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6. 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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7. 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<sub>2.5</sub> Collected in Japan on the Respiratory and Immune Systems. Int J Toxicol; 2017 Mar/Apr;36(2):153-164
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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
  • [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 / aqueous extracts / asthma / industrial area / organic extracts / urban area
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8. Hellmuth I, Freund I, Schlöder J, Seidu-Larry S, Thüring K, Slama K, Langhanki J, Kaloyanova S, Eigenbrod T, Krumb M, Röhm S, Peneva K, Opatz T, Jonuleit H, Dalpke AH, Helm M: Bioconjugation of Small Molecules to RNA Impedes Its Recognition by Toll-Like Receptor 7. Front Immunol; 2017;8:312

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  • [Title] Bioconjugation of Small Molecules to RNA Impedes Its Recognition by Toll-Like Receptor 7.
  • Among these, the endosomal toll-like receptor 7 (TLR7) is known to be activated by single-stranded RNA (ssRNA), which can be specifically influenced through elements of sequence structure and posttranscriptional modifications.

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  • (PMID = 28392787.001).
  • [ISSN] 1664-3224
  • [Journal-full-title] Frontiers in immunology
  • [ISO-abbreviation] Front Immunol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; bioconjugate / click chemistry / immunostimulation / mRNA / siRNA / small molecules / toll-like receptor
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9. 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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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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  • [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. 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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12. Yu J, Zhang B, Zhang Y, Xu CQ, Zhuo W, Ge J, Li J, Gao N, Li Y, Yang M: A binding-block ion selective mechanism revealed by a Na/K selective channel. Protein Cell; 2017 Sep 18;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] A binding-block ion selective mechanism revealed by a Na/K selective channel.
  • Mechanosensitive (MS) channels are extensively studied membrane protein for maintaining intracellular homeostasis through translocating solutes and ions across the membrane, but its mechanisms of channel gating and ion selectivity are largely unknown.
  • Here, we identified the YnaI channel as the Na<sup>+</sup>/K<sup>+</sup> cation-selective MS channel and solved its structure at 3.8 Å by cryo-EM single-particle method.
  • YnaI exhibits low conductance among the family of MS channels in E. coli, and shares a similar overall heptamer structure fold with previously studied MscS channels.
  • By combining structural based mutagenesis, quantum mechanical and electrophysiological characterizations, we revealed that ion selective filter formed by seven hydrophobic methionine (YnaI<sup>Met158</sup>) in the transmembrane pore determined ion selectivity, and both ion selectivity and gating of YnaI channel were affected by accompanying anions in solution.
  • Further quantum simulation and functional validation support that the distinct binding energies with various anions to YnaI<sup>Met158</sup> facilitate Na<sup>+</sup>/K<sup>+</sup> pass through, which was defined as binding-block mechanism.
  • Our structural and functional studies provided a new perspective for understanding the mechanism of how MS channels select ions driven by mechanical force.

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  • (PMID = 28921397.001).
  • [ISSN] 1674-8018
  • [Journal-full-title] Protein & cell
  • [ISO-abbreviation] Protein Cell
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Keywords] NOTNLM ; MscS / Na+/K+ selective channel / cryo-EM
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13. 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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4. Liu B, Li Y, Ji H, Lu H, Li H, Shi Y: Glutamine attenuates obstructive cholestasis in rats via farnesoid X receptor-mediated regulation of Bsep and Mrp2. Can J Physiol Pharmacol; 2017 Feb;95(2):215-223
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  • [Title] Glutamine attenuates obstructive cholestasis in rats via farnesoid X receptor-mediated regulation of Bsep and Mrp2.
  • To investigate the protective effect of glutamine (Gln) against obstructive cholestasis in association with farnesoid X receptor (FXR) activation, an obstructive cholestasis model was established in male Sprague-Dawley rats by bile duct ligation (BDL).
  • [MeSH-minor] Animals. Cholesterol 7-alpha-Hydroxylase / antagonists & inhibitors. Hepatocytes / metabolism. Liver Function Tests. Male. Organic Anion Transporters, Sodium-Dependent / antagonists & inhibitors. Primary Cell Culture. Protective Agents / adverse effects. Protective Agents / pharmacology. RNA, Small Interfering / pharmacology. Rats. Symporters / antagonists & inhibitors

