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1. Vuorio J, Vattulainen I, Martinez-Seara H: Atomistic fingerprint of hyaluronan-CD44 binding. PLoS Comput Biol; 2017 Jul;13(7):e1005663
NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Hyaluronan is a polyanionic, megadalton-scale polysaccharide, which initiates cell signaling by interacting with several receptor proteins including CD44 involved in cell-cell interactions and cell adhesion.

  • Hazardous Substances Data Bank. HYALURONIC ACID .
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  • (PMID = 28715483.001).
  • [ISSN] 1553-7358
  • [Journal-full-title] PLoS computational biology
  • [ISO-abbreviation] PLoS Comput. Biol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Antigens, CD44; 0 / CD44 protein, human; 9004-61-9 / Hyaluronic Acid
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2. Stevens MY, Chow SY, Estrada S, Eriksson J, Asplund V, Orlova A, Mitran B, Antoni G, Larhed M, Åberg O, Odell LR: Synthesis of <sup>11</sup>C-labeled Sulfonyl Carbamates through a Multicomponent Reaction Employing Sulfonyl Azides, Alcohols, and [<sup>11</sup>C]CO. ChemistryOpen; 2016 Dec;5(6):566-573

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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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3. 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<sub>3</sub> on cartilage formation deduced from comparisons between Cyp27b1 and Vdr knockout mice. Biochem Biophys Res Commun; 2017 Jan 29;483(1):359-365
Mouse Genome Informatics (MGI). Mouse Genome Informatics (MGI) .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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).
  • [MeSH-minor] Alopecia / genetics. Animals. Body Weight. Calcium / blood. Calcium / metabolism. Cell Differentiation. Cell Proliferation. Chondrocytes / cytology. Female. Femur / metabolism. Male. Mice. Mice, Knockout. Osteogenesis. Osteoporosis / metabolism. Parathyroid Hormone / metabolism. Phenotype. Phosphorus / metabolism. Real-Time Polymerase Chain Reaction

  • Hazardous Substances Data Bank. 1,25-DIHYDROXYCHOLECALCIFEROL .
  • Hazardous Substances Data Bank. CALCIUM, ELEMENTAL .
  • Hazardous Substances Data Bank. PHOSPHORUS, ELEMENTAL .
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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
  • [Chemical-registry-number] 0 / Parathyroid Hormone; 0 / Receptors, Calcitriol; 142508-67-6 / 1 alpha-(hydroxymethyl)-25-hydroxyvitamin D3; 27YLU75U4W / Phosphorus; EC 1.14.13.13 / 25-Hydroxyvitamin D3 1-alpha-Hydroxylase; FXC9231JVH / Calcitriol; SY7Q814VUP / Calcium
  • [Keywords] NOTNLM ; Bone remodeling / CYP27B1 / Genomic action / Knockout mice / VDR / Vitamin D
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4. Wang T, Tang H: The physical characteristics of human proteins in different biological functions. PLoS One; 2017;12(5):e0176234

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • The biological functions are defined from 4 aspects: biological process, molecular function, cellular component and cell/tissue/organ expression.
  • Immune and peripheral cell proteins tend to be mRNA stable/protein unstable.
  • The proteins involved in the cell adhesion tend to consist of large proteins with high proportion of small amino acids.
  • The proteins of organic acid transport, neurological system process and amine transport have significantly high hydrophobicity.
  • Interestingly, the proteins involved in olfactory receptor activity tend to have high frequency of aromatic, sulfuric and hydroxyl amino acids.

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  • (PMID = 28459865.001).
  • [ISSN] 1932-6203
  • [Journal-full-title] PloS one
  • [ISO-abbreviation] PLoS ONE
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Proteins; 0 / RNA, Messenger
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5. Denisov EV, Skryabin NA, Gerashchenko TS, Tashireva LA, Wilhelm J, Buldakov MA, Sleptcov AA, Lebedev IN, Vtorushin SV, Zavyalova MV, Cherdyntseva NV, Perelmuter VM: Clinically relevant morphological structures in breast cancer represent transcriptionally distinct tumor cell populations with varied degrees of epithelial-mesenchymal transition and CD44&lt;sup&gt;+&lt;/sup&gt;CD24&lt;sup&gt;-&lt;/sup&gt; stemness. Oncotarget; 2017 Sep 22;8(37):61163-61180
NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Clinically relevant morphological structures in breast cancer represent transcriptionally distinct tumor cell populations with varied degrees of epithelial-mesenchymal transition and CD44<sup>+</sup>CD24<sup>-</sup> stemness.
  • By contrast, morphological structures were characterized by specific gene expression profiles and signaling pathways and significantly differed in progesterone receptor and Ki-67 expression.
  • Solid (large shapeless) structures retained epithelial features but demonstrated an increase in mesenchymal traits and collective cell migration hallmarks.

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  • (PMID = 28977854.001).
  • [ISSN] 1949-2553
  • [Journal-full-title] Oncotarget
  • [ISO-abbreviation] Oncotarget
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; breast cancer / cancer invasion / cancer stem cell / epithelial-mesenchymal transition / tumor heterogeneity
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6. Jiráček J, Žáková L: Structural Perspectives of Insulin Receptor Isoform-Selective Insulin Analogs. Front Endocrinol (Lausanne); 2017;8:167

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Structural Perspectives of Insulin Receptor Isoform-Selective Insulin Analogs.
  • The insulin receptor (IR) exists in two alternatively spliced variants, IR-A and IR-B, with different tissue distribution.

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  • (PMID = 28798723.001).
  • [ISSN] 1664-2392
  • [Journal-full-title] Frontiers in endocrinology
  • [ISO-abbreviation] Front Endocrinol (Lausanne)
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; CT-peptide / IR-A / IR-B / binding affinity / exon 11 / insulin analog / insulin receptor isoform
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7. Dobitz S, Aronoff MR, Wennemers H: Oligoprolines as Molecular Entities for Controlling Distance in Biological and Material Sciences. Acc Chem Res; 2017 Oct 17;50(10):2420-2428
NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Nature utilizes large biomolecules to fulfill tasks that require spatially well-defined arrangements at the molecular level such as electron transfer, ligand-receptor interactions, or catalysis.
  • These molecules must ideally be equally applicable in aqueous and organic environments, they must be easy to synthesize in a controlled stepwise fashion, and they must be easily modified with a palette of chemical appendages having diverse functionalities.
  • Within the biological realm, we have applied oligoprolines to probe the role of distance on G-protein coupled receptor-mediated ligand uptake by cancerous cells and to investigate the effects of charge preorganization on the efficacy of cationic cell-penetrating peptides.

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  • NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .
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  • (PMID = 28885830.001).
  • [ISSN] 1520-4898
  • [Journal-full-title] Accounts of chemical research
  • [ISO-abbreviation] Acc. Chem. Res.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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8. 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 May;97(5):519-529
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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
  • [Chemical-registry-number] 0 / Bile Acids and Salts; 0 / Carrier Proteins; 0 / Membrane Glycoproteins; 0 / Receptors, Cytoplasmic and Nuclear; 0 / bile acid binding proteins; 516-35-8 / Taurochenodeoxycholic Acid; 60EUX8MN5X / tauroursodeoxycholic acid
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9. Taniguchi R, Inoue A, Sayama M, Uwamizu A, Yamashita K, Hirata K, Yoshida M, Tanaka Y, Kato HE, Nakada-Nakura Y, Otani Y, Nishizawa T, Doi T, Ohwada T, Ishitani R, Aoki J, Nureki O: Structural insights into ligand recognition by the lysophosphatidic acid receptor LPA&lt;sub&gt;6&lt;/sub&gt;. Nature; 2017 Aug 17;548(7667):356-360
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  • [Title] Structural insights into ligand recognition by the lysophosphatidic acid receptor LPA<sub>6</sub>.
  • Docking and mutagenesis analyses also indicated that the conserved positively charged residues within the central cavity recognize the phosphate head group of LPA by inducing an inward shift of transmembrane helices 6 and 7, suggesting that the receptor activation is triggered by this conformational rearrangement.

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  • (PMID = 28792932.001).
  • [ISSN] 1476-4687
  • [Journal-full-title] Nature
  • [ISO-abbreviation] Nature
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
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10. Hunakova L, Brtko J: Sn- and Ge- triorganometallics exert different cytotoxicity and modulation of migration in triple-negative breast cancer cell line MDA-MB-231. Toxicol Lett; 2017 Sep 05;279:16-21
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Sn- and Ge- triorganometallics exert different cytotoxicity and modulation of migration in triple-negative breast cancer cell line MDA-MB-231.
  • Among a variety of metal containing organic compounds, tin derivatives are enjoying an increasing interest and appear to be very promising as potential drug candidates.
  • We studied eight organometallic derivatives, nuclear retinoid X receptor (RXR) ligands and two germanium containing derivates that do not serve as RXR ligands.
  • [MeSH-major] Antineoplastic Agents / pharmacology. Cell Movement / drug effects. Organometallic Compounds / pharmacology. Organotin Compounds / pharmacology. Triple Negative Breast Neoplasms / drug therapy
  • [MeSH-minor] Apoptosis / drug effects. Caspase 3 / metabolism. Caspase 7 / metabolism. Cell Line, Tumor. Cell Proliferation / drug effects. Cell Survival / drug effects. Dose-Response Relationship, Drug. Female. Humans. Inhibitory Concentration 50. Neoplasm Invasiveness. Retinoid X Receptors / drug effects. Retinoid X Receptors / metabolism. Signal Transduction / drug effects. Time Factors. Trialkyltin Compounds / pharmacology

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  • Hazardous Substances Data Bank. TRI-N-BUTYLTIN HYDRIDE .
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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28709983.001).
  • [ISSN] 1879-3169
  • [Journal-full-title] Toxicology letters
  • [ISO-abbreviation] Toxicol. Lett.
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Antineoplastic Agents; 0 / Organometallic Compounds; 0 / Organotin Compounds; 0 / Retinoid X Receptors; 0 / Trialkyltin Compounds; 10038-98-9 / germanium chloride; 4XDX163P3D / tributyltin; 95T92AGN0V / triphenyltin; EC 3.4.22.- / CASP3 protein, human; EC 3.4.22.- / CASP7 protein, human; EC 3.4.22.- / Caspase 3; EC 3.4.22.- / Caspase 7
  • [Keywords] NOTNLM ; Apoptosis / Cytotoxicity / Nuclear retinoid x receptor / Triorganotin/triorganogermanium derivatives / Triple negative breast cancer
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11. Wang Y, Shang X, Liu J, Guo Y: ATP mediated rolling circle amplification and opening DNA-gate for drug delivery to cell. Talanta; 2018 Jan 01;176:652-658
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  • [Title] ATP mediated rolling circle amplification and opening DNA-gate for drug delivery to cell.
  • After the above-mentioned RCA process, its result that long DNA chain containing a base fragment complementary to gate DNA, would be hybridized to the gate DNA strand on the surface of MSN, which opened the MSN hole and released the drug DOX into cell for HeLa cell therapy.
  • And the specificity to folate receptor overexpressed on cell surface was satisfactory which would be beneficial for cancer therapy.

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  • [Copyright] Copyright © 2017. Published by Elsevier B.V.
  • (PMID = 28917803.001).
  • [ISSN] 1873-3573
  • [Journal-full-title] Talanta
  • [ISO-abbreviation] Talanta
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; ATP / Drug delivery / Mesoporous silica nanoparticle / Proximity ligation / Rolling circle amplification
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12. Castiglione GM, Schott RK, Hauser FE, Chang BSW: Convergent selection pressures drive the evolution of rhodopsin kinetics at high altitudes via non-parallel mechanisms. Evolution; 2017 Nov 16;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Convergent selection pressures drive the evolution of rhodopsin kinetics at high altitudes via non-parallel mechanisms.
  • Convergent evolution in response to similar selective pressures is a well-known phenomenon in evolutionary biology.
  • Less well understood is how selection drives convergence in protein function, and the underlying mechanisms by which this can be achieved.
  • Here we investigate functional convergence in the visual system of two distantly related lineages of high-altitude adapted Andean and Himalayan catfishes.
  • Statistical analyses revealed in the two high-altitude lineages, a parallel acceleration of evolutionary rates in rhodopsin, the dim-light visual pigment.
  • However, the elevated rates were found to be accompanied by substitutions at different sites in the protein.
  • Experiments substituting Andean- or Himalayan-specific residues significantly accelerated the kinetic rates of rhodopsin, destabilizing the ligand-bound forms.
  • As found in cold-adapted enzymes, this phenotype likely compensates for a cold-induced decrease in kinetic rates, properties of rhodopsin mediating rod sensitivity and visual performance.
  • Our study suggests that molecular convergence in protein function can be driven by parallel shifts in evolutionary rates but via non-parallel molecular mechanisms.
  • Signatures of natural selection may therefore be a powerful guide for identifying complex instances of functional convergence across a wider range of protein systems.
  • This article is protected by copyright.
  • All rights reserved.

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  • [Copyright] This article is protected by copyright. All rights reserved.
  • (PMID = 29143302.001).
  • [ISSN] 1558-5646
  • [Journal-full-title] Evolution; international journal of organic evolution
  • [ISO-abbreviation] Evolution
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; G protein-coupled receptor / codon models of evolution / dim-light vision / high altitude catfish / molecular convergence / protein cold adaptation / visual pigment
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13. Li L, Weng Y, Wang W, Bai M, Lei H, Zhou H, Jiang H: Multiple organic cation transporters contribute to the renal transport of sulpiride. Biopharm Drug Dispos; 2017 Dec;38(9):526-534
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  • [Title] Multiple organic cation transporters contribute to the renal transport of sulpiride.
  • Sulpiride, a selective dopamine D2 receptor blocker, is used widely for the treatment of schizophrenia, depression and gastric/duodenal ulcers.
  • The results demonstrated that sulpiride was a substrate of human carnitine/organic cation transporter 1 (hOCTN1) and 2 (hOCTN2), human organic cation transporter 2 (hOCT2), human multidrug and toxin efflux extrusion protein 1 (hMATE1) and 2-K (hMATE2-K).
  • Sulpiride accumulation from the basolateral (BL) to the apical (AP) side in MDCK-hOCT2/pcDNA3.1 cell monolayers was much greater than that in MDCK-hOCT2/hMATE1 cells, and cimetidine dramatically reduced the intracellular accumulation of sulpiride from BL to AP.

