Mutations at position 2' (alpha Thr244, beta Gly255, gamma Thr253, delta Ser258) near the intracellular end of M2 changed the organic cation permeability ratios as much as twofold and reduced PCs/PNa and PK/PNa by 16-18%.
  • The wild-type mouse receptor displayed a surprising interaction with the primary ammonium cations; relative permeability peaked at a chain length equal to four carbons.
  • Analysis of the organic permeability ratios for the wild-type mouse receptor shows that (a) the diameter of the narrowest part of the pore is 8.4 A;.
  • (b) the mouse receptor departs significantly from size selectivity for monovalent organic cations; and (c) lowering the temperature reduces Pguanidinium/PNa by 38% and Pbutylammonium/PNa more than twofold.
  • The results reinforce present views that positions -1' and 2' are the narrowest part of the pore and suggest that positions 6' and 10' align some permeant organic cations in the pore in an interaction similar to that with channel blocker, QX-222.

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  • (PMID = 1431803.001).
  • [ISSN] 0022-1295
  • [Journal-full-title] The Journal of general physiology
  • [ISO-abbreviation] J. Gen. Physiol.
  • [Language] ENG
  • [Grant] United States / NINDS NIH HHS / NS / NS-11756
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Cations; 0 / Guanidines; 0 / Receptors, Nicotinic; 1KSV9V4Y4I / Cesium; 21236-55-5 / QX-222; 459-73-4 / glycine ethyl ester; 616-34-2 / glycine methyl ester; 7664-41-7 / Ammonia; 98PI200987 / Lidocaine; 9NEZ333N27 / Sodium; JU58VJ6Y3B / Guanidine; TE7660XO1C / Glycine
  • [Other-IDs] NLM/ PMC2229089
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98. Kometani T, Ikeda Y, Kasai M: Acetylcholine-binding substance extracted by using organic solvent and acetylcholine receptor of electric organ of Narke japonica. Biochim Biophys Acta; 1975 Dec 16;413(3):415-24
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  • [Title] Acetylcholine-binding substance extracted by using organic solvent and acetylcholine receptor of electric organ of Narke japonica.
  • From the heaviest, the fractions were acetylcholine receptor rich, ATPase rich, and acetylcholinesterase rich.
  • 3. The membrane fraction having acetylcholine receptor showed the excitability, the increase of Na+ permeability by the application of cholinergic agonists.
  • However, the acetylcholine binding substance extracted by the organic solvent was richer in the lighter fraction.
  • This substance differed from the true acetylcholine receptor.
  • [MeSH-minor] Acetylcholinesterase / analysis. Adenosine Triphosphatases / analysis. Animals. Binding Sites. Biological Transport, Active. Cell Membrane / analysis. Cell Membrane / metabolism. Fishes. Lipoproteins / isolation & purification. Lipoproteins / metabolism. Nerve Tissue Proteins / isolation & purification. Nerve Tissue Proteins / metabolism. Sodium / metabolism

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  • (PMID = 127623.001).
  • [ISSN] 0006-3002
  • [Journal-full-title] Biochimica et biophysica acta
  • [ISO-abbreviation] Biochim. Biophys. Acta
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] NETHERLANDS
  • [Chemical-registry-number] 0 / Lipoproteins; 0 / Nerve Tissue Proteins; 0 / Receptors, Cholinergic; 9NEZ333N27 / Sodium; EC 3.1.1.7 / Acetylcholinesterase; EC 3.6.1.- / Adenosine Triphosphatases; N9YNS0M02X / Acetylcholine
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99. Poole JA, Wyatt TA, Kielian T, Oldenburg P, Gleason AM, Bauer A, Golden G, West WW, Sisson JH, Romberger DJ: Toll-like receptor 2 regulates organic dust-induced airway inflammation. Am J Respir Cell Mol Biol; 2011 Oct;45(4):711-9
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  • [Title] Toll-like receptor 2 regulates organic dust-induced airway inflammation.
  • Organic dust exposure in agricultural environments results in significant airway inflammatory diseases.
  • Gram-positive cell wall components are present in high concentrations in animal farming dusts, but their role in mediating dust-induced airway inflammation is not clear.
  • This study investigated the role of Toll-like receptor (TLR) 2, a pattern recognition receptor for gram-positive cell wall products, in regulating swine facility organic dust extract (DE)-induced airway inflammation in mice.
  • Collectively, these results demonstrate that the TLR2 pathway is important in regulating swine facility organic dust-induced airway inflammation, which suggests the importance of TLR2 agonists in mediating large animal farming-induced airway inflammatory responses.