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  • (PMID = 28051334.001).
  • [ISSN] 1205-7541
  • [Journal-full-title] Canadian journal of physiology and pharmacology
  • [ISO-abbreviation] Can. J. Physiol. Pharmacol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Canada
  • [Chemical-registry-number] 0 / Abcb11 protein, rat; 0 / Multidrug Resistance-Associated Proteins; 0 / Organic Anion Transporters, Sodium-Dependent; 0 / Protective Agents; 0 / RNA, Small Interfering; 0 / Receptors, Cytoplasmic and Nuclear; 0 / Symporters; 0 / farnesoid X-activated receptor; 0 / nuclear receptor subfamily 0, group B, member 2; 0RH81L854J / Glutamine; 145420-23-1 / sodium-bile acid cotransporter; 4AF605U6JN / multidrug resistance-associated protein 2; EC 1.14.14.23 / Cholesterol 7-alpha-Hydroxylase
  • [Keywords] NOTNLM ; Bsep / FXR / Mrp2 / acide biliaire / bile acid / cholestase obstructive / glutamine / obstructive cholestasis
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15. 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 Oct 13;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [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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16. Dobitz S, Aronoff MR, Wennemers H: Oligoprolines as Molecular Entities for Controlling Distance in Biological and Material Sciences. Acc Chem Res; 2017 Sep 08;
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  • [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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  • (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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17. Abdullahi W, Brzica H, Ibbotson K, Davis TP, Ronaldson PT: Bone morphogenetic protein-9 increases the functional expression of organic anion transporting polypeptide 1a4 at the blood-brain barrier via the activin receptor-like kinase-1 receptor. J Cereb Blood Flow Metab; 2017 Jul;37(7):2340-2345

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Bone morphogenetic protein-9 increases the functional expression of organic anion transporting polypeptide 1a4 at the blood-brain barrier via the activin receptor-like kinase-1 receptor.
  • Targeting uptake transporters such as organic anion transporting polypeptide 1a4 (Oatp1a4) at the blood-brain barrier (BBB) can facilitate central nervous system (CNS) drug delivery.
  • Here, we show that activation of activin receptor-like kinase (ALK)-1 using bone morphogenetic protein (BMP)-9 increases Oatp1a4 protein expression in rat brain microvessels in vivo.
  • [MeSH-major] Activin Receptors / metabolism. Blood-Brain Barrier / drug effects. Growth Differentiation Factor 2 / pharmacology. Microvessels / drug effects. Organic Anion Transporters / genetics

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  • (PMID = 28387157.001).
  • [ISSN] 1559-7016
  • [Journal-full-title] Journal of cerebral blood flow and metabolism : official journal of the International Society of Cerebral Blood Flow and Metabolism
  • [ISO-abbreviation] J. Cereb. Blood Flow Metab.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Acvrl1 protein, rat; 0 / Growth Differentiation Factor 2; 0 / LDN 193189; 0 / Organic Anion Transporters; 0 / Pyrazoles; 0 / Pyrimidines; 0 / Slco1a4 protein, rat; EC 2.7.11.30 / Activin Receptors
  • [Keywords] NOTNLM ; Basic science / blood–brain barrier / endothelium / pharmacology / vascular biology
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18. Yang L, Hu Z, Luo J, Tang C, Zhang S, Ning W, Dong C, Huang J, Liu X, Zhou HB: Dual functional small molecule fluorescent probes for image-guided estrogen receptor-specific targeting coupled potent antiproliferative potency for breast cancer therapy. Bioorg Med Chem; 2017 Jul 01;25(13):3531-3539
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Dual functional small molecule fluorescent probes for image-guided estrogen receptor-specific targeting coupled potent antiproliferative potency for breast cancer therapy.
  • Furthermore, target molecule 3e could cross the cell membrane, localize and image drug-target interaction in real time without cell washing.
  • [MeSH-major] Breast Neoplasms / diagnostic imaging. Breast Neoplasms / drug therapy. Coumarins / pharmacology. Estrogen Receptor alpha / antagonists & inhibitors. Fluorescent Dyes / pharmacology. Small Molecule Libraries / pharmacology
  • [MeSH-minor] Cell Proliferation / drug effects. Dose-Response Relationship, Drug. Drug Design. Drug Screening Assays, Antitumor. Female. Humans. MCF-7 Cells. Molecular Structure. Structure-Activity Relationship. Tamoxifen / chemistry. Tamoxifen / pharmacology