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  • [Copyright] Copyright © 2017 John Wiley & Sons, Ltd.
  • (PMID = 28926871.001).
  • [ISSN] 1099-081X
  • [Journal-full-title] Biopharmaceutics & drug disposition
  • [ISO-abbreviation] Biopharm Drug Dispos
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; primary renal tubular cells / renal transfer / sulpiride / transporters
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14. Truebenbach I, Gorges J, Kuhn J, Kern S, Baratti E, Kazmaier U, Wagner E, Lächelt U: Sequence-Defined Oligoamide Drug Conjugates of Pretubulysin and Methotrexate for Folate Receptor Targeted Cancer Therapy. Macromol Biosci; 2017 Oct;17(10)

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Sequence-Defined Oligoamide Drug Conjugates of Pretubulysin and Methotrexate for Folate Receptor Targeted Cancer Therapy.
  • The conjugation of small molecule drugs to ligand containing carrier systems facilitates receptor targeted delivery.
  • The folate receptor (FR) constitutes an ideal target for tumor selective therapy, being overexpressed on several tumor types.
  • Their structure activity relationships are assessed in respect to dihydrofolate reductase inhibition, receptor mediated endocytosis, and cytotoxicity.
  • In a combined PT/MTX cytotoxicity study in FR-overexpressing KB and L1210 cells, a 2-arm MTX-PT construct or the 4-arm analog displays the highest potency in the respective cell lines.

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  • [Copyright] © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
  • (PMID = 28371444.001).
  • [ISSN] 1616-5195
  • [Journal-full-title] Macromolecular bioscience
  • [ISO-abbreviation] Macromol Biosci
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; combination therapy / drug conjugate / methotrexate / pretubulysin / targeting
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15. Nagy L, Márton J, Vida A, Kis G, Bokor É, Kun S, Gönczi M, Docsa T, Tóth A, Antal M, Gergely P, Csóka B, Pacher P, Somsák L, Bai P: Glycogen phosphorylase inhibition improves beta cell function. Br J Pharmacol; 2017 Apr 13;
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  • [Title] Glycogen phosphorylase inhibition improves beta cell function.
  • Glycogen metabolism has implications in beta cell function.
  • Furthermore, GPi treatment induced insulin receptor β (InsRβ), Akt and p70S6K phosphorylation, as well as pancreatic and duodenal homeobox 1(PDX1) and insulin expression.
  • CONCLUSION AND IMPLICATIONS: These data suggest that GPi-s also target beta cells and can be repurposed as agents to preserve beta cell function or even ameliorate beta cell dysfunction in different forms of diabetes.

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  • [Copyright] © 2017 The British Pharmacological Society.
  • (PMID = 28409826.001).
  • [ISSN] 1476-5381
  • [Journal-full-title] British journal of pharmacology
  • [ISO-abbreviation] Br. J. Pharmacol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
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16. Amata E, Dichiara M, Arena E, Pittalà V, Pistarà V, Cardile V, Graziano ACE, Fraix A, Marrazzo A, Sortino S, Prezzavento O: Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect. J Med Chem; 2017 Dec 14;60(23):9531-9544

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Novel Sigma Receptor Ligand-Nitric Oxide Photodonors: Molecular Hybrids for Double-Targeted Antiproliferative Effect.
  • This contribution reports the synthesis and evaluation of novel hybrid compounds that conjugate a sigma (σ) receptor pharmacophore and a nitric oxide (NO) photodonor.
  • All compounds preserve their capability to generate NO under visible light and possess overall σ receptor nanomolar affinity, with one of them (8b) exhibiting remarkable σ<sub>2</sub> receptor selectivity.
  • Compounds 8b, 11a, and 11b were tested on tumorigenic MCF-7 and A2058 cells expressing high levels of σ<sub>2</sub> and σ<sub>1</sub> receptor, respectively.
  • Considerable loss of cell viability was detected under light excitation, while negligible effects in the dark were detected.
  • NO-induced reduction of cellular viability was demonstrated by in-cell NO detection and total nitrite estimation.
  • For the first time, a combination of σ receptor moieties and a NO photodonor is reported, providing distinctive ligands potentially useful for cancer management.

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  • (PMID = 29172528.001).
  • [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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17. Nami B, Wang Z: Application of Immunofluorescence Staining to Study ErbB Family of Receptor Tyrosine Kinases. Methods Mol Biol; 2017;1652:109-116
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Application of Immunofluorescence Staining to Study ErbB Family of Receptor Tyrosine Kinases.
  • Immunofluorescence staining is an effective method for visualizing ErbB family of receptor tyrosine kinases and to monitor their expression, phosphorylation, and localization in individual cells.
  • However, immunofluorescence staining for membrane proteins is required preserving integrity of cell membrane intact by protecting the cells from organic solvents.

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  • (PMID = 28791637.001).
  • [ISSN] 1940-6029
  • [Journal-full-title] Methods in molecular biology (Clifton, N.J.)
  • [ISO-abbreviation] Methods Mol. Biol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; EGFR / ErbB / HER2 / Immunofluorescence / Receptor / Staining
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18. 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 04;1864(4):613-624
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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; Research Support, Non-U.S. Gov't
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / GRB2 Adaptor Protein; 0 / GRB2 protein, human; 0 / RNA, Small Interfering; 0 / Stilbenes; 26R60S6A5I / pterostilbene; EC 2.7.1.1 / MTOR protein, human; EC 2.7.1.1 / TOR Serine-Threonine Kinases; EC 2.7.11.1 / AMP-Activated Protein Kinases; EC 3.6.1.- / RAB13 protein, human; EC 3.6.5.2 / rab GTP-Binding Proteins
  • [Keywords] NOTNLM ; AMP-activated protein kinase (major topic) / Growth factor receptor-bound protein 2 (major topic) / Macroautophagy (major topic) / Pterostilbene (major topic) / Small GTPase Rab13 (major topic) / Vascular endothelial cell (major topic)
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19. Chatziathanasiadou MV, Geromichalou EG, Sayyad N, Vrettos EI, Katsikoudi A, Stylos E, Bellou S, Geromichalos GD, Tzakos AG: Amplifying and broadening the cytotoxic profile of quercetin in cancer cell lines through bioconjugation. Amino Acids; 2017 Nov 28;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Amplifying and broadening the cytotoxic profile of quercetin in cancer cell lines through bioconjugation.
  • Quercetin is a flavonoid presenting cytotoxicity against different cancer cell lines.
  • A quercetin-alanine bioconjugate was synthesized, its cellular internalization was monitored through confocal microscopy and its cytotoxic activity was explored against ten different cell lines.
  • In silico studies suggested that quercetin-alanine possesses enhanced binding affinity to human estrogen receptor alpha corroborating to its activity to MCF-7, overexpressing this receptor.

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  • (PMID = 29185031.001).
  • [ISSN] 1438-2199
  • [Journal-full-title] Amino acids
  • [ISO-abbreviation] Amino Acids
  • [Language] eng
  • [Grant] United States / by Greek national funds through the operational program "THESSALY- MAINLAND GREECE AND EPIRUS-2007 to 2013" of the National Strategic Reference Framework (NSRF 2007 to 2013) / / not applicable
  • [Publication-type] Journal Article
  • [Publication-country] Austria
  • [Keywords] NOTNLM ; BSA / Cytotoxic activity / Fluorescence spectroscopy / Isothermal titration calorimetry / Natural product / Quercetin–alanine
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20. El-Azab AS, Al-Dhfyan A, Abdel-Aziz AA, Abou-Zeid LA, Alkahtani HM, Al-Obaid AM, Al-Gendy MA: Synthesis, anticancer and apoptosis-inducing activities of quinazoline-isatin conjugates: epidermal growth factor receptor-tyrosine kinase assay and molecular docking studies. J Enzyme Inhib Med Chem; 2017 Dec;32(1):935-944
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  • [Title] Synthesis, anticancer and apoptosis-inducing activities of quinazoline-isatin conjugates: epidermal growth factor receptor-tyrosine kinase assay and molecular docking studies.
  • The antitumor efficacy of the compounds against MDA-MB-231, a breast cancer cell line, and LOVO, a colon cancer cell line, was assessed.
  • [MeSH-major] Antineoplastic Agents / pharmacology. Apoptosis / drug effects. Isatin / pharmacology. Molecular Docking Simulation. Quinazolines / pharmacology. Receptor, Epidermal Growth Factor / antagonists & inhibitors
  • [MeSH-minor] Cell Line, Tumor. Cell Proliferation / drug effects. Drug Screening Assays, Antitumor. Humans. Molecular Structure. Structure-Activity Relationship

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  • (PMID = 28718672.001).
  • [ISSN] 1475-6374
  • [Journal-full-title] Journal of enzyme inhibition and medicinal chemistry
  • [ISO-abbreviation] J Enzyme Inhib Med Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Antineoplastic Agents; 0 / Quinazolines; 82X95S7M06 / Isatin; EC 2.7.10.1 / EGFR protein, human; EC 2.7.10.1 / Receptor, Epidermal Growth Factor
  • [Keywords] NOTNLM ; EGFR-TK / Synthesis / antitumor / isatin / molecular docking / quinazolinone
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21. 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] Evaluation Studies; Journal Article
  • [Publication-country] France
  • [Chemical-registry-number] 0 / 3-(4-(2-(2,5-bis-trifluoromethyl-phenyl)-acetylamino)-phenyl)-coumarin-7-O-sulfamate; 0 / 3-(4-(3,4-difluoro-benzoylamino)-phenyl)-coumarin-7-O-sulfamate; 0 / Coumarins; 0 / Enzyme Inhibitors; 0 / Receptors, Estrogen; 0 / Sulfonamides; 0 / coumarin 7-O-sulfamate; EC 3.1.6.2 / Steryl-Sulfatase
  • [Keywords] NOTNLM ; Breast cancer (major topic) / Coumarin (major topic) / STS inhibitors (major topic) / Steroid sulfatase (major topic) / Sulfamates (major topic)
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22. Kang TH, Yoon G, Kang IA, Oh HN, Chae JI, Shim JH: Natural Compound Licochalcone B Induced Extrinsic and Intrinsic Apoptosis in Human Skin Melanoma (A375) and Squamous Cell Carcinoma (A431) Cells. Phytother Res; 2017 Dec;31(12):1858-1867
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  • [Title] Natural Compound Licochalcone B Induced Extrinsic and Intrinsic Apoptosis in Human Skin Melanoma (A375) and Squamous Cell Carcinoma (A431) Cells.
  • Licochalcone B (Lico B), which is normally isolated from the roots of Glycyrrhiza inflata (Chinese Licorice), generally classified into organic compounds including retrochalcones.
  • However, its biological effects on melanoma and squamous cell carcinoma (SCC) are unknown.
  • Based on these known facts, this study investigated the role of Lico B in apoptosis, through the extrinsic and intrinsic pathways and additional regulation of specificity protein 1 in human skin cancer cell lines.
  • Annexin V/7-aminoactinomycin D staining, western blot analysis, mitochondrial membrane potential assay, and an anchorage-independent cell transformation assay demonstrated that Lico B treatment of human melanoma and SCC cells significantly inhibited cell proliferation and induced apoptotic cell death.

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  • [Copyright] Copyright © 2017 John Wiley & Sons, Ltd.
  • (PMID = 29027311.001).
  • [ISSN] 1099-1573
  • [Journal-full-title] Phytotherapy research : PTR
  • [ISO-abbreviation] Phytother Res
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; apoptosis / death receptor / human skin cancer / licochalcone B / mitochondrial membrane potential / specificity protein 1
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23. Kruglov E, Ananthanarayanan M, Sousa P, Weerachayaphorn J, Guerra MT, Nathanson MH: Type 2 inositol trisphosphate receptor gene expression in hepatocytes is regulated by cyclic AMP. Biochem Biophys Res Commun; 2017 05 06;486(3):659-664
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  • [Title] Type 2 inositol trisphosphate receptor gene expression in hepatocytes is regulated by cyclic AMP.
  • The type 2 inositol 1,4,5-trisphosphate receptor (IP3R2) is the principal intracellular Ca<sup>2+</sup> release channel in hepatocytes, and so is important for bile secretion and other functions.
  • Adenylyl cyclase (AC) 6 and 9 were the principal AC isoforms detected in rat hepatocytes, and silencing either one decreased organic anion secretion, which depends on IP3R2.
  • [MeSH-minor] Adenylyl Cyclases / genetics. Adenylyl Cyclases / metabolism. Animals. Binding Sites. Colforsin / pharmacology. Dactinomycin / pharmacology. Fasting. Gene Expression Regulation. Hep G2 Cells. Humans. Male. Mutation. Primary Cell Culture. Promoter Regions, Genetic. Protein Binding. Rats. Rats, Sprague-Dawley. Signal Transduction. Thionucleotides / pharmacology

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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
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  • (PMID = 28327356.001).
  • [ISSN] 1090-2104
  • [Journal-full-title] Biochemical and biophysical research communications
  • [ISO-abbreviation] Biochem. Biophys. Res. Commun.
  • [Language] eng
  • [Grant] United States / NIDDK NIH HHS / DK / P01 DK057751; United States / NIDDK NIH HHS / DK / P30 DK034989; United States / NIDDK NIH HHS / DK / R01 DK045710; United States / NIDDK NIH HHS / DK / R56 DK099470
  • [Publication-type] Journal Article; Research Support, N.I.H., Extramural
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Inositol 1,4,5-Trisphosphate Receptors; 0 / RNA, Messenger; 0 / Thionucleotides; 1CC1JFE158 / Dactinomycin; 1F7A44V6OU / Colforsin; 41941-66-6 / 8-((4-chlorophenyl)thio)cyclic-3',5'-AMP; E0399OZS9N / Cyclic AMP; EC 2.3.1.48 / CREB-Binding Protein; EC 2.3.1.48 / Crebbp protein, rat; EC 4.6.1.1 / Adenylyl Cyclases; EC 4.6.1.1 / adenylate cyclase 9; EC 4.6.1.1 / adenylyl cyclase 6
  • [Keywords] NOTNLM ; Bile secretion (major topic) / Calcium signaling (major topic) / Cyclic AMP (major topic) / Hepatocytes (major topic) / Type 2 inositol 1,4,5-trisphosphate receptor (major topic)
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24. Jiang XF, Dai Y, Peng X, Shen YY, Su Y, Wei MM, Liu WR, Ding ZB, Zhang A, Shi YH, Ai J: SOMCL-085, a novel multi-targeted FGFR inhibitor, displays potent anticancer activity in FGFR-addicted human cancer models. Acta Pharmacol Sin; 2017 Sep 14;
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  • Aberrant fibroblast growth factor receptor (FGFR) activation is found across a diverse spectrum of malignancies, especially those lacking effective treatments.
  • In 3 representative human cancer cell lines with different mechanisms of FGFR activation tested, SOMCL-085 (20-500 nmol/L) dose-dependently inhibited FGFR1-3 phosphorylation and the phosphorylation of their key downstream effectors PLCγ and Erk.
  • In 7 FGFR aberrant human cancer cell lines, regardless of the mechanistic complexity of FGFR over-activation, SOMCL-085 potently inhibited FGFR-driven cell proliferation by arresting cells at the G<sub>1</sub>/S phase.
  • In the FGFR1-amplified lung cancer cell line H1581 xenograft mice and FGFR2-amplified gastric cancer cell line SNU16 xenograft mice, oral administration of SOMCL-085 (25, 50 mg·kg<sup>-1</sup>·d<sup>-1</sup>) for 21 days substantially suppressed tumor growth without affecting their body-weight.