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  • (PMID = 21278324.001).
  • [ISSN] 1535-4989
  • [Journal-full-title] American journal of respiratory cell and molecular biology
  • [ISO-abbreviation] Am. J. Respir. Cell Mol. Biol.
  • [Language] ENG
  • [Grant] United States / NIOSH CDC HHS / OH / R01 OH008539-01; United States / NIAAA NIH HHS / AA / R01 AA017993; United States / NIEHS NIH HHS / ES / ES015522-03S1; United States / NIOSH CDC HHS / OH / R01 OH008539; United States / NIEHS NIH HHS / ES / K08 ES015522-01; United States / NIEHS NIH HHS / ES / R01 ES019325; United States / NIAAA NIH HHS / AA / K99 AA019499; United States / NIEHS NIH HHS / ES / K08 ES015522; United States / NINDS NIH HHS / NS / R01 NS055385
  • [Publication-type] Journal Article; Research Support, American Recovery and Reinvestment Act; Research Support, N.I.H., Extramural; Research Support, Non-U.S. Gov't; Research Support, U.S. Gov't, P.H.S.
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Bronchoconstrictor Agents; 0 / Chemokines; 0 / Cytokines; 0 / Dust; 0 / Inflammation Mediators; 0 / Lipopolysaccharides; 0 / Peptidoglycan; 0 / Tlr2 protein, mouse; 0 / Toll-Like Receptor 2; 0W5ETF9M2K / Methacholine Chloride; 31C4KY9ESH / Nitric Oxide
  • [Other-IDs] NLM/ PMC3208620
  •  go-up   go-down


100. Bauer C, Kielian T, Wyatt TA, Romberger DJ, West WW, Gleason AM, Poole JA: Myeloid differentiation factor 88-dependent signaling is critical for acute organic dust-induced airway inflammation in mice. Am J Respir Cell Mol Biol; 2013 Jun;48(6):781-9
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Myeloid differentiation factor 88-dependent signaling is critical for acute organic dust-induced airway inflammation in mice.
  • Organic dust exposure within agricultural environments results in airway diseases.
  • Toll-like receptor 2 (TLR2) and TLR4 only partly account for the innate response to these complex dust exposures.
  • To determine the central pathway in mediating complex organic dust-induced airway inflammation, this study targeted the common adaptor protein, myeloid differentiation factor 88 (MyD88), and investigated the relative contributions of receptors upstream from this adaptor.
  • Wild-type, MyD88, TLR9, TLR4, IL-1 receptor I (RI), and IL-18R knockout (KO) mice were challenged intranasally with organic dust extract (ODE) or saline, according to an established protocol.
  • Lung cell apoptosis was determined by a terminal deoxynucleotidyl transferase dUTP nick-end labeling assay, and lymphocyte influx and intercellular adhesion molecule-1 (ICAM-1) expression were assessed by immunohistochemistry.
  • ODE-induced epithelial-cell ICAM-1 expression was diminished in MyD88 KO mice.
  • No difference was evident in the small degree of ODE-induced lung-cell apoptosis.
  • Collectively, the acute organic dust-induced airway inflammatory response is highly dependent on MyD88 signaling, and is dictated, in part, by important contributions from upstream TLRs and IL-18R.