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  • [Copyright] Copyright © 2017 Elsevier Ltd. All rights reserved.
  • (PMID = 28506582.001).
  • [ISSN] 1464-3391
  • [Journal-full-title] Bioorganic & medicinal chemistry
  • [ISO-abbreviation] Bioorg. Med. Chem.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Coumarins; 0 / Estrogen Receptor alpha; 0 / Fluorescent Dyes; 0 / Small Molecule Libraries; 0 / estrogen receptor alpha, human; 094ZI81Y45 / Tamoxifen
  • [Keywords] NOTNLM ; Antiproliferative activity / Breast cancer / Coumarin derivatives / Estrogen receptor / Fluorescent probes
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19. 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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20. 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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21. Hirota Y, Nakagawa K, Mimatsu S, Sawada N, Sakaki T, Kubodera N, Kamao M, Tsugawa N, Suhara Y, Okano T: Nongenomic effects of 1α,25-dihydroxyvitamin D&lt;sub&gt;3&lt;/sub&gt; on cartilage formation deduced from comparisons between Cyp27b1 and Vdr knockout mice. Biochem Biophys Res Commun; 2017 Jan 29;483(1):359-365
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

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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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22. 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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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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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23. Attignon EA, Distel E, Le-Grand B, Leblanc AF, Barouki R, de Oliveira E, Aggerbeck M, Blanc EB: Down-regulation of the expression of alcohol dehydrogenase 4 and CYP2E1 by the combination of α-endosulfan and dioxin in HepaRG human cells. Toxicol In Vitro; 2017 Jul 01;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Pesticides and other persistent organic pollutants are considered as risk factors for liver diseases.
  • We treated the human hepatic cell line HepaRG with both 2,3,7,8 tetrachlorodibenzo-p-dioxin (TCDD) and the organochlorine pesticide, α-endosulfan, to evaluate their combined impact on the expression of hepatic genes involved in alcohol metabolism.
  • The PXR, CAR and estrogen receptor alpha transcription factors were not modulators of the effects of α-endosulfan, as assessed by siRNA transfection.
  • In another human hepatic cell line, HepG2, TCDD decreased the expression of ADH4 and CYP2E1 mRNAs whereas α-endosulfan had no effect on these genes.

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  • [Copyright] Copyright © 2017. Published by Elsevier Ltd.
  • (PMID = 28673560.001).
  • [ISSN] 1879-3177
  • [Journal-full-title] Toxicology in vitro : an international journal published in association with BIBRA
  • [ISO-abbreviation] Toxicol In Vitro
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; ADH4 / Liver / Organochlorine pesticide / Persistent organic pollutant / Pollutant mixture / TCDD
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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;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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. 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

  • [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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26. Rosa M, Gonzalez-Nunez V, Barreto-Valer K, Marcelo F, Sánchez-Sánchez J, Calle LP, Arévalo JC, Rodríguez RE, Jiménez-Barbero J, Arsequell G, Valencia G: Role of the sugar moiety on the opioid receptor binding and conformation of a series of enkephalin neoglycopeptides. Bioorg Med Chem; 2017 Apr 01;25(7):2260-2265
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
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Carbohydrates; 0 / Enkephalins; 0 / Glycopeptides; 0 / Receptors, Opioid
  • [Keywords] NOTNLM ; Enkephalin-related / Glycosylation / Neoglycopeptides / Neuropeptide / Opioid receptors / Pharmacology
  •  go-up   go-down


27. 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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  • [ISSN] 1476-4687
  • [Journal-full-title] Nature
  • [ISO-abbreviation] Nature
  • [Language] eng
  • [Publication-type] Journal Article
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28. 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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29. 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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30. 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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31. 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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  • [ErratumIn] Pflugers Arch. 2017 Aug 24;: [28840222.001]
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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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32. 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

  • MedlinePlus Health Information. consumer health - Lung Diseases.
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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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33. Kobayashi T, Koizumi T, Kobayashi M, Ogura J, Horiuchi Y, Kimura Y, Kondo A, Furugen A, Narumi K, Takahashi N, Iseki K: Insulin stimulates transport of organic anion compounds mediated by organic anion transporting polypeptide 2B1 in the human intestinal cell line Caco-2. Drug Metab Pharmacokinet; 2017 Apr;32(2):157-163
Hazardous Substances Data Bank. TAUROCHOLIC ACID .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Insulin stimulates transport of organic anion compounds mediated by organic anion transporting polypeptide 2B1 in the human intestinal cell line Caco-2.
  • Organic anion transporting polypeptide 2B1 (OATP2B1) is the major uptake transporter in the intestine, and transports various clinically used therapeutic agents.
  • Insulin acts through the insulin receptor in targeted cells, and Rab8A is one of the insulin signaling pathways.
  • The small intestine in humans also expresses insulin receptor and Rab8A.
  • Caco-2 cells treated with insulin showed increased OATP2B1 expression at the cell surface.
  • [MeSH-major] Insulin / pharmacology. Organic Anion Transporters / metabolism