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  • (PMID = 28905937.001).
  • [ISSN] 1745-7254
  • [Journal-full-title] Acta pharmacologica Sinica
  • [ISO-abbreviation] Acta Pharmacol. Sin.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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25. Honda A, Fukushima W, Oishi M, Tsuji K, Sawahara T, Hayashi T, Kudo H, Kashima Y, Takahashi K, Sasaki H, Ueda K, Takano H: Effects of Components of PM&lt;sub&gt;2.5&lt;/sub&gt; Collected in Japan on the Respiratory and Immune Systems. Int J Toxicol; 2017 Mar/Apr;36(2):153-164
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  • Airway epithelial cells and immune cells were exposed to aqueous or organic extracts of PM<sub>2.5</sub>.
  • Exposure to extracts from both areas, especially to organic extracts rather than aqueous extracts, caused a pro-inflammatory response via interleukin (IL) 6 production from airway epithelial cells, and it induced the maturation/activation of bone marrow-derived antigen-presenting cells via dendritic and epithelial cell (DEC) 205 and cluster of differentiation (CD) 86 expression and proportional changes in the constitution of the splenocytes.
  • These results suggest that organic components of PM<sub>2.5</sub> affect the respiratory and immune systems.
  • [MeSH-minor] Animals. Antigens, CD / metabolism. Antigens, CD19 / metabolism. Antigens, CD86 / metabolism. Biomarkers / metabolism. Bronchi / cytology. Cell Line. Cell Survival / drug effects. Humans. Interleukin-6 / metabolism. Japan. Lectins, C-Type / metabolism. Male. Mice. Minor Histocompatibility Antigens / metabolism. Nitrogen Oxides / toxicity. Receptors, Antigen, T-Cell / metabolism. Receptors, Cell Surface / metabolism. Spleen / cytology. Sulfur Dioxide / toxicity

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  • (PMID = 28056587.001).
  • [ISSN] 1092-874X
  • [Journal-full-title] International journal of toxicology
  • [ISO-abbreviation] Int. J. 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 / Antigens, CD; 0 / Antigens, CD19; 0 / Antigens, CD86; 0 / Biomarkers; 0 / DEC-205 receptor; 0 / Interleukin-6; 0 / Lectins, C-Type; 0 / Minor Histocompatibility Antigens; 0 / Nitrogen Oxides; 0 / Particulate Matter; 0 / Receptors, Antigen, T-Cell; 0 / Receptors, Cell Surface; 0UZA3422Q4 / Sulfur Dioxide
  • [Keywords] NOTNLM ; PM2.5 (major topic) / aqueous extracts (major topic) / asthma (major topic) / industrial area (major topic) / organic extracts (major topic) / urban area (major topic)
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26. Ahijado-Guzmán R, Menten J, Prasad J, Lambertz C, Rivas G, Sönnichsen C: Plasmonic Nanosensors for the Determination of Drug Effectiveness on Membrane Receptors. ACS Appl Mater Interfaces; 2017 01 11;9(1):218-223

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  • As the NanoSPR method relies on individual gold nanorods as sensing elements, there is no need for fluorescent labels or organic cosolvents, and it provides intrinsically high statistics.
  • [MeSH-minor] Bacterial Proteins. Carrier Proteins. Cell Cycle Proteins. Cytoskeletal Proteins. Escherichia coli. Escherichia coli Proteins. Protein Binding. Surface Plasmon Resonance

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  • (PMID = 27976859.001).
  • [ISSN] 1944-8252
  • [Journal-full-title] ACS applied materials & interfaces
  • [ISO-abbreviation] ACS Appl Mater Interfaces
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Bacterial Proteins; 0 / Carrier Proteins; 0 / Cell Cycle Proteins; 0 / Cytoskeletal Proteins; 0 / Escherichia coli Proteins
  • [Keywords] NOTNLM ; FtsZ inhibitors (major topic) / NanoSPR (major topic) / drug effectiveness (major topic) / optical dark-field spectroscopy (major topic) / plasmonic nanosensors (major topic) / protein−membrane receptor interactions (major topic)
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27. Korsak B, Almeida GM, Rocha S, Pereira C, Mendes N, Osório H, Pereira PMR, Rodrigues JMM, Schneider RJ, Sarmento B, Tomé JPC, Oliveira C: Porphyrin modified trastuzumab improves efficacy of HER2 targeted photodynamic therapy of gastric cancer. Int J Cancer; 2017 Oct 01;141(7):1478-1489
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  • Human epidermal growth factor receptor-2 (HER2) is overexpressed in ∼20% of GC cases and anti-HER2 antibody trastuzumab in combination with conventional chemotherapy, is recognized as standard therapy for HER2-positive metastatic GC.
  • The in vitro data demonstrates that Trast:Porph specifically binds to HER2-positive cells, accumulates intracellularly, co-localizes with lysosomal marker LAMP1, and induces massive HER2-positive cell death upon cellular irradiation.
  • The high selectivity and cytotoxicity of Trast:Porph based photoimmunotherapy is confirmed in vivo in comparison with trastuzumab alone, using nude mice xenografted with a HER2-positive GC cell line.
  • [MeSH-major] Antineoplastic Agents / therapeutic use. Cell Death. Immunotherapy / methods. Photochemotherapy / methods. Porphyrins / therapeutic use. Receptor, ErbB-2. Stomach Neoplasms / drug therapy. Trastuzumab / therapeutic use
  • [MeSH-minor] Animals. Cell Line, Tumor. Cell Survival / drug effects. Humans. Lysine / chemistry. Lysosome-Associated Membrane Glycoproteins / pharmacokinetics. Male. Mass Spectrometry. Mice, Nude. Random Allocation. Xenograft Model Antitumor Assays

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  • [Copyright] © 2017 UICC.
  • (PMID = 28639285.001).
  • [ISSN] 1097-0215
  • [Journal-full-title] International journal of cancer
  • [ISO-abbreviation] Int. J. Cancer
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Antineoplastic Agents; 0 / LAMP1 protein, human; 0 / Lysosome-Associated Membrane Glycoproteins; 0 / Porphyrins; EC 2.7.10.1 / ERBB2 protein, human; EC 2.7.10.1 / Receptor, ErbB-2; K3Z4F929H6 / Lysine; P188ANX8CK / Trastuzumab
  • [Keywords] NOTNLM ; HER2 / gastric cancer / photoimmunoconjugate / photoimmunotherapy / trastuzumab
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28. Prokhorov NS, Riccio C, Zdorovenko EL, Shneider MM, Browning C, Knirel YA, Leiman PG, Letarov AV: Function of bacteriophage G7C esterase tailspike in host cell adsorption. Mol Microbiol; 2017 Aug;105(3):385-398

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  • [Title] Function of bacteriophage G7C esterase tailspike in host cell adsorption.
  • Bacteriophages recognize and bind to their hosts with the help of receptor-binding proteins (RBPs) that emanate from the phage particle in the form of fibers or tailspikes.

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  • [Copyright] © 2017 John Wiley & Sons Ltd.
  • (PMID = 28513100.001).
  • [ISSN] 1365-2958
  • [Journal-full-title] Molecular microbiology
  • [ISO-abbreviation] Mol. Microbiol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Polysaccharides, Bacterial; 0 / Viral Tail Proteins; EC 3.1.- / Esterases
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29. Planas-Rigol E, Terrades-Garcia N, Corbera-Bellalta M, Lozano E, Alba MA, Segarra M, Espígol-Frigolé G, Prieto-González S, Hernández-Rodríguez J, Preciado S, Lavilla R, Cid MC: Endothelin-1 promotes vascular smooth muscle cell migration across the artery wall: a mechanism contributing to vascular remodelling and intimal hyperplasia in giant-cell arteritis. Ann Rheum Dis; 2017 Sep;76(9):1624-1634
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  • [Title] Endothelin-1 promotes vascular smooth muscle cell migration across the artery wall: a mechanism contributing to vascular remodelling and intimal hyperplasia in giant-cell arteritis.
  • BACKGROUND: Giant-cell arteritis (GCA) is an inflammatory disease of large/medium-sized arteries, frequently involving the temporal arteries (TA).
  • In inflamed arteries, ET-1 was predominantly expressed by infiltrating mononuclear cells whereas ET receptors, particularly ET-1 receptor B (ET<sub>B</sub>R), were expressed by both mononuclear cells and VSMC.
  • ET-1 promoted VSMC motility by increasing activation of focal adhesion kinase (FAK), a crucial molecule in the turnover of focal adhesions during cell migration.
  • Consistently, ET-1 receptor A and ET<sub>B</sub>R antagonists reduced αSMA expression and delayed VSMC outgrowth from cultured GCA-involved artery explants.
  • [MeSH-major] Cell Movement / genetics. Endothelin-1 / genetics. Giant Cell Arteritis / genetics. Muscle, Smooth, Vascular / metabolism. Myocytes, Smooth Muscle / metabolism. Vascular Remodeling / genetics
  • [MeSH-minor] Actins / drug effects. Actins / genetics. Actins / metabolism. Aged. Blotting, Western. Case-Control Studies. Endothelin Receptor Antagonists / pharmacology. Female. Fluorescent Antibody Technique. Focal Adhesion Kinase 1 / antagonists & inhibitors. Focal Adhesion Kinase 1 / metabolism. Humans. Hyperplasia. In Vitro Techniques. Leukocytes, Mononuclear. Male. Microscopy, Confocal. Phosphatidylinositol 3-Kinases / antagonists & inhibitors. Phosphatidylinositol 3-Kinases / metabolism. Phosphorylation. Receptor, Endothelin A / drug effects. Receptor, Endothelin A / metabolism. Receptor, Endothelin B / metabolism. Reverse Transcriptase Polymerase Chain Reaction. Tunica Intima / pathology. src-Family Kinases / metabolism

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  • [Copyright] © Article author(s) (or their employer(s) unless otherwise stated in the text of the article) 2017. All rights reserved. No commercial use is permitted unless otherwise expressly granted.
  • (PMID = 28606962.001).
  • [ISSN] 1468-2060
  • [Journal-full-title] Annals of the rheumatic diseases
  • [ISO-abbreviation] Ann. Rheum. Dis.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / ACTA2 protein, human; 0 / Actins; 0 / Endothelin Receptor Antagonists; 0 / Endothelin-1; 0 / Receptor, Endothelin A; 0 / Receptor, Endothelin B; EC 2.7.1.- / Phosphatidylinositol 3-Kinases; EC 2.7.10.2 / Focal Adhesion Kinase 1; EC 2.7.10.2 / PTK2 protein, human; EC 2.7.10.2 / src-Family Kinases
  • [Keywords] NOTNLM ; 5-bisphosphate 3-kinase (PI3K) / Giant-cell arteritis / Src kinase / cell migration / endothelin / extracellular signal -regulated kinase / focal adhesion kinase / matrix metaloproteinases. Heterotrimeric G proteins. / myofibroblast / phosphatidylinositol-4 / vascular inflammation / vascularremodelling
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30. Guesdon W, Kosaraju R, Brophy P, Clark A, Dillingham S, Aziz S, Moyer F, Willson K, Dick JR, Patil SP, Balestrieri N, Armstrong M, Reisdroph N, Shaikh SR: Effects of fish oils on ex vivo B-cell responses of obese subjects upon BCR/TLR stimulation: a pilot study. J Nutr Biochem; 2017 Nov 02;53:72-80

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  • [Title] Effects of fish oils on ex vivo B-cell responses of obese subjects upon BCR/TLR stimulation: a pilot study.
  • Therefore, in this pilot study, we tested how n-3 LC-PUFAs influence B-cell responses of obese humans.
  • Next, ex vivo B-cell cytokines were assayed after stimulation of Toll-like receptors (TLRs) and/or the B-cell receptor (BCR) to determine if the effects of n-3 LC-PUFAs were pathway-dependent.
  • B-cell IL-10 and TNFα secretion was respectively increased with high DHA-FO (n=10), relative to baseline, with respective TLR9 and TLR9+BCR stimulation.
  • OO (n=12) and FO (n=12) had no influence on B-cell cytokines compared to baseline, and there were no differences in postintervention cytokine levels between treatment groups.
  • Altogether, the results suggest that n-3 LC-PUFAs could modulate B-cell activity in humans, which will require further testing in a larger cohort.

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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
  • (PMID = 29195133.001).
  • [ISSN] 1873-4847
  • [Journal-full-title] The Journal of nutritional biochemistry
  • [ISO-abbreviation] J. Nutr. Biochem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Antibody levels / B cells / B-cell receptor / Cytokines / Fish oil / Lipidomics / Toll-like receptors
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31. 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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  • [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.
  • [MeSH-minor] ADP-ribosyl Cyclase 1 / metabolism. Actin Cytoskeleton / metabolism. Animals. COS Cells. Cell Line. Cercopithecus aethiops. Female. Male. Mice. RAW 264.7 Cells

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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
  • [Chemical-registry-number] 0 / Liver X Receptors; 0 / Receptors, Cytoplasmic and Nuclear; 0U46U6E8UK / NAD; EC 3.2.2.6 / ADP-ribosyl Cyclase 1
  • [Keywords] NOTNLM ; CD38 / LXR / NAD / bacterial infection / cytoskeleton / macrophage / nuclear receptor
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32. Pesce M, D'Alessandro A, Borrelli O, Gigli S, Seguella L, Cuomo R, Esposito G, Sarnelli G: Endocannabinoid-related compounds in gastrointestinal diseases. J Cell Mol Med; 2017 Oct 09;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • In recent years, it has become apparent that the ECS is pivotal in the regulation of GI motility, secretion and sensitivity, but endocannabinoids (ECs) are also involved in the regulation of intestinal inflammation and mucosal barrier permeability, suggesting their role in the pathophysiology of both functional and organic GI disorders.
  • Genetic studies in patients with irritable bowel syndrome (IBS) or inflammatory bowel disease have indeed shown significant associations with polymorphisms or mutation in genes encoding for cannabinoid receptor or enzyme responsible for their catabolism, respectively.

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  • [Copyright] © 2017 The Authors. Journal of Cellular and Molecular Medicine published by John Wiley & Sons Ltd and Foundation for Cellular and Molecular Medicine.
  • (PMID = 28990365.001).
  • [ISSN] 1582-4934
  • [Journal-full-title] Journal of cellular and molecular medicine
  • [ISO-abbreviation] J. Cell. Mol. Med.
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] England
  • [Keywords] NOTNLM ; endocannabinoid system / functional gastrointestinal disorders / gastrointestinal pathophysiology / inflammatory bowel disease / non-alcoholic steatohepatitis
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33. Pati ML, Fanizza E, Hager S, Groza D, Heffeter P, Laurenza AG, Laquintana V, Curri ML, Depalo N, Abate C, Denora N: Quantum Dot Based Luminescent Nanoprobes for Sigma-2 Receptor Imaging. Mol Pharm; 2017 Dec 11;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Quantum Dot Based Luminescent Nanoprobes for Sigma-2 Receptor Imaging.
  • The increasing importance of sigma-2 receptor as target for the diagnosis and therapy of tumours paves the way for the development of innovative optically traceable fluorescent probes as tumour cell contrast and therapeutic agents.
  • Here, a novel hybrid organic-inorganic nanostructure is developed by combining the superior fluorescent properties of inorganic quantum dots (QDs), coated with a hydrophilic silica shell (QD@SiO2 NPs), the versatility of the silica shell and the high selectivity for sigma-2 receptors of the two synthetic ligands, namely the 6-[(6-aminohexyl)oxy]-2-(3-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)propyl)-3,4-dihydroisoquinolin-1(2H)-one (MLP66) and 6-[1-[3-(4-cyclohexylpiperazin-1-yl)propyl]-1,2,3,4-tetrahydronaphthalen-5-yloxy]hexylamine (TA6).
  • Therefore, the proposed nanostructures represent a challenging alternative to all previously studied organic small fluorescent molecules, based on the same sigma-2 receptor affinity moieties.
  • The presented QD-based nanoprobes possess a great potential as in vitro selective sigma-2 receptor imaging agent and, consequently, could provide a significant impact to future theranostic applications.

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  • (PMID = 29226684.001).
  • [ISSN] 1543-8392
  • [Journal-full-title] Molecular pharmaceutics
  • [ISO-abbreviation] Mol. Pharm.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
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34. Thakkar SS, Thakor P, Ray A, Doshi H, Thakkar VR: Benzothiazole analogues: Synthesis, characterization, MO calculations with PM6 and DFT, in silico studies and in vitro antimalarial as DHFR inhibitors and antimicrobial activities. Bioorg Med Chem; 2017 10 15;25(20):5396-5406
Hazardous Substances Data Bank. BENZOTHIAZOLE .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • The active compounds J 1, J 2, J 3, J 5 and J 6 were further evaluated for enzyme inhibition efficacy against the receptor Pf-DHFR, computational and in vitro studies were carried out to examine their candidatures as lead dihydrofolate reductase inhibitors.
  • [MeSH-minor] Cell Survival / drug effects. Computer Simulation. Dose-Response Relationship, Drug. Gram-Negative Bacteria / drug effects. Gram-Positive Bacteria / drug effects. Microbial Sensitivity Tests. Molecular Structure. Plasmodium falciparum / drug effects. Quantum Theory. Schizosaccharomyces / cytology. Schizosaccharomyces / drug effects. Structure-Activity Relationship. Tetrahydrofolate Dehydrogenase / metabolism

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  • [Copyright] Copyright © 2017 Elsevier Ltd. All rights reserved.
  • (PMID = 28789907.001).
  • [ISSN] 1464-3391
  • [Journal-full-title] Bioorganic & medicinal chemistry
  • [ISO-abbreviation] Bioorg. Med. Chem.
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Anti-Bacterial Agents; 0 / Antifungal Agents; 0 / Antimalarials; 0 / Benzothiazoles; 0 / Folic Acid Antagonists; EC 1.5.1.3 / Tetrahydrofolate Dehydrogenase; G5BW2593EP / benzothiazole
  • [Keywords] NOTNLM ; Antimalarial activity (major topic) / Antimicrobial activity (major topic) / Benzothiazole (major topic) / DFT (major topic) / DHFR (major topic) / Molecular docking (major topic) / PM6 (major topic)
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35. Fu L, Hu H, Liu Y, Jing Z, Li W: Woodchuck sodium taurocholate cotransporting polypeptide supports low-level hepatitis B and D virus entry. Virology; 2017 May;505:1-11
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  • Sodium taurocholate cotransporting polypeptide (NTCP) is the functional receptor for human hepatitis B virus (HBV) and its satellite hepatitis D virus (HDV).
  • [MeSH-major] Hepatitis B virus / metabolism. Hepatitis Delta Virus / metabolism. Host Specificity / genetics. Organic Anion Transporters, Sodium-Dependent / genetics. Receptors, Virus / genetics. Symporters / genetics. Virus Internalization
  • [MeSH-minor] Amino Acid Sequence / genetics. Animals. Binding Sites / genetics. Cell Line, Tumor. Cloning, Molecular. Hep G2 Cells. Hepatocytes / virology. Humans. Liver / metabolism. Liver / virology. Male. Marmota / virology. Protein Binding / genetics

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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
  • (PMID = 28213271.001).
  • [ISSN] 1096-0341
  • [Journal-full-title] Virology
  • [ISO-abbreviation] Virology
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Organic Anion Transporters, Sodium-Dependent; 0 / Receptors, Virus; 0 / Symporters; 145420-23-1 / sodium-bile acid cotransporter
  • [Keywords] NOTNLM ; Hepatitis B virus / Hepatitis D virus / Sodium taurocholate cotransporting polypeptide / Viral entry / Woodchuck
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36. 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 May;32(5):1628-1636
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [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.
  • [MeSH-major] Interleukin-8 / metabolism. Lung Diseases. Mitogen-Activated Protein Kinases / metabolism. NF-kappa B / metabolism. Particulate Matter / toxicity. Receptor, Epidermal Growth Factor / metabolism

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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
  • [Chemical-registry-number] 0 / Interleukin-8; 0 / NF-kappa B; 0 / Particulate Matter; EC 2.7.10.1 / Receptor, Epidermal Growth Factor; EC 2.7.11.24 / Mitogen-Activated Protein Kinases
  • [Keywords] NOTNLM ; Cytokine / epidermal growth factor receptor (EGFR) / erlotinib / mitogen-activated protein kinase (MAPK) / particulate matter2.5(PM2.5)
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37. 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
  • [Chemical-registry-number] 0 / Antioxidants; 0 / Neuroprotective Agents; JL5DK93RCL / Melatonin; SY7Q814VUP / Calcium
  • [Keywords] NOTNLM ; Brain ischemia / Free radicals / Melatonin / Neuroprotection
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38. Plano D, Alcolea V, Sanmartín C, Sharma AK: Methods of selecting combination therapy for colorectal cancer patients: a patent evaluation of US20160025730A1. Expert Opin Ther Pat; 2017 May;27(5):527-538
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  • Targeted therapy drugs (TTDs) are a valid treatment, epithelial growth factor receptor (EGFR) inhibitors being one of the most commonly used for CRC patients.
  • Areas covered: The invention proposes the use of ErbB protein levels and ErbB receptor dimer formation as biomarkers for selecting, predicting and monitoring CRC patients showing sensitivity to the action of EGFR inhibitors to benefit from the combination therapy of EGFR and HER2 inhibitors.
  • Expert opinion: To assess the clinical applicability of this invention, further studies are needed since the conclusions are derived solely based on the data obtained from only one CRC cell line (Lim1215).
  • [MeSH-minor] Humans. Mitogen-Activated Protein Kinase Kinases / antagonists & inhibitors. Patents as Topic. Receptor, Epidermal Growth Factor / antagonists & inhibitors. Receptor, ErbB-2 / antagonists & inhibitors. Receptor, ErbB-3 / antagonists & inhibitors

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  • (PMID = 28366103.001).
  • [ISSN] 1744-7674
  • [Journal-full-title] Expert opinion on therapeutic patents
  • [ISO-abbreviation] Expert Opin Ther Pat
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] EC 2.7.10.1 / Receptor, Epidermal Growth Factor; EC 2.7.10.1 / Receptor, ErbB-2; EC 2.7.10.1 / Receptor, ErbB-3; EC 2.7.12.2 / Mitogen-Activated Protein Kinase Kinases
  • [Keywords] NOTNLM ; Biomarkers / EGFR inhibitors / colorectal cancer / combination therapy / monoclonal antibodies
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39. Pajaro-Castro N, Caballero-Gallardo K, Olivero-Verbel J: Toxicity of Naphthalene and Benzene on Tribollium castaneum Herbst. Int J Environ Res Public Health; 2017 Jun 21;14(6)

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Naphthalene and benzene are widely-used volatile organic compounds.
  • Real-time polymerase chain reaction (PCR) analysis revealed expression changes in genes related to oxidative stress and metabolism [Glutathione S-Transferase (Gst), and Cytochrome P450 6BQ8 (Cyp6bq8)]; reproduction and metamorphosis [Hormone receptor in 39-like protein (Hr39), Ecdysone receptor: (Ecr), and Chitin synthase 2 (Chs2)]; and neurotransmission [Histamine-gated chloride channel 2 (Hiscl2)] in insects exposed for 4 h to 70.2 µL/L naphthalene.
  • Adults exposed to benzene (80 µL/L; 4 h) overexpressed genes related to neurotransmission [GABA-gated anion channel (Rdl), Hiscl2, and GABA-gated ion channel (Grd)]; reproduction and metamorphosis [Ultraspiracle nuclear receptor (USP), Ecr; and Hr39]; and development (Chs2).

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  • (PMID = 28635673.001).
  • [ISSN] 1660-4601
  • [Journal-full-title] International journal of environmental research and public health
  • [ISO-abbreviation] Int J Environ Res Public Health
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Chemical-registry-number] 0 / Environmental Pollutants; 0 / Naphthalenes; 0 / Receptors, Cytoplasmic and Nuclear; 0 / Receptors, Steroid; 0 / ecdysone receptor; 2166IN72UN / naphthalene; EC 2.5.1.18 / Glutathione Transferase; J64922108F / Benzene
  • [Keywords] NOTNLM ; abnormalities / benzene / gene expression / mortality / naphthalene / naphthalin
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40. 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 04 01;25(7):2260-2265
ZFIN. ZFIN .

  • [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; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Carbohydrates; 0 / Enkephalins; 0 / Glycopeptides; 0 / Receptors, Opioid
  • [Keywords] NOTNLM ; Enkephalin-related (major topic) / Glycosylation (major topic) / Neoglycopeptides (major topic) / Neuropeptide (major topic) / Opioid receptors (major topic) / Pharmacology (major topic)
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41. Hirsch I, Janovec V, Stranska R, Bendriss-Vermare N: Cross Talk between Inhibitory Immunoreceptor Tyrosine-Based Activation Motif-Signaling and Toll-Like Receptor Pathways in Macrophages and Dendritic Cells. Front Immunol; 2017;8:394

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Cross Talk between Inhibitory Immunoreceptor Tyrosine-Based Activation Motif-Signaling and Toll-Like Receptor Pathways in Macrophages and Dendritic Cells.
  • Surprisingly, interference of ITAM-associated receptor signaling with TLR pathways has not been reported in conventional dendritic cells.

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  • (PMID = 28439271.001).
  • [ISSN] 1664-3224
  • [Journal-full-title] Frontiers in immunology
  • [ISO-abbreviation] Front Immunol
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; B cell receptor-like signaling / conventional dendritic cells / immunoreceptor tyrosine-based activation motif-associated receptor / macrophage / plasmacytoid dendritic cell / regulatory receptors / toll-like receptors
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42. Philippaert K, Pironet A, Mesuere M, Sones W, Vermeiren L, Kerselaers S, Pinto S, Segal A, Antoine N, Gysemans C, Laureys J, Lemaire K, Gilon P, Cuypers E, Tytgat J, Mathieu C, Schuit F, Rorsman P, Talavera K, Voets T, Vennekens R: Steviol glycosides enhance pancreatic beta-cell function and taste sensation by potentiation of TRPM5 channel activity. Nat Commun; 2017 Mar 31;8:14733

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Steviol glycosides enhance pancreatic beta-cell function and taste sensation by potentiation of TRPM5 channel activity.
  • Steviol glycosides (SGs), such as stevioside and rebaudioside A, are natural, non-caloric sweet-tasting organic molecules, present in extracts of the scrub plant Stevia rebaudiana, which are widely used as sweeteners in consumer foods and beverages.
  • TRPM5 is a Ca<sup>2+</sup>-activated cation channel expressed in type II taste receptor cells and pancreatic β-cells.

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  • (PMID = 28361903.001).
  • [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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43. Li S, Luo Z, Xu Y, Ren H, Deng L, Zhang X, Huang F, Yue T: Interaction pathways between soft lipid nanodiscs and plasma membranes: A molecular modeling study. Biochim Biophys Acta; 2017 10;1859(10):2096-2105

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Three typical interaction pathways, including the membrane attachment with lipid domain exchange of nanodiscs, the partial membrane wrapping with nanodisc vesiculation, and the receptor-mediated endocytosis, are discovered.
  • Finally, by setting both central normal lipids and boundary bola lipids as ligands, the receptor-mediated endocytosis occurs via both deformation and self-rotation of the nanodiscs.
  • [MeSH-major] Cell Membrane / metabolism. Lipid Bilayers / metabolism. Lipids / physiology

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28782501.001).
  • [ISSN] 0006-3002
  • [Journal-full-title] Biochimica et biophysica acta
  • [ISO-abbreviation] Biochim. Biophys. Acta
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Lipid Bilayers; 0 / Lipids; 0 / Membrane Proteins
  • [Keywords] NOTNLM ; Dissipative particle dynamics (major topic) / Drug delivery (major topic) / Lipid nanodisc (major topic) / Plasma membrane (major topic)
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44. Zhou XM, Wang D, He HL, Tang J, Wu J, Xu L, Li JX: Bone Marrow Derived Mesenchymal Stem Cells Involve in the Lymphangiogenesis of Lung Cancer and Jinfukang Inhibits the Involvement In Vivo. J Cancer; 2017;8(10):1786-1794

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Jinfukang has clinically been used for the treatment of non small cell lung cancer (NSCLC) in China.
  • Then, the chimeric mice were injected subcutaneously with freshly prepared Lewis lung carcinoma cell suspension to make lung tumor model, and the model mice were further orally administrated with Jinfukang once per day for 3 weeks.
  • Immunofluorescent analyses of lymphatic vessel endothelial hyaluronan receptor-1 (LYVE-1), a lymphatic endothelium marker, demonstrated a part of lymphatic endothelial cells in lung cancer were derived from BMMSCs, and those lymphatic endothelial cells contributed to the lung tumor lymphangiogenesis.