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  • [Copyright] Copyright © 2016 The Japanese Society for the Study of Xenobiotics. Published by Elsevier Ltd. All rights reserved.
  • (PMID = 28318878.001).
  • [ISSN] 1880-0920
  • [Journal-full-title] Drug metabolism and pharmacokinetics
  • [ISO-abbreviation] Drug Metab. Pharmacokinet.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Insulin; 0 / Organic Anion Transporters; 0 / SLCO2B1 protein, human; 5E090O0G3Z / Taurocholic Acid
  • [Keywords] NOTNLM ; Caco-2 cell / Estrone-3-sulfate / Insulin / Intestinal absorption / OATP2B1
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34. Kaitsiotou H, Keul M, Hardick J, Mühlenberg T, Ketzer J, Ehrt C, Krüll J, Medda F, Koch O, Giordanetto F, Bauer S, Rauh D: Inhibitors to overcome secondary mutations in the stem cell factor receptor KIT. J Med Chem; 2017 Oct 09;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Inhibitors to overcome secondary mutations in the stem cell factor receptor KIT.
  • In modern cancer therapy, the use of small organic molecules against receptor tyrosine kinases (RTKs) has been shown to be a valuable strategy.
  • The tyrosine kinase mast/stem cell growth factor receptor KIT is an example of a clinically relevant RTK.

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  • (PMID = 28991465.001).
  • [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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35. 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 May 06;486(3):659-664
Hazardous Substances Data Bank. DACTINOMYCIN .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [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
  • [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 / Calcium signaling / Cyclic AMP / Hepatocytes / Type 2 inositol 1,4,5-trisphosphate receptor
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36. 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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37. 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
Genetic Alliance. consumer health - Hepatitis.

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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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38. 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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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [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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39. Kersseboom S, van Gucht ALM, van Mullem A, Brigante G, Farina S, Carlsson B, Donkers JM, van de Graaf SFJ, Peeters RP, Visser TJ: Role of the Bile Acid Transporter SLC10A1 in Liver Targeting of the Lipid-Lowering Thyroid Hormone Analog Eprotirome. Endocrinology; 2017 Oct 01;158(10):3307-3318

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • The thyroid hormone (TH) analog eprotirome (KB2115) was developed to lower cholesterol through selective activation of the TH receptor (TR) β1 in the liver.
  • We explored the transport of eprotirome across the plasma membrane by members of three TH transporter families: monocarboxylate transporters MCT8 and MCT10; Na-independent organic anion transporters 1A2, 1B1, 1B3, 1C1, 2A1, and 2B1; and Na-dependent organic anion transporters SLC10A1 to SLC10A7.
  • [MeSH-major] Anilides / pharmacokinetics. Anilides / pharmacology. Anticholesteremic Agents. Liver / drug effects. Organic Anion Transporters, Sodium-Dependent / physiology. Symporters / physiology
  • [MeSH-minor] Animals. Biological Transport. COS Cells. Cell Membrane / metabolism. Cercopithecus aethiops. Humans. Mice. Mice, Knockout. Molecular Targeted Therapy. Monocarboxylic Acid Transporters / metabolism. Organic Anion Transporters / metabolism. RNA, Messenger / analysis. Reverse Transcriptase Polymerase Chain Reaction. Sodium / pharmacology. Thyroid Hormones / metabolism. Transfection

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  • [Copyright] Copyright © 2017 Endocrine Society.
  • (PMID = 28938430.001).
  • [ISSN] 1945-7170
  • [Journal-full-title] Endocrinology
  • [ISO-abbreviation] Endocrinology
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / 3-((3,5-dibromo-4-(4-hydroxy-3-(1-methylethyl)phenoxy)phenyl)amino)-3-oxopropanoic acid; 0 / Anilides; 0 / Anticholesteremic Agents; 0 / Monocarboxylic Acid Transporters; 0 / Organic Anion Transporters; 0 / Organic Anion Transporters, Sodium-Dependent; 0 / RNA, Messenger; 0 / Symporters; 0 / Thyroid Hormones; 145420-23-1 / sodium-bile acid cotransporter; 9NEZ333N27 / Sodium
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40. 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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41. 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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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • 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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42. 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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43. 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 Sep 05;

  • [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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44. 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

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [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
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45. 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
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46. 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.
  • Mimicking in that way important in vivo features of tumor microenvironments, we found that only low molecular weight HA (LMW-HA) in soluble form promoted proliferation of a melanoma cell line (BRO), while it enhanced cell invasion in bound form.
  • The molecular weight specificity of LMW-HA was verified to be CD44 receptor dependent and was correlated to adhesive ligand-receptor interactions in quantitative colloidal force spectroscopy at single cell level.