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  • (PMID = 28819375.001).
  • [ISSN] 1837-9664
  • [Journal-full-title] Journal of Cancer
  • [ISO-abbreviation] J Cancer
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Australia
  • [Keywords] NOTNLM ; Jinfukang / bone marrow-derived mesenchymal stem cells / chimeric mice / lung cancer / lymphangiogenesis
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45. Szychowski KA, Leja ML, Kaminskyy DV, Kryshchyshyn AP, Binduga UE, Pinyazhko OR, Lesyk RB, Tobiasz J, Gmiński J: Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma (PPARγ). Eur J Med Chem; 2017 Dec 01;141:162-168
NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Anticancer properties of 4-thiazolidinone derivatives depend on peroxisome proliferator-activated receptor gamma (PPARγ).
  • The aim of this study was to elucidate the involvement of PPARs in the mechanism of cytotoxic and pro-apoptotic action of novel anticancer 4-thiazolidinone derivatives (Les-2194, Les-3377, Les-3640) and approved 4-thiazolidinones (Rosiglitazone, Pioglitazone) towards the human squamous carcinoma (SCC-15) cell line.
  • Moreover, after PPARα, PPARβ and PPARγ siRNA gene silencing, cell viability, cell metabolism and caspase-3 activity were measured.
  • [MeSH-minor] Apoptosis / drug effects. Cell Line, Tumor. Cell Proliferation / drug effects. Dose-Response Relationship, Drug. Drug Screening Assays, Antitumor. Humans. Molecular Structure. RNA, Messenger / drug effects. RNA, Messenger / genetics. Structure-Activity Relationship

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  • [Copyright] Copyright © 2017 Elsevier Masson SAS. All rights reserved.
  • (PMID = 29031063.001).
  • [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 / 4-thiazolidinone; 0 / Antineoplastic Agents; 0 / PPAR gamma; 0 / RNA, Messenger; 0 / Thiazolidines
  • [Keywords] NOTNLM ; Cytotoxicity / PPARs / SCC-15 / Thiazolidinone / Thiazolothiopyranes
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46. Abraham L, Lu HY, Falcão RC, Scurll J, Jou T, Irwin B, Tafteh R, Gold MR, Coombs D: Limitations of Qdot labelling compared to directly-conjugated probes for single particle tracking of B cell receptor mobility. Sci Rep; 2017 Sep 12;7(1):11379

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Limitations of Qdot labelling compared to directly-conjugated probes for single particle tracking of B cell receptor mobility.
  • To test this, we labelled B cell receptors on the surface of B-lymphocytes with monovalent Fab fragments of antibodies that were either linked to Qdots via streptavidin or directly conjugated to the small organic fluorophore Cy3.
  • Imaging of receptor mobility by total internal reflection fluorescence microscopy (TIRFM), followed by quantitative single-molecule diffusion and confinement analysis, definitively showed that Qdots sterically hinder lateral mobility regardless of the substrate to which the cells were adhered.
  • Although we show that Qdot-labelled probes can detect large differences in receptor mobility, they fail to resolve subtle differences in lateral diffusion that are readily detectable using Cy3-labelled Fabs.

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  • (PMID = 28900238.001).
  • [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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47. Gourronc FA, Robertson LW, Klingelhutz AJ: A delayed proinflammatory response of human preadipocytes to PCB126 is dependent on the aryl hydrocarbon receptor. Environ Sci Pollut Res Int; 2017 Jul 11;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] A delayed proinflammatory response of human preadipocytes to PCB126 is dependent on the aryl hydrocarbon receptor.
  • Exposure to persistent organic pollutants such as polychlorinated biphenyls (PCBs) has been associated with the development of type II diabetes.
  • We show here that PCB126, a dioxin-like PCB, activates a robust proinflammatory state in fat cell precursors (preadipocytes).
  • The response was found to be dependent on aryl hydrocarbon receptor (AhR) activation, although induction of the response was delayed compared to upregulation of CYP1A1, a classic AhR-responsive gene.
  • Treatment of preadipocytes with a nuclear factor kappa-light-chain-enhancer of activated B cell (NF-κB) inhibitor partially attenuated the PCB126-induced inflammatory response and partly, but not completely, ameliorated disruption of adipogenesis caused by PCB126.

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  • (PMID = 28699004.001).
  • [ISSN] 1614-7499
  • [Journal-full-title] Environmental science and pollution research international
  • [ISO-abbreviation] Environ Sci Pollut Res Int
  • [Language] eng
  • [Grant] United States / NIEHS NIH HHS / ES / P30 ES005605; United States / NIEHS NIH HHS / ES / P42 ES013661
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; Adipocytes / AhR / Diabetes / Fat / Inflammation / PCB / Preadipocytes
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48. Iturrioz-Rodríguez N, González-Domínguez E, González-Lavado E, Marín-Caba L, Vaz B, Pérez-Lorenzo M, Correa-Duarte MA, Fanarraga ML: A Biomimetic Escape Strategy for Cytoplasm Invasion by Synthetic Particles. Angew Chem Int Ed Engl; 2017 Oct 23;56(44):13736-13740

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • After receptor-mediated endocytosis, most nanomaterials are sequestered and undergo degradation, therapy inactivation, or exocytosis.
  • Herein we explore a novel surface particle coating made of adsorbed carbon nanotubes that provides coated materials with new properties that reproduce the viral cell-invasive mechanisms, namely, receptor-mediated endocytosis, endolysosomal escape, and cytosolic particle release preserving cell viability.

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  • [Copyright] © 2017 Wiley-VCH Verlag GmbH & Co. KGaA, Weinheim.
  • (PMID = 28873280.001).
  • [ISSN] 1521-3773
  • [Journal-full-title] Angewandte Chemie (International ed. in English)
  • [ISO-abbreviation] Angew. Chem. Int. Ed. Engl.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; biomimetic coatings / carbon nanotubes / cell recognition / cytoplasmic invasion / endocytosis
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49. 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

  • [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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50. 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

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [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).
  • [ISSN] 1662-5102
  • [Journal-full-title] Frontiers in cellular neuroscience
  • [ISO-abbreviation] Front Cell Neurosci
  • [Language] eng
  • [Publication-type] Journal Article
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  • [Keywords] NOTNLM ; 1-AG / 2-AG / CB1 / calcium signaling / cannabinoid / modulation
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51. Rodrigues L, Espanca R, Costa AR, Antunes CM, Pomar C, Capela-Silva F, Pinheiro CC, Amado F, Lamy E: Association between Salivary Leptin Levels and Taste Perception in Children. J Nutr Metab; 2017;2017:7260169

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • The mode of action of salivary leptin at taste receptor level should be elucidated in future studies.

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  • (PMID = 28811937.001).
  • [ISSN] 2090-0724
  • [Journal-full-title] Journal of nutrition and metabolism
  • [ISO-abbreviation] J Nutr Metab
  • [Language] eng
  • [Publication-type] Journal Article
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52. 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

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [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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53. Irannejad R, Pessino V, Mika D, Huang B, Wedegaertner PB, Conti M, von Zastrow M: Functional selectivity of GPCR-directed drug action through location bias. Nat Chem Biol; 2017 Jul;13(7):799-806
Hazardous Substances Data Bank. EPINEPHRINE .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • We show here that the homologous human β<sub>1</sub>-adrenergic receptor initiates an internal G<sub>s</sub>-cAMP signal from the Golgi apparatus.
  • Golgi signaling utilizes a preexisting receptor pool rather than receptors delivered from the cell surface, requiring separate access of extracellular ligands.
  • Epinephrine, a hydrophilic endogenous ligand, accesses the Golgi-localized receptor pool by facilitated transport requiring the organic cation transporter 3 (OCT3), whereas drugs can access the Golgi pool by passive diffusion according to hydrophobicity.
  • We demonstrate marked differences, among both agonist and antagonist drugs, in Golgi-localized receptor access and show that β-blocker drugs currently used in the clinic differ markedly in ability to antagonize the Golgi signal.

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  • (PMID = 28553949.001).
  • [ISSN] 1552-4469
  • [Journal-full-title] Nature chemical biology
  • [ISO-abbreviation] Nat. Chem. Biol.
  • [Language] eng
  • [Grant] United States / NHLBI NIH HHS / HL / K99 HL122508; United States / NHLBI NIH HHS / HL / R00 HL122508; United States / NIBIB NIH HHS / EB / R21 EB022798
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Adrenergic beta-Antagonists; 0 / Ligands; 0 / Receptors, Adrenergic, beta-1; 3S12J47372 / Dobutamine; YKH834O4BH / Epinephrine
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54. Jia C, Zuo W, Yang D, Chen Y, Cao L, Custelcean R, Hostaš J, Hobza P, Glaser R, Wang YY, Yang XJ, Wu B: Selective binding of choline by a phosphate-coordination-based triple helicate featuring an aromatic box. Nat Commun; 2017 Oct 16;8(1):938

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Here, the authors design a biomimetic triple anion helicate receptor whose selectivity for choline arises from a similar binding mechanism.

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  • (PMID = 29038482.001).
  • [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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55. Dietrich S, Oleś M, Lu J, Sellner L, Anders S, Velten B, Wu B, Hüllein J, da Silva Liberio M, Walther T, Wagner L, Rabe S, Ghidelli-Disse S, Bantscheff M, Oleś AK, Słabicki M, Mock A, Oakes CC, Wang S, Oppermann S, Lukas M, Kim V, Sill M, Benner A, Jauch A, Sutton LA, Young E, Rosenquist R, Liu X, Jethwa A, Lee KS, Lewis J, Putzker K, Lutz C, Rossi D, Mokhir A, Oellerich T, Zirlik K, Herling M, Nguyen-Khac F, Plass C, Andersson E, Mustjoki S, von Kalle C, Ho AD, Hensel M, Dürig J, Ringshausen I, Zapatka M, Huber W, Zenz T: Drug-perturbation-based stratification of blood cancer. J Clin Invest; 2017 Dec 11;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • We assembled a primary blood cancer cell encyclopedia data set that revealed disease-specific sensitivities for each cancer.
  • Within chronic lymphocytic leukemia (CLL), responses to 62% of drugs were associated with 2 or more mutations, and linked the B cell receptor (BCR) pathway to trisomy 12, an important driver of CLL.

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  • (PMID = 29227286.001).
  • [ISSN] 1558-8238
  • [Journal-full-title] The Journal of clinical investigation
  • [ISO-abbreviation] J. Clin. Invest.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; B cell receptor / Drug screens / Hematology / Leukemias / Oncology
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56. 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 May;62(4)
Hazardous Substances Data Bank. MELATONIN .

  • [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 this 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.
  • [MeSH-minor] Blotting, Western. Caco-2 Cells. Cell Line. Chromatography, Liquid. Flow Cytometry. HeLa Cells. Humans. Membrane Potential, Mitochondrial / genetics. Membrane Potential, Mitochondrial / physiology. Reactive Oxygen Species / metabolism. Tandem Mass Spectrometry

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  • [Copyright] © 2017 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.
  • (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
  • [Chemical-registry-number] 0 / PepT1 protein; 0 / Reactive Oxygen Species; 0 / Symporters; 0 / hydrogen-coupled oligopeptide transporter PepT2; JL5DK93RCL / Melatonin
  • [Keywords] NOTNLM ; PEPT1/2 / apoptosis / cancer / melatonin / mitochondria / transporters
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57. Jouan E, Le Vée M, Denizot C, Parmentier Y, Fardel O: Drug Transporter Expression and Activity in Human Hepatoma HuH-7 Cells. Pharmaceutics; 2016 Dec 28;9(1)
NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • By contrast, they failed to display functional activities of the uptake transporters sodium taurocholate co-transporting polypeptide (NTCP), organic anion-transporting polypeptides (OATPs) and organic cation transporter 1 (OCT1), and of the canalicular transporters P-glycoprotein and breast cancer resistance protein (BCRP).
  • Concomitantly, mRNA expressions of various sinusoidal and canalicular hepatic drug transporters were not detected (NTCP, OATP1B1, organic anion transporter 2 (OAT2), OCT1 and bile salt export pump) or were found to be lower (OATP1B3, OATP2B1, multidrug and toxin extrusion protein 1, BCRP and MRP3) in hepatoma HuH-7 cells than those found in human hepatocytes, whereas other transporters such as OAT7, MRP4 and MRP5 were up-regulated.
  • HuH-7 cells additionally exhibited farnesoid X receptor (FXR)- and nuclear factor erythroid 2-related factor 2 (Nrf2)-related up-regulation of some transporters.

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  • (PMID = 28036031.001).
  • [Journal-full-title] Pharmaceutics
  • [ISO-abbreviation] Pharmaceutics
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; HuH-7 / MRP2 / drug transporters / hepatocytes / hepatoma
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58. Szybinski M, Sektas K, Sicinski RR, Plum LA, Frelek J, DeLuca HF: Design, synthesis and biological properties of seco-d-ring modified 1α,25-dihydroxyvitamin D&lt;sub&gt;3&lt;/sub&gt; analogues. J Steroid Biochem Mol Biol; 2017 07;171:144-154
Hazardous Substances Data Bank. 1,25-DIHYDROXYCHOLECALCIFEROL .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [MeSH-minor] Animals. Binding Sites. Bone Density Conservation Agents / chemistry. Bone Density Conservation Agents / metabolism. Bone Density Conservation Agents / pharmacology. Bone Density Conservation Agents / therapeutic use. Cell Differentiation / drug effects. Gastrointestinal Agents / chemistry. Gastrointestinal Agents / metabolism. Gastrointestinal Agents / pharmacology. Gastrointestinal Agents / therapeutic use. Genes, Reporter / drug effects. HL-60 Cells. Humans. Ligands. Male. Molecular Conformation. Molecular Docking Simulation. Rats, Sprague-Dawley. Recombinant Proteins / chemistry. Recombinant Proteins / metabolism. Stereoisomerism. Structure-Activity Relationship. Vitamin D3 24-Hydroxylase / chemistry. Vitamin D3 24-Hydroxylase / genetics. Vitamin D3 24-Hydroxylase / metabolism. Weaning

  • MedlinePlus Health Information. consumer health - Vitamin D Deficiency.
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  • [Copyright] Copyright © 2017 Elsevier Ltd. All rights reserved.
  • (PMID = 28285018.001).
  • [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; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Bone Density Conservation Agents; 0 / Gastrointestinal Agents; 0 / Ligands; 0 / Receptors, Calcitriol; 0 / Recombinant Proteins; EC 1.14.15.16 / Vitamin D3 24-Hydroxylase; FXC9231JVH / Calcitriol
  • [Keywords] NOTNLM ; 19-Norvitamin D (major topic) / Cellular differentiation (major topic) / D-seco vitamin D (major topic) / Secosteroids (major topic) / Transcriptional activity (major topic) / Vitamin D analogues (major topic) / Vitamin D receptor (major topic)
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59. 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

  • [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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60. Gobbo F, Bonsignore F, Amodeo R, Cattaneo A, Marchetti L: Site-Specific Direct Labeling of Neurotrophins and Their Receptors: From Biochemistry to Advanced Imaging Applications. Methods Mol Biol; 2018;1727:295-314

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • We describe here a versatile methodological platform to achieve site-directed and stoichiometry-controlled labeling of neurotrophins and their receptors with various probes, ranging from biotin to small organic dyes.
  • This labeling method works in vitro on purified neurotrophins as well as in a living cell context, where it achieves selective labeling of surface-exposed neurotrophin receptors.

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  • (PMID = 29222790.001).
  • [ISSN] 1940-6029
  • [Journal-full-title] Methods in molecular biology (Clifton, N.J.)
  • [ISO-abbreviation] Methods Mol. Biol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Astrocyte culture / Axonal transport / Biotinylation / Fluorescence labeling / Inducible lentivirus / Membrane receptor pool / Nerve growth factor / Neuron culture / Neurotrophin / TrkA tyrosine kinase
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61. García-Jiménez MJ, Gil-Caballero S, Canales Á, Jiménez-Barbero J, de Paz JL, Nieto PM: Interactions between a Heparin Trisaccharide Library and FGF-1 Analyzed by NMR Methods. Int J Mol Sci; 2017 Jun 17;18(6)

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • FGF-1 is a potent mitogen that, by interacting simultaneously with Heparan Sulfate Glycosaminoglycan HSGAG and the extracellular domains of its membrane receptor (FGFR), generates an intracellular signal that finally leads to cell division.

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  • (PMID = 28629128.001).
  • [ISSN] 1422-0067
  • [Journal-full-title] International journal of molecular sciences
  • [ISO-abbreviation] Int J Mol Sci
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; FGF-1 / NMR / STD-NMR / transient complexes
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62. 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
NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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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63. De Falco G, Colarusso C, Terlizzi M, Popolo A, Pecoraro M, Commodo M, Minutolo P, Sirignano M, D'Anna A, Aquino RP, Pinto A, Molino A, Sorrentino R: Chronic Obstructive Pulmonary Disease-Derived Circulating Cells Release IL-18 and IL-33 under Ultrafine Particulate Matter Exposure in a Caspase-1/8-Independent Manner. Front Immunol; 2017;8:1415
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  • (1) sub-10 nm particles, named nano organic carbon (NOC) particles and (2) primarily soot particles of 20-40 nm and their agglomerates (200 nm).
  • It was interesting that IL-18 and IL-33 release from PBMCs of unstable COPD patients was not NOD-like receptor 3/caspase-1 or caspase-8-dependent, but rather correlated to caspase-4 release.

  • NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .
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  • [Keywords] NOTNLM ; airway disease / chronic obstructive pulmonary disease / combustion-generated ultrafine particles / inflammation / peripheral blood mononuclear cells
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64. Guzik K, Magiera K, Musielak B, Pachota M, Szelazek B, Kocik J, Grudnik P, Tomala M, Krzanik S, Pyrc K, Dömling A, Dubin G, Holak TA: Small-molecule inhibitors of PD-1/PD-L1 immune checkpoint alleviate the PD-L1-induced exhaustion of T-cells. Oncotarget; 2017 Sep 22;8(42):72167-72181

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • The compounds present low toxicity towards tested cell lines and block the interaction of soluble PD-L1 with the cell surface-expressed PD-1.
  • As a result, BMS-1001 and BMS-1166 alleviate the inhibitory effect of the soluble PD-L1 on the T-cell receptor-mediated activation of T-lymphocytes.
  • Moreover, the compounds were effective in attenuating the inhibitory effect of the cell surface-associated PD-L1.

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  • (PMID = 29069777.001).
  • [ISSN] 1949-2553
  • [Journal-full-title] Oncotarget
  • [ISO-abbreviation] Oncotarget
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; PD-1 / PD-L1 / immune checkpoint blockade / inhibitor / small-molecules
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65. Mendes FB, Bergamin LS, Dos Santos Stuepp C, Braganhol E, Terroso T, Pohlmann AR, Guterres SS, Battastini AM: Alpha-bisabolol Promotes Glioma Cell Death by Modulating the Adenosinergic System. Anticancer Res; 2017 04;37(4):1819-1823
Genetic Alliance. consumer health - Glioma.

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Alpha-bisabolol Promotes Glioma Cell Death by Modulating the Adenosinergic System.
  • Alpha-bisabolol is an essential oil reported as a potent cell death agent.
  • Pre-treatment with an A<sub>3</sub> antagonist reverted the effect of α-bisabolol with an increase of mRNA expression of this receptor.
  • CONCLUSION: Our data indicated the participation of ecto-5'-nucleotidase/CD73 and A<sub>3</sub> receptor in the anti-proliferative effect of α-bisabolol on glioma cells.
  • [MeSH-major] 5'-Nucleotidase / metabolism. Cell Survival / drug effects. Glioma / pathology. Receptor, Adenosine A3 / chemistry. Sesquiterpenes / pharmacology
  • [MeSH-minor] Animals. Blotting, Western. Cell Proliferation / drug effects. Humans. RNA, Messenger / genetics. Rats. Real-Time Polymerase Chain Reaction. Reverse Transcriptase Polymerase Chain Reaction. Tumor Cells, Cultured

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  • [Copyright] Copyright© 2017, International Institute of Anticancer Research (Dr. George J. Delinasios), All rights reserved.
  • (PMID = 28373446.001).
  • [ISSN] 1791-7530
  • [Journal-full-title] Anticancer research
  • [ISO-abbreviation] Anticancer Res.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Greece
  • [Chemical-registry-number] 0 / RNA, Messenger; 0 / Receptor, Adenosine A3; 0 / Sesquiterpenes; 24WE03BX2T / bisabolol; EC 3.1.3.5 / 5'-Nucleotidase
  • [Keywords] NOTNLM ; Glioma (major topic) / adenosine (major topic) / ecto-5’-NT/CD73 (major topic) / α-bisabolol (major topic)
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66. Appelman MD, Chakraborty A, Protzer U, McKeating JA, van de Graaf SF: N-Glycosylation of the Na+-Taurocholate Cotransporting Polypeptide (NTCP) Determines Its Trafficking and Stability and Is Required for Hepatitis B Virus Infection. PLoS One; 2017;12(1):e0170419
MedlinePlus Health Information. consumer health - Hepatitis B.

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  • The sodium/bile acid cotransporter NTCP was recently identified as a receptor for hepatitis B virus (HBV).
  • NTCP is glycosylated and the role of glycans in protein trafficking or viral receptor activity is not known.
  • [MeSH-major] Hepatitis B / metabolism. Organic Anion Transporters, Sodium-Dependent / metabolism. Symporters / metabolism

  • Genetic Alliance. consumer health - Hepatitis.
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  • (PMID = 28125599.001).
  • [ISSN] 1932-6203
  • [Journal-full-title] PloS one
  • [ISO-abbreviation] PLoS ONE
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Organic Anion Transporters, Sodium-Dependent; 0 / Symporters; 145420-23-1 / sodium-bile acid cotransporter
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67. Gomes de Castro MA, Höbartner C, Opazo F: Aptamers provide superior stainings of cellular receptors studied under super-resolution microscopy. PLoS One; 2017;12(2):e0173050
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  • [MeSH-major] Aptamers, Nucleotide / chemistry. Receptor, EphA2 / metabolism. Receptor, Epidermal Growth Factor / metabolism. Receptor, ErbB-2 / metabolism

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  • NCI CPTAC Assay Portal. NCI CPTAC Assay Portal .
  • NCI CPTAC Assay Portal. NCI CPTAC Assay Portal .
  • NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .
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  • (PMID = 28235049.001).
  • [ISSN] 1932-6203
  • [Journal-full-title] PloS one
  • [ISO-abbreviation] PLoS ONE
  • [Language] eng
  • [Publication-type] Comparative Study; Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Antibodies; 0 / Aptamers, Nucleotide; 0 / Epitopes; EC 2.7.10.1 / EGFR protein, human; EC 2.7.10.1 / ERBB2 protein, human; EC 2.7.10.1 / Receptor, EphA2; EC 2.7.10.1 / Receptor, Epidermal Growth Factor; EC 2.7.10.1 / Receptor, ErbB-2
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68. Johnson N, Březinová J, Stephens E, Burbridge E, Freeman M, Adrain C, Strisovsky K: Quantitative proteomics screen identifies a substrate repertoire of rhomboid protease RHBDL2 in human cells and implicates it in epithelial homeostasis. Sci Rep; 2017 Aug 04;7(1):7283
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  • They regulate epidermal growth factor receptor signalling in Drosophila by releasing signalling ligands from their transmembrane tethers.
  • We reveal a range of novel substrates that are specifically cleaved by RHBDL2, including the interleukin-6 receptor (IL6R), cell surface protease inhibitor Spint-1, the collagen receptor tyrosine kinase DDR1, N-Cadherin, CLCP1/DCBLD2, KIRREL, BCAM and others.
  • We further demonstrate that these substrates can be shed by endogenously expressed RHBDL2 and that a subset of them is resistant to shedding by cell surface metalloproteases.


69. Martínez R, de Villavicencio-Díaz TN, Sánchez A, Ramos Y, Ferro JN, González LG, Méndez M, Rodríguez E, Marcos E, Sánchez B, Masforrol Y, Garay H, Albericio F, Hermida L, González LJ, Vonasek E, Estrada MP, Besada V: Comparative proteomic analysis of growth hormone secretagogue A233 treatment of murine macrophage cells J774A.2 indicates it has a role in antiviral innate response. Biochem Biophys Rep; 2016 Mar;5:379-387
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  • [Title] Comparative proteomic analysis of growth hormone secretagogue A233 treatment of murine macrophage cells J774A.2 indicates it has a role in antiviral innate response.
  • BACKGROUND: Growth hormone secretagogues (GHS), among other factors, regulate the release of GH.
  • The biological activity of the secretagogue peptide A233 as a promoter of growth and innate immunity in teleost fish has previously been demonstrated, but its role in the immune system of mammals is not well understood.
  • METHODS: The effect of the peptide was investigated in J774A.2 macrophage cells using a comparative proteomics approach after 6 and 12 h of peptide stimulation.
  • RESULTS: The functional analysis of differentially modulated proteins showed that A233 peptide treatment appears to promote activation and ROS-dependent cytotoxic functions in macrophages and enhanced expression of antiviral protein complexes such as MAvs. In accordance with this hypothesis, we found that A233 treatment enhanced superoxide anion production and the IFN-γ level in J774A.2 cells and mouse splenocytes, respectively, and reduced viral load in a dengue virus mouse model of infection.
  • CONCLUSIONS: The growth hormone secretagogue A233 peptide promotes activation of ROS-dependent cytotoxic functions and exerts immunomodulatory effects that enable an antiviral state in a dengue virus mouse model.
  • GENERAL SIGNIFICANCE: The increase of IFN-γ level and the differential modulation of antiviral proteins by the A233 peptide suggest that the molecule could activate an innate immune response with a possible further impact in the treatment of acute and chronic diseases.

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  • (PMID = 28955845.001).
  • [ISSN] 2405-5808
  • [Journal-full-title] Biochemistry and biophysics reports
  • [ISO-abbreviation] Biochem Biophys Rep
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Antiviral activity / Comparative proteomics / DENV, dengue virus / GHRP-6, growth hormone releasing peptide-6 / GHS, growth hormone secretagogue / Growth Hormone Secretagogue / IFN-γ, interferon gamma / LPS, lipopolysaccharide / O2•−, superoxide anion / RNS, reactive nitrogen species / ROS production / ROS, reactive oxygen species / [d-Lys3]-GHRP-6t, ghrelin receptor antagonist
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70. Alvarado A, Gil da Costa RM, Faustino-Rocha AI, Ferreira R, Lopes C, Oliveira PA, Colaço B: Effects of exercise training on breast cancer metastasis in a rat model. Int J Exp Pathol; 2017 02;98(1):40-46
MedlinePlus Health Information. consumer health - Breast Cancer.

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [MeSH-major] Breast Neoplasms / pathology. Estrogen Receptor alpha / metabolism. Estrogens / metabolism. Physical Conditioning, Animal

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  • [Copyright] © 2017 The Authors. International Journal of Experimental Pathology © 2017 International Journal of Experimental Pathology.
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  • (PMID = 28556395.001).
  • [ISSN] 1365-2613
  • [Journal-full-title] International journal of experimental pathology
  • [ISO-abbreviation] Int J Exp Pathol
  • [Language] eng
  • [Publication-type] Journal Article; Research Support, Non-U.S. Gov't
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Estrogen Receptor alpha; 0 / Estrogens
  • [Keywords] NOTNLM ; chemical carcinogenesis (major topic) / mammary tumours (major topic) / oestrogen receptor α (major topic) / progesterone receptor (major topic) / treadmill (major topic) / vascularization (major topic)
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71. Abdelazeem AH, El-Saadi MT, Said EG, Youssif BGM, Omar HA, El-Moghazy SM: Novel diphenylthiazole derivatives with multi-target mechanism: Synthesis, docking study, anticancer and anti-inflammatory activities. Bioorg Chem; 2017 12;75:127-138
NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • In this regard, a novel series of compounds bearing a COXs privilege scaffold, diphenyl thiazole, was synthesized and evaluated for their anticancer activity against a panel of cancer cell lines.
  • [MeSH-minor] A549 Cells. Animals. Binding Sites. Cell Survival / drug effects. Cyclooxygenase 1 / chemistry. Cyclooxygenase 1 / metabolism. Cyclooxygenase 2 / chemistry. Cyclooxygenase 2 / metabolism. Cyclooxygenase 2 Inhibitors / chemical synthesis. Cyclooxygenase 2 Inhibitors / chemistry. Cyclooxygenase 2 Inhibitors / metabolism. Edema / chemically induced. Edema / drug therapy. Edema / pathology. HT29 Cells. Humans. Inhibitory Concentration 50. MCF-7 Cells. Molecular Docking Simulation. Protein Structure, Tertiary. Proto-Oncogene Proteins B-raf / antagonists & inhibitors. Proto-Oncogene Proteins B-raf / metabolism. Rats. Receptor, Epidermal Growth Factor / antagonists & inhibitors. Receptor, Epidermal Growth Factor / metabolism. Tubulin / chemistry. Tubulin / metabolism

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  • NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .
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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
  • (PMID = 28938224.001).
  • [ISSN] 1090-2120
  • [Journal-full-title] Bioorganic chemistry
  • [ISO-abbreviation] Bioorg. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Anti-Inflammatory Agents; 0 / Antineoplastic Agents; 0 / Cyclooxygenase 2 Inhibitors; 0 / Thiazoles; 0 / Tubulin; EC 1.14.99.1 / Cyclooxygenase 1; EC 1.14.99.1 / Cyclooxygenase 2; EC 2.7.10.1 / Receptor, Epidermal Growth Factor; EC 2.7.11.1 / Proto-Oncogene Proteins B-raf
  • [Keywords] NOTNLM ; Anti-inflammatory (major topic) / Anticancer (major topic) / BRAF (major topic) / COX-2 (major topic) / Diphenylthiazole (major topic) / EGFR (major topic)
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72. 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 29;139(12):4513-4520

  • [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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73. Zackova Suchanova J, Neburkova J, Spanielova H, Forstova J, Cigler P: Retargeting Polyomavirus-Like Particles to Cancer Cells by Chemical Modification of Capsid Surface. Bioconjug Chem; 2017 Feb 15;28(2):307-313
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  • Here, we describe a chemical approach to retarget PVLPs to cancer cells displaying abnormally high levels of transferrin receptor.
  • [MeSH-minor] Biological Transport. Cell Line, Tumor. Humans. Models, Molecular. Molecular Conformation. Surface Properties

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  • (PMID = 28035816.001).
  • [ISSN] 1520-4812
  • [Journal-full-title] Bioconjugate chemistry
  • [ISO-abbreviation] Bioconjug. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Drug Carriers
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74. 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 01 11;139(1):218-230
MedlinePlus Health Information. consumer health - Botox.