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  • [Copyright] Copyright © 2016 Acta Materialia Inc. Published by Elsevier Ltd. All rights reserved.
  • (PMID = 27965172.001).
  • [ISSN] 1878-7568
  • [Journal-full-title] Acta biomaterialia
  • [ISO-abbreviation] Acta Biomater
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; CD44 receptor / Collagen / Extracellular matrix / Hyaluronan / Melanoma cells
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47. 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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  • [Journal-full-title] Journal of nutrition and metabolism
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48. 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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49. 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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50. 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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51. 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 Jul;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

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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
  • [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 / Cellular differentiation / D-seco vitamin D / Secosteroids / Transcriptional activity / Vitamin D analogues / Vitamin D receptor
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52. Chubanov V, Ferioli S, Gudermann T: Assessment of TRPM7 functions by drug-like small molecules. Cell Calcium; 2017 Nov;67:166-173

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  • 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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53. Haruta M, Sussman MR: Ligand Receptor-Mediated Regulation of Growth in Plants. Curr Top Dev Biol; 2017;123:331-363
SciCrunch. BioNumbers: The Database of Useful Biological Numbers: Data: Value observation .

  • [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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54. 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

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  • [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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55. 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.


56. 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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57. 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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58. 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
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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

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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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59. 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
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  • The highly poisonous botulinum neurotoxins, produced by the bacterium Clostridium botulinum, act on their hosts by a high-affinity association to two receptors on neuronal cell surfaces as the first step of invasion.
  • The glycan motifs of gangliosides serve as initial coreceptors for these protein complexes, whereby a membrane protein receptor is bound.
  • We here propose that the glycan part of the ganglioside receptors mainly provides abundance and specificity, whereas the interaction with the membrane itself and protein receptor brings about the strong total binding of the toxin to the neuronal membrane.
  • [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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60. 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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61. Keller AN, Eckle SB, Xu W, Liu L, Hughes VA, Mak JY, Meehan BS, Pediongco T, Birkinshaw RW, Chen Z, Wang H, D'Souza C, Kjer-Nielsen L, Gherardin NA, Godfrey DI, Kostenko L, Corbett AJ, Purcell AW, Fairlie DP, McCluskey J, Rossjohn J: Drugs and drug-like molecules can modulate the function of mucosal-associated invariant T cells. Nat Immunol; 2017 Apr;18(4):402-411
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  • Here we identified a range of small organic molecules, drugs, drug metabolites and drug-like molecules, including salicylates and diclofenac, as MR1-binding ligands.
  • Crystal structures of a T cell antigen receptor (TCR) from a MAIT cell in complex with MR1 bound to the non-stimulatory and stimulatory compounds showed distinct ligand orientations and contacts within MR1, which highlighted the versatility of the MR1 binding pocket.
  • This indicated that drugs and drug-like molecules can modulate MAIT cell function in mammals.
  • [MeSH-minor] Binding Sites. Cell Line. Crystallography, X-Ray. Drug Discovery. Humans. Hydrogen Bonding. Ligands. Lymphocyte Activation / drug effects. Lymphocyte Activation / immunology. Models, Molecular. Molecular Conformation. Molecular Structure. Protein Binding. Receptors, Antigen, T-Cell / chemistry. Receptors, Antigen, T-Cell / metabolism. Structure-Activity Relationship

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  • (PMID = 28166217.001).
  • [ISSN] 1529-2916
  • [Journal-full-title] Nature immunology
  • [ISO-abbreviation] Nat. Immunol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Chemical-registry-number] 0 / Histocompatibility Antigens Class I; 0 / Ligands; 0 / MR1 protein, human; 0 / Minor Histocompatibility Antigens; 0 / Receptors, Antigen, T-Cell
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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
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  • Further, molecular docking analysis reveals that compound 2a binds to δ-opioid receptor (DOR) with comparatively better D-score than to μ (MOR) and κ (KOR) receptors.
  • [MeSH-minor] Animals. Cell Line. Chemistry Techniques, Synthetic. Drug Design. Female. Humans. Male. Mice. Pain / drug therapy. Prostaglandin-Endoperoxide Synthases / metabolism. Protein Conformation. Receptors, Opioid / chemistry. Receptors, Opioid / metabolism

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  • [Copyright] Copyright © 2016 Elsevier Masson SAS. All rights reserved.
  • (PMID = 28063353.001).
  • [ISSN] 1768-3254
  • [Journal-full-title] European journal of medicinal chemistry
  • [ISO-abbreviation] Eur J Med Chem
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] France
  • [Chemical-registry-number] 0 / Amino Alcohols; 0 / Analgesics; 0 / Benzopyrans; 0 / Isoxazoles; 0 / Receptors, Opioid; EC 1.14.99.1 / Prostaglandin-Endoperoxide Synthases
  • [Keywords] NOTNLM ; Antinociceptive activity / Benzopyran fused isoxazolidines / Intramolecular 1,3-dipolar cycloaddition / Opioid receptor / Reductive cleavage
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63. 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 Feb;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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  • [ISSN] 1365-2613
  • [Journal-full-title] International journal of experimental pathology
  • [ISO-abbreviation] Int J Exp Pathol
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Chemical-registry-number] 0 / Estrogen Receptor alpha; 0 / Estrogens
  • [Keywords] NOTNLM ; chemical carcinogenesis / mammary tumours / oestrogen receptor α / progesterone receptor / treadmill / vascularization
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64. 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 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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65. 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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66. Park WH, Kang S, Lee HK, Salihovic S, Bavel BV, Lind PM, Pak YK, Lind L: Relationships between serum-induced AhR bioactivity or mitochondrial inhibition and circulating polychlorinated biphenyls (PCBs). Sci Rep; 2017 Aug 24;7(1):9383

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Metabolic syndrome and mitochondrial dysfunction have been linked to elevated serum levels of persistent organic pollutants (POPs).
  • However, it is not clear which specific POPs contribute to aryl hydrocarbon receptor (AhR)-dependent bioactivity or inhibit mitochondrial function in human subjects.

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  • (PMID = 28839207.001).
  • [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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67. Lee MS, Jung S, Shin Y, Lee S, Kim CT, Kim IH, Kim Y: Lipolytic efficacy of alginate double-layer nanoemulsion containing oleoresin capsicum in differentiated 3T3-L1 adipocytes. Food Nutr Res; 2017;61(1):1339553

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • <b>Background</b>: Oleoresin capsicum (OC) is an organic extract from fruits of the genus <i>Capsicum</i>, and has been reported to have an anti-obesity effect.
  • In AN-treated cells, mRNA levels of peroxisome proliferator-activated receptor-γ and the fatty acid-binding protein adipocyte protein-2, which are involved in adipogenesis, were down-regulated, whereas those of genes related to lipolysis, including hormone-sensitive lipase and carnitine palmitoyl transferase-1α, were up-regulated compared with SN-treated cells.

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  • (PMID = 28747860.001).
  • [ISSN] 1654-661X
  • [Journal-full-title] Food & nutrition research
  • [ISO-abbreviation] Food Nutr Res
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Free fatty acid / glycerol / lipolysis / mRNA expression / obesity
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68. 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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69. 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
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; 1-AG / 2-AG / CB1 / calcium signaling / cannabinoid / modulation
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70. 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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71. 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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72. 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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73. 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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74. 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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75. 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

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • The plethora of physiopathological events associated with brain ischemia are regulate through multiple signaling pathways leading to the activation of oxidative stress process, Ca<sup>2+</sup> dyshomeostasis, mitochondrial dysfunction, proinflammatory mediators, excitotoxicity and/or programmed neuronal cell death.
  • Additionally, experimental evidence supports its actions to ameliorate ischemic long-term behavioural and neuronal deficits, preserving the functional integrity of the blood-brain barrier, inducing neurogenesis and cell proliferation through receptor-dependent mechanism, as well as improving synaptic transmission.

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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
  • (PMID = 28065781.001).
  • [ISSN] 1873-4596
  • [Journal-full-title] Free radical biology & medicine
  • [ISO-abbreviation] Free Radic. Biol. Med.
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Brain ischemia / Free radicals / Melatonin / Neuroprotection
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76. Deng T, Peng Y, Zhang R, Wang J, Zhang J, Gu Y, Huang D, Deng D: Water-Solubilizing Hydrophobic ZnAgInSe/ZnS QDs with Tumor-Targeted cRGD-Sulfobetaine-PIMA-Histamine Ligands via a Self-Assembly Strategy for Bioimaging. ACS Appl Mater Interfaces; 2017 Apr 05;9(13):11405-11414

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Exploring the organic-to-aqueous phase transfer of quantum dots (QDs) is significant for achieving their versatile applications in biomedical fields.
  • Herein, the new highly fluorescent tumor-targeted QDs-clusters consisting of ZnAgInSe/ZnS (ZAISe/ZnS) QDs and sulfobetaine-PIMA-histamine (SPH) polymer with the α<sub>ν</sub>β<sub>3</sub> integrin receptor cyclic RGD (c-RGD) were developed via ligand exchange and an accompanying self-assembly process.
  • In the meantime, those clusters also recognized and enriched the cell surface when cocultured with the α<sub>ν</sub>β<sub>3</sub> integrin receptor overexpressed malignant cells (U87MG tumor).