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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.
  • [MeSH-major] Botulinum Toxins, Type A / chemistry. Polysaccharides / chemistry. Receptors, Cell Surface / chemistry

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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; Research Support, Non-U.S. Gov't
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Ligands; 0 / Polysaccharides; 0 / Receptors, Cell Surface; 0 / ganglioside receptor; EC 3.4.24.69 / Botulinum Toxins, Type A
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75. Minamiki T, Sasaki Y, Tokito S, Minami T: Label-Free Direct Electrical Detection of a Histidine-Rich Protein with Sub-Femtomolar Sensitivity using an Organic Field-Effect Transistor. ChemistryOpen; 2017 Aug;6(4):472-475

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Label-Free Direct Electrical Detection of a Histidine-Rich Protein with Sub-Femtomolar Sensitivity using an Organic Field-Effect Transistor.
  • Herein, a new strategy for highly sensitive protein detection at sub-femtomolar levels without any labelling has been demonstrated by using an organic field-effect transistor (OFET).
  • An artificial histidine-rich protein receptor (Ni<sup>II</sup>-nitrilotriacetic acid complex, Ni<sup>II</sup>-nta) functionalizes a detection portion (i.e. an extended-gate electrode) of the fabricated OFET device.
  • Our results demonstrate that the combination of the OFET with the artificial receptor is an ideal approach for label-free and immune-free protein detection.

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  • (PMID = 28794937.001).
  • [ISSN] 2191-1363
  • [Journal-full-title] ChemistryOpen
  • [ISO-abbreviation] ChemistryOpen
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; molecular recognition / organic transistors / self-assembled monolayers / sensors / serum albumin
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76. Guzik K, Zak KM, Grudnik P, Magiera K, Musielak B, Törner R, Skalniak L, Dömling A, Dubin G, Holak TA: Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1. J Med Chem; 2017 Jul 13;60(13):5857-5867

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Small-Molecule Inhibitors of the Programmed Cell Death-1/Programmed Death-Ligand 1 (PD-1/PD-L1) Interaction via Transiently Induced Protein States and Dimerization of PD-L1.
  • [MeSH-major] Antigens, CD274 / antagonists & inhibitors. Programmed Cell Death 1 Receptor / antagonists & inhibitors. Protein Interaction Maps / drug effects. Protein Multimerization / drug effects. Small Molecule Libraries / chemistry. Small Molecule Libraries / pharmacology

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  • (PMID = 28613862.001).
  • [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
  • [Chemical-registry-number] 0 / Antigens, CD274; 0 / Programmed Cell Death 1 Receptor; 0 / Small Molecule Libraries
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77. 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

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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).
  • [ISSN] 1662-5102
  • [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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78. He L, Brasino M, Mao C, Cho S, Park W, Goodwin AP, Cha JN: DNA-Assembled Core-Satellite Upconverting-Metal-Organic Framework Nanoparticle Superstructures for Efficient Photodynamic Therapy. Small; 2017 Jun;13(24)
NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] DNA-Assembled Core-Satellite Upconverting-Metal-Organic Framework Nanoparticle Superstructures for Efficient Photodynamic Therapy.
  • DNA-mediated assembly of core-satellite structures composed of Zr(IV)-based porphyrinic metal-organic framework (MOF) and NaYF<sub>4</sub> ,Yb,Er upconverting nanoparticles (UCNPs) for photodynamic therapy (PDT) is reported.
  • The MOF-UCNP core-satellite superstructures also induce strong cell cytotoxicity against cancer cells, which are further enhanced by attaching epidermal growth factor receptor targeting affibodies to the PDT clusters, highlighting their promise as theranostic photodynamic agents.

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  • [Copyright] © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
  • (PMID = 28481463.001).
  • [ISSN] 1613-6829
  • [Journal-full-title] Small (Weinheim an der Bergstrasse, Germany)
  • [ISO-abbreviation] Small
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; DNA self-assembly / core-satellite / metal-organic frameworks / photodynamic therapy / upconverting nanoparticles
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79. Jin L, Wang W, Degroote J, Van Noten N, Yan H, Majdeddin M, Van Poucke M, Peelman L, Goderis A, Van De Mierop K, Mombaerts R, De Smet S, Michiels J: Mycotoxin binder improves growth rate in piglets associated with reduction of toll-like receptor-4 and increase of tight junction protein gene expression in gut mucosa. J Anim Sci Biotechnol; 2017;8:80

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Mycotoxin binder improves growth rate in piglets associated with reduction of toll-like receptor-4 and increase of tight junction protein gene expression in gut mucosa.
  • Method: The effect of a mycotoxin binder (containing acid-activated bentonite, clinoptilolite, yeast cell walls and organic acids) on growth performance and gut health was studied.
  • On d14, one pig from each pen was euthanized and distal small intestinal mucosa samples were collected for the assessment of intestinal permeability, and gene expression of tight junction proteins, toll-like receptor 4, inflammatory cytokines and intestinal alkaline phosphatase.
  • Groups with binder in the diet also exhibited lower expression of toll-like receptor 4 in distal small intestinal mucosa at d14, compared to groups without binder (<i>P</i> ≤ 0.05).
  • Addition of binder to DON contaminated diets, also down-regulated the gene expression of toll-like receptor 4 (<i>P</i> ≤ 0.05) and increased mRNA level zona occludens 1 (<i>P</i> ≤ 0.10) as compared to DON.
  • Conclusions: The present data provide evidence that the binder improves growth rate in piglets associated with reduction of toll-like receptor-4 and increase of tight junction protein gene expression.

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  • (PMID = 29118977.001).
  • [ISSN] 1674-9782
  • [Journal-full-title] Journal of animal science and biotechnology
  • [ISO-abbreviation] J Anim Sci Biotechnol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; Binder / Deoxynivalenol / Gut barrier / Gut health / Mycotoxin / Pigs
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80. Qin HL, Leng J, Youssif BGM, Amjad MW, Raja MAG, Hussain MA, Hussain Z, Kazmi SN, Bukhari SNA: Synthesis and mechanistic studies of curcumin analog-based oximes as potential anticancer agents. Chem Biol Drug Des; 2017 Sep;90(3):443-449
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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.
  • [MeSH-minor] Antineoplastic Agents / chemical synthesis. Antineoplastic Agents / chemistry. Antineoplastic Agents / pharmacology. Cell Line, Tumor. Cell Proliferation / drug effects. Cell Survival / drug effects. Humans. Proto-Oncogene Proteins B-raf / antagonists & inhibitors. Proto-Oncogene Proteins B-raf / genetics. Proto-Oncogene Proteins B-raf / metabolism. Receptor, Epidermal Growth Factor / antagonists & inhibitors. Receptor, Epidermal Growth Factor / metabolism. Structure-Activity Relationship. Tubulin / chemistry. Tubulin / metabolism. Tubulin Modulators / chemical synthesis. Tubulin Modulators / pharmacology

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  • [Copyright] © 2017 John Wiley & Sons A/S.
  • (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
  • [Chemical-registry-number] 0 / Antineoplastic Agents; 0 / Oximes; 0 / Tubulin; 0 / Tubulin Modulators; EC 2.7.10.1 / Receptor, Epidermal Growth Factor; EC 2.7.11.1 / Proto-Oncogene Proteins B-raf; IT942ZTH98 / Curcumin
  • [Keywords] NOTNLM ; Natural compounds / epidermal growth factor receptor (EGFR) / multidrug resistance (MDR) / tubulin polymerization / α, β-unsaturated carbonyl
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81. Bello AR, Puertas-Avendaño RA, González-Gómez MJ, González-Gómez M, Laborda J, Damas C, Ruiz-Hidalgo M, Diaz C: Delta-like protein 1 in the pituitary-adipose axis in the adult male mouse. J Neuroendocrinol; 2017 Aug;29(8)
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  • The results obtained showed that, in WT adipose cells, all of the adenohypophyseal hormone receptors were present, with a higher mRNA expression for growth hormone (GH) receptor and thyroid-stimulating hormone (TSH) receptor.
  • Of the total cells in the anterior pituitary lobe, 17.09±0.9% were leptin receptor (LEPR) immunoreactive (-IR), mainly in GH-IR and prolactin (PRL)-IR cells (41.5±3.8%; 13.5±1.7%, respectively).
  • In Dlk1<sup>-/-</sup> mice, adipocyte cells showed a significant increase in the TSH receptor mRNA expression level.

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  • [Copyright] © 2017 British Society for Neuroendocrinology.
  • (PMID = 28718206.001).
  • [ISSN] 1365-2826
  • [Journal-full-title] Journal of neuroendocrinology
  • [ISO-abbreviation] J. Neuroendocrinol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; anterior pituitary / hormone receptors / leptin / leptin receptor
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82. Haruta M, Sussman MR: Ligand Receptor-Mediated Regulation of Growth in Plants. Curr Top Dev Biol; 2017;123:331-363
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [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.
  • [MeSH-major] Plant Development. Plants / metabolism. Receptors, Cell Surface / metabolism

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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; Review
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Ligands; 0 / Plant Growth Regulators; 0 / Receptors, Cell Surface
  • [Keywords] NOTNLM ; Arabidopsis (major topic) / Cell expansion (major topic) / Peptide hormone (major topic) / Phosphorylation (major topic) / Protein kinase (major topic) / Receptor-like kinase (major topic)
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83. 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

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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.
  • [MeSH-major] Antipsychotic Agents / metabolism. Brain / metabolism. Chlorpromazine / metabolism. Clozapine / metabolism. Receptor, Muscarinic M1 / metabolism. Receptor, Muscarinic M3 / metabolism. Receptor, Serotonin, 5-HT2A / metabolism. Receptor, Serotonin, 5-HT2C / metabolism. Receptors, Dopamine D4 / metabolism

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  • (PMID = 28221369.001).
  • [ISSN] 2158-3188
  • [Journal-full-title] Translational psychiatry
  • [ISO-abbreviation] Transl Psychiatry
  • [Language] eng
  • [Grant] United States / NLM NIH HHS / LM / RC2 LM010994
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Antipsychotic Agents; 0 / CHRM1 protein, human; 0 / CHRM3 protein, human; 0 / DRD4 protein, human; 0 / Receptor, Muscarinic M1; 0 / Receptor, Muscarinic M3; 0 / Receptor, Serotonin, 5-HT2A; 0 / Receptor, Serotonin, 5-HT2C; 137750-34-6 / Receptors, Dopamine D4; J60AR2IKIC / Clozapine; U42B7VYA4P / Chlorpromazine
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84. Denisov EV, Skryabin NA, Gerashchenko TS, Tashireva LA, Wilhelm J, Buldakov MA, Sleptcov AA, Lebedev IN, Vtorushin SV, Zavyalova MV, Cherdyntseva NV, Perelmuter VM: Clinically relevant morphological structures in breast cancer represent transcriptionally distinct tumor cell populations with varied degrees of epithelial-mesenchymal transition and CD44+CD24- stemness. Oncotarget; 2017 May 19;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Clinically relevant morphological structures in breast cancer represent transcriptionally distinct tumor cell populations with varied degrees of epithelial-mesenchymal transition and CD44+CD24- stemness.
  • By contrast, morphological structures were characterized by specific gene expression profiles and signaling pathways and significantly differed in progesterone receptor and Ki-67 expression.
  • Solid (large shapeless) structures retained epithelial features but demonstrated an increase in mesenchymal traits and collective cell migration hallmarks.

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  • (PMID = 28591736.001).
  • [ISSN] 1949-2553
  • [Journal-full-title] Oncotarget
  • [ISO-abbreviation] Oncotarget
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; breast cancer / cancer invasion / cancer stem cell / epithelial-mesenchymal transition / tumor heterogeneity
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85. Bigliardi PL, Rout B, Pant A, Krishnan-Kutty V, Eberle AN, Srinivas R, Burkett BA, Bigliardi-Qi M: Specific Targeting of Melanotic Cells with Peptide Ligated Photosensitizers for Photodynamic Therapy. Sci Rep; 2017 Nov 16;7(1):15750

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • A strategy combining covalent conjugation of photosensitizers to a peptide ligand directed to the melanocortin 1 (MC1) receptor with the application of sequential LED light dosage at near-IR wavelengths was developed to achieve specific cytotoxicity to melanocytes and melanoma (MEL) with minimal collateral damage to surrounding cells such as keratinocytes (KER).