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  • (PMID = 28293947.001).
  • [ISSN] 1944-8252
  • [Journal-full-title] ACS applied materials & interfaces
  • [ISO-abbreviation] ACS Appl Mater Interfaces
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; QDs-clusters / optical imaging / quaternary quantum dots / self-assembly / tumor targeting polymer
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77. Elshenawy OH, Abdelhamid G, Soshilov AA, Denison MS, El-Kadi AO: Down-regulation of cytochrome P450 1A1 by monomethylarsonous acid in human HepG2 cells. Toxicol Lett; 2017 Mar 15;270:34-50

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • Arsenic is capable of modulating the expression of aryl hydrocarbon receptor (AhR)-regulated genes, nevertheless, whether its trivalent organic metabolites have similar effects or not need to be investigated.
  • [MeSH-minor] Arsenites / toxicity. Basic Helix-Loop-Helix Transcription Factors / genetics. Basic Helix-Loop-Helix Transcription Factors / metabolism. Cell Survival / drug effects. Heme Oxygenase-1 / genetics. Heme Oxygenase-1 / metabolism. Hep G2 Cells. Humans. Oxidative Stress / drug effects. Polychlorinated Dibenzodioxins / toxicity. Protein Processing, Post-Translational. Protein Stability / drug effects. RNA, Messenger / genetics. RNA, Messenger / metabolism. Reactive Oxygen Species / metabolism. Receptors, Aryl Hydrocarbon / genetics. Receptors, Aryl Hydrocarbon / metabolism. Signal Transduction. Sodium Compounds / toxicity

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28189647.001).
  • [ISSN] 1879-3169
  • [Journal-full-title] Toxicology letters
  • [ISO-abbreviation] Toxicol. Lett.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / AHR protein, human; 0 / Arsenites; 0 / Basic Helix-Loop-Helix Transcription Factors; 0 / Organometallic Compounds; 0 / Polychlorinated Dibenzodioxins; 0 / RNA, Messenger; 0 / Reactive Oxygen Species; 0 / Receptors, Aryl Hydrocarbon; 0 / Sodium Compounds; 0 / monomethylarsonous acid; 48OVY2OC72 / sodium arsenite; EC 1.14.14.1 / CYP1A1 protein, human; EC 1.14.14.1 / Cytochrome P-450 CYP1A1; EC 1.14.14.18 / HMOX1 protein, human; EC 1.14.14.18 / Heme Oxygenase-1
  • [Keywords] NOTNLM ; Arsenite / Aryl hydrocarbon receptor / CYP1A1 / Free radicals / Monomethylarsonous acid / ROS / XRE
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78. Panduga V, Stocks MJ, Bosquillon C: Ipratropium is 'luminally recycled' by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers. Int J Pharm; 2017 Oct 30;532(1):328-336

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Ipratropium is 'luminally recycled' by an inter-play between apical uptake and efflux transporters in Calu-3 bronchial epithelial cell layers.
  • In order to elucidate the role of drug transporters, ipratropium bidirectional transport as well as accumulation and release studies were performed in layers of the broncho-epithelial cell line Calu-3 grown at an air-liquid interface, in presence or absence of a range of transporter inhibitors.
  • Interestingly, monitoring drug release post cell loading revealed the presence of an efficient efflux system on the apical side of the cell layers.
  • The data are in agreement with an apical Organic Cation Transporter (OCT) being involved in this process but also suggest the participation of unknown uptake and efflux transporters sensitive to probenecid.

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28855136.001).
  • [ISSN] 1873-3476
  • [Journal-full-title] International journal of pharmaceutics
  • [ISO-abbreviation] Int J Pharm
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Keywords] NOTNLM ; Carrier-mediated transport / Drug inhalation / Drug transporters / In vitro models / Muscarinic M3 receptor antagonists / Pulmonary drug delivery
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79. 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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80. 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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81. Zhang S, Nava MJ, Chow GK, Lopez N, Wu G, Britt DR, Nocera DG, Cummins CC: On the incompatibility of lithium-O&lt;sub&gt;2&lt;/sub&gt; battery technology with CO&lt;sub&gt;2&lt;/sub&gt;. Chem Sci; 2017 Sep 01;8(9):6117-6122