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  • (PMID = 29146972.001).
  • [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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86. Mahalingam SM, Dudkin VY, Goldberg S, Klein D, Yi F, Singhal S, O'Neil KT, Low PS: Evaluation of a Centyrin-Based Near-Infrared Probe for Fluorescence-Guided Surgery of Epidermal Growth Factor Receptor Positive Tumors. Bioconjug Chem; 2017 Nov 15;28(11):2865-2873
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Evaluation of a Centyrin-Based Near-Infrared Probe for Fluorescence-Guided Surgery of Epidermal Growth Factor Receptor Positive Tumors.
  • Although the tumor-targeted fluorescent dyes used in humans to date have been either small organic molecules or high molecular weight antibodies, low molecular weight protein scaffolds have attracted significant attention because they penetrate solid tumors almost as efficiently as small molecules, but can be infinitely mutated to bind almost any antigen.
  • Here we describe the use of a 10 kDa protein scaffold, a Centyrin, to target a near-infrared fluorescent dye to tumors that overexpress the epidermal growth factor receptor (EGFR) for fluorescence-guided surgery (FGS).
  • [MeSH-major] Fluorescent Dyes / chemistry. Neoplasms / diagnostic imaging. Neoplasms / surgery. Optical Imaging / methods. Receptor, Epidermal Growth Factor / analysis
  • [MeSH-minor] Animals. Cell Line, Tumor. Fluorescence. Humans. Infrared Rays. Mice. Mice, Nude. Models, Molecular. Proteins / chemistry. Proteins / metabolism

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  • (PMID = 28945346.001).
  • [ISSN] 1520-4812
  • [Journal-full-title] Bioconjugate chemistry
  • [ISO-abbreviation] Bioconjug. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Fluorescent Dyes; 0 / Proteins; EC 2.7.10.1 / Receptor, Epidermal Growth Factor
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87. Chubanov V, Ferioli S, Gudermann T: Assessment of TRPM7 functions by drug-like small molecules. Cell Calcium; 2017 Nov;67:166-173

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Transient receptor potential cation channel subfamily M member 7 (TRPM7) is a plasma membrane ion channel linked to a cytosolic protein kinase domain.
  • Genetic inactivation of this bi-functional protein revealed its crucial role in Ca<sup>2+</sup> signalling, Mg<sup>2+</sup> metabolism, immune responses, cell motility, proliferation and differentiation.
  • Recently, several groups have identified small organic compounds acting as inhibitors or activators of the TRPM7 channel.

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  • [Copyright] Copyright © 2017 Elsevier Ltd. All rights reserved.
  • (PMID = 28356194.001).
  • [ISSN] 1532-1991
  • [Journal-full-title] Cell calcium
  • [ISO-abbreviation] Cell Calcium
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Calcium / Magnesium / TRP channel / TRPM6 / TRPM7 / α-kinase
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88. Yoon KB, Cho SY, An SJ, Park KR, Lee HJ, Yoon HS, Lee SM, Kim YC, Han SY: Characterization of the aminopyridine derivative KRC-180 as a JAK2 inhibitor. Oncol Lett; 2017 Aug;14(2):1347-1354
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  • Janus kinase 2 (JAK2) is a non-receptor tyrosine kinase that regulates the signal transducer and activator of transcription (STAT) signaling pathway.
  • The growth of HEL92.1.7 erythroleukemia cells harboring a constitutively activated form of JAK2 was suppressed by KRC-180 treatment; KRC-180 induced apoptotic cell death and cell cycle arrest.

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  • (PMID = 28789350.001).
  • [ISSN] 1792-1074
  • [Journal-full-title] Oncology letters
  • [ISO-abbreviation] Oncol Lett
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Greece
  • [Keywords] NOTNLM ; Janus kinase 2 / KRC-180 / leukemia / signal transducer and activator of transcription
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89. Mihajlovic M, Fedecostante M, Oost MJ, Steenhuis SKP, Lentjes EGWM, Maitimu-Smeele I, Janssen MJ, Hilbrands LB, Masereeuw R: Role of Vitamin D in Maintaining Renal Epithelial Barrier Function in Uremic Conditions. Int J Mol Sci; 2017 Nov 26;18(12)

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • The organic anion transporter 1 (OAT-1) overexpressing ciPTEC line presented 1α-hydroxylase (CYP27B1), 24-hydroxylase (CYP24A1) and vitamin D receptor (VDR), responsible for vitamin D activation, degradation and function, respectively.
  • The beneficial effect of vitamin D on cell function and behavior in uremic conditions was studied in the presence of an anionic uremic toxins mixture.
  • Vitamin D could restore cell viability, and inflammatory and oxidative status, as shown by cell metabolic activity, interleukin-6 (IL-6) levels and reactive oxygen species (ROS) production, respectively.

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  • (PMID = 29186865.001).
  • [ISSN] 1422-0067
  • [Journal-full-title] International journal of molecular sciences
  • [ISO-abbreviation] Int J Mol Sci
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; bioartificial kidney / chronic kidney disease / conditionally immortalized proximal tubule cells / end-stage renal disease / epithelial barrier / uremic toxins / vitamin D
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90. 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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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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.
  • [MeSH-minor] Animals. Cell Line, Tumor. Cell Proliferation / drug effects. Cell Shape / drug effects. Colloids. Humans. Molecular Weight. Neoplasm Invasiveness. Porosity. Rats. Solubility

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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
  • [Chemical-registry-number] 0 / Antigens, CD44; 0 / CD44 protein, human; 0 / Colloids; 9004-61-9 / Hyaluronic Acid; 9007-34-5 / Collagen
  • [Keywords] NOTNLM ; CD44 receptor / Collagen / Extracellular matrix / Hyaluronan / Melanoma cells
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91. 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

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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.
  • [MeSH-minor] Animals. Cell Proliferation / drug effects. Dose-Response Relationship, Drug. Drug Screening Assays, Antitumor. Female. HCT116 Cells. Humans. MCF-7 Cells. Mice. Models, Molecular. Molecular Structure. Neoplasms, Experimental / drug therapy. Neoplasms, Experimental / pathology. Receptors, Vascular Endothelial Growth Factor / antagonists & inhibitors. Receptors, Vascular Endothelial Growth Factor / metabolism. Structure-Activity Relationship

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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
  • [Chemical-registry-number] 0 / Antineoplastic Agents; 0 / Protein Kinase Inhibitors; 0 / Pyridazines; 449GLA0653 / pyridazine; EC 2.7.10.1 / Receptors, Vascular Endothelial Growth Factor
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92. Saulite L, Vavers E, Zvejniece L, Dambrova M, Riekstina U: The Differentiation of Skin Mesenchymal Stem Cells Towards a Schwann Cell Phenotype: Impact of Sigma-1 Receptor Activation. Mol Neurobiol; 2017 Apr 28;
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] The Differentiation of Skin Mesenchymal Stem Cells Towards a Schwann Cell Phenotype: Impact of Sigma-1 Receptor Activation.
  • Recently, it was shown that 2-3% of the human dermis mesenchymal stem cell (MSC) population expresses the NCSC marker CD271, thus enabling the use of skin MSCs for studying Schwann cell differentiation in vitro.
  • The aims of this study were to establish a protocol for human skin MSC differentiation towards Schwann cell-like cells (SC-lcs) and to analyse the expression of sigma-1 receptor (S1R) in SC-lcs.
  • The impact of S1R ligands, namely the selective agonist PRE-084, the positive allosteric modulator E1R and the selective antagonist NE-100, on Schwann cell differentiation was assessed.
  • The expression of the neuron-specific genes Tubulin-βIII and Integrin-6α, the Schwann cell-specific gene S100b, MBP and the NCSC-specific genes p75NTR, Sox10, Notch1, Integrin-4α, Ap2α and Pax6 was analysed in MSCs and SC-lcs by real-time RT-PCR.

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  • (PMID = 28455697.001).
  • [ISSN] 1559-1182
  • [Journal-full-title] Molecular neurobiology
  • [ISO-abbreviation] Mol. Neurobiol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; BDNF / MBP / Mesenchymal stem cells / Schwann cells / Sigma-1 receptor
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93. Wongwan T, Kittayaruksakul S, Asavapanumas N, Chatsudthipong V, Soodvilai S: Activation of liver X receptor inhibits OCT2-mediated organic cation transport in renal proximal tubular cells. Pflugers Arch; 2017 Jul 25;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Activation of liver X receptor inhibits OCT2-mediated organic cation transport in renal proximal tubular cells.
  • Liver X receptor (LXR) is transcriptional factor that plays an important role in the regulation of energy metabolism such as cholesterol, lipid, and glucose metabolism as well as membrane transporters and channels.
  • Using both in vitro and in vivo models, LXR regulation of the expression and function of renal organic cation transporter 2 (OCT2) was observed.
  • In addition, co-treatment with a retinoic X receptor (RXR) ligand, 9-cis retinoic acid enhanced the inhibitory effect of GW3965, indicating negative regulation of OCT2 transport activity by the LXR/RXR complex.

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  • (PMID = 28741179.001).
  • [ISSN] 1432-2013
  • [Journal-full-title] Pflugers Archiv : European journal of physiology
  • [ISO-abbreviation] Pflugers Arch.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; Kidney / Nuclear receptors / Proximal tubule / Regulation / Retinoic x receptor / Secretion
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94. Darbre PD: Endocrine Disruptors and Obesity. Curr Obes Rep; 2017 Mar;6(1):18-27
MedlinePlus Health Information. consumer health - Obesity.

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [MeSH-minor] Adipocytes / drug effects. Adipogenesis / drug effects. Animals. Appetite / drug effects. Female. Food Preferences. Health Status. Humans. Mice, Obese. Organic Chemicals / pharmacology. Organic Chemicals / toxicity. PPAR gamma / drug effects. Pregnancy. Prenatal Exposure Delayed Effects. Receptors, Aryl Hydrocarbon / drug effects. Receptors, Steroid / drug effects. Risk Assessment. Satiation / physiology

  • Genetic Alliance. consumer health - Obesity.
  • MedlinePlus Health Information. consumer health - Endocrine Diseases.
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  • (PMID = 28205155.001).
  • [ISSN] 2162-4968
  • [Journal-full-title] Current obesity reports
  • [ISO-abbreviation] Curr Obes Rep
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Endocrine Disruptors; 0 / Organic Chemicals; 0 / PPAR gamma; 0 / Receptors, Aryl Hydrocarbon; 0 / Receptors, Steroid
  • [Keywords] NOTNLM ; Adipogenesis / Bisphenol A / Diethylstilbestrol / Endocrine disruptor / Endocrine-disrupting chemicals / Obesity / Obesogen / Paraben / Peroxisome proliferator-activated receptor / Persistent organic pollutants / Tributyltin
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95. Özek G, Schepetkin IA, Utegenova GA, Kirpotina LN, Andrei SR, Özek T, Başer KHC, Abidkulova KT, Kushnarenko SV, Khlebnikov AI, Damron DS, Quinn MT: Chemical composition and phagocyte immunomodulatory activity of &lt;i&gt;Ferula iliensis&lt;/i&gt; essential oils. J Leukoc Biol; 2017 06;101(6):1361-1371
Hazardous Substances Data Bank. CALCIUM, ELEMENTAL .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Chemical composition and phagocyte immunomodulatory activity of <i>Ferula iliensis</i> essential oils.
  • Essential oil extracts from <i>Ferula iliensis</i> have been used traditionally in Kazakhstan for treatment of inflammation and other illnesses.
  • Because little is known about the biologic activity of these essential oils that contributes to their therapeutic properties, we analyzed their chemical composition and evaluated their phagocyte immunomodulatory activity.
  • The main components of the extracted essential oils were (<i>E</i>)-propenyl <i>sec</i>-butyl disulfide (15.7-39.4%) and (<i>Z</i>)-propenyl <i>sec</i>-butyl disulfide (23.4-45.0%).
  • <i>Ferula</i> essential oils stimulated [Ca<sup>2+</sup>]<sub>i</sub> mobilization in human neutrophils and activated ROS production in human neutrophils and murine bone marrow phagocytes.
  • Activation of human neutrophil [Ca<sup>2+</sup>]<sub>i</sub> flux by <i>Ferula</i> essential oils was dose-dependently inhibited by capsazepine, a TRPV1 channel antagonist, indicating that TRPV1 channels mediate this response.
  • Furthermore, <i>Ferula</i> essential oils stimulated Ca<sup>2+</sup> influx in TRPV1 channel-transfected HEK293 cells and desensitized the capsaicin-induced response in these cells.
  • Additional molecular modeling with known TRPV1 channel agonists suggested that the active component is likely to be (<i>Z</i>)-propenyl <i>sec</i>-butyl disulfide.
  • Our results provide a cellular and molecular basis to explain at least part of the beneficial therapeutic properties of FEOs.
  • [MeSH-major] Ferula / chemistry. Neutrophils / immunology. Oils, Volatile / chemistry. Oils, Volatile / pharmacology. Phagocytes / immunology
  • [MeSH-minor] Animals. Calcium / metabolism. Cells, Cultured. HEK293 Cells. Humans. Mice. TRPV Cation Channels / metabolism

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  • [Copyright] © Society for Leukocyte Biology.
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  • (PMID = 28258152.001).
  • [ISSN] 1938-3673
  • [Journal-full-title] Journal of leukocyte biology
  • [ISO-abbreviation] J. Leukoc. Biol.
  • [Language] eng
  • [Grant] United States / NIGMS NIH HHS / GM / P30 GM110732
  • [Publication-type] Journal Article; Research Support, U.S. Gov't, Non-P.H.S.; Research Support, Non-U.S. Gov't; Research Support, N.I.H., Extramural
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Oils, Volatile; 0 / TRPV Cation Channels; SY7Q814VUP / Calcium
  • [Keywords] NOTNLM ; calcium flux (major topic) / molecular modeling (major topic) / neutrophil (major topic) / reactive oxygen species (major topic) / transient receptor potential vanilloid 1 channel (major topic)
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96. Ryzhov S, Matafonov A, Galindo CL, Zhang Q, Tran TL, Lenihan DJ, Lenneman CG, Feoktistov I, Sawyer DB: ERBB signaling attenuates proinflammatory activation of nonclassical monocytes. Am J Physiol Heart Circ Physiol; 2017 May 01;312(5):H907-H918
NCI CPTC Antibody Characterization Program. NCI CPTC Antibody Characterization Program .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [MeSH-major] Inflammation / physiopathology. Monocytes. Receptor, Epidermal Growth Factor / biosynthesis. Signal Transduction
  • [MeSH-minor] Female. Humans. In Vitro Techniques. Macrophage Activation. Male. Middle Aged. Neuregulin-1 / metabolism. Neuregulin-1 / therapeutic use. Phosphatidylinositol 3-Kinases / metabolism. Receptor, ErbB-2 / biosynthesis. Receptor, ErbB-2 / genetics. Receptor, ErbB-3 / biosynthesis. Receptor, ErbB-3 / genetics. Recombinant Proteins / metabolism. Tumor Necrosis Factor-alpha / biosynthesis