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • When solubilized in a hexacarboxamide cryptand anion receptor, the peroxide dianion reacts rapidly with CO<sub>2</sub> in polar aprotic organic media to produce hydroperoxycarbonate (HOOCO<sub>2</sub><sup>-</sup>) and peroxydicarbonate (<sup>-</sup>O<sub>2</sub>COOCO<sub>2</sub><sup>-</sup>).
  • Peroxydicarbonate is subject to thermal fragmentation into two equivalents of the highly reactive carbonate radical anion, which promotes hydrogen atom abstraction reactions responsible for the oxidative degradation of organic solvents.
  • Exposure of solid lithium peroxide (Li<sub>2</sub>O<sub>2</sub>) to CO<sub>2</sub> in polar aprotic organic media results in aggressive oxidation.
  • These findings indicate that CO<sub>2</sub> must not be introduced in conditions relevant to typical lithium-O<sub>2</sub> cell configurations, as production of HOOCO<sub>2</sub><sup>-</sup> and <sup>-</sup>O<sub>2</sub>COOCO<sub>2</sub><sup>-</sup> during lithium-O<sub>2</sub> cell cycling will lead to cell degradation <i>via</i> oxidation of organic electrolytes and other vulnerable cell components.

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  • (PMID = 28989641.001).
  • [ISSN] 2041-6520
  • [Journal-full-title] Chemical science
  • [ISO-abbreviation] Chem Sci
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] England
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82. 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
Diposit Digital de la Universitat de Barcelona. Full text from .

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] The Nuclear Receptor LXR Limits Bacterial Infection of Host Macrophages through a Mechanism that Impacts Cellular NAD Metabolism.
  • Using a model of infection by Salmonella Typhimurium, we have identified a molecular mechanism regulated by the nuclear receptor LXR that limits infection of host macrophages through transcriptional activation of the multifunctional enzyme CD38.
  • Altogether, this work reveals an unappreciated role for CD38 in bacterial-host cell interaction that can be pharmacologically exploited by activation of the LXR pathway.

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  • [Copyright] Copyright © 2017 The Author(s). Published by Elsevier Inc. All rights reserved.
  • (PMID = 28147278.001).
  • [ISSN] 2211-1247
  • [Journal-full-title] Cell reports
  • [ISO-abbreviation] Cell Rep
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; CD38 / LXR / NAD / bacterial infection / cytoskeleton / macrophage / nuclear receptor
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83. Huang Q, Chi Y, Deng J, Liu Y, Lu Y, Chen J, Dong S: Fine particulate matter 2.5 exerted its toxicological effect by regulating a new layer, long non-coding RNA. Sci Rep; 2017 Aug 24;7(1):9392
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.
  • Fine particulate matter (PM2.5) exposure, especially to its organic components, induces adverse health effects on the respiratory system.
  • Organic extracts of PM2.5 from Nanjing and Shanghai cities were adopted to treat human bronchial epithelial cell lines (BEAS-2B and A549).
  • Similar response was observed between both cell lines.
  • Antagonism of aryl hydrocarbon receptor (AHR) or inhibition of CYP1A1 diminished the effects stimulated by PM2.5.

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  • (PMID = 28839203.001).
  • [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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84. 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
  • [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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85. 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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  • [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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91. Sato Y, Kinoshita M, Takemura S, Tanaka S, Hamano G, Nakamori S, Fujikawa M, Sugawara Y, Yamamoto T, Arimoto A, Yamamura M, Sasaki M, Harada K, Nakanuma Y, Kubo S: The PD-1/PD-L1 axis may be aberrantly activated in occupational cholangiocarcinoma. Pathol Int; 2017 Mar;67(3):163-170
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [MeSH-major] Antigens, CD274 / biosynthesis. Bile Duct Neoplasms / pathology. Cholangiocarcinoma / pathology. Occupational Diseases / pathology. Programmed Cell Death 1 Receptor / biosynthesis

  • MedlinePlus Health Information. consumer health - Bile Duct Cancer.
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  • [Copyright] © 2017 Japanese Society of Pathology and John Wiley & Sons Australia, Ltd.
  • (PMID = 28139862.001).
  • [ISSN] 1440-1827
  • [Journal-full-title] Pathology international
  • [ISO-abbreviation] Pathol. Int.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Australia
  • [Chemical-registry-number] 0 / Antigens, CD274; 0 / CD274 protein, human; 0 / PDCD1 protein, human; 0 / Programmed Cell Death 1 Receptor; 0 / Solvents
  • [Keywords] NOTNLM ; immune escape / multistep carcinogenesis / occupational cholangiocarcinoma / organic solvent exposure
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92. Thompson CA, Wojta K, Pulakanti K, Rao S, Dawson P, Battle MA: GATA4 Is Sufficient to Establish Jejunal Versus Ileal Identity in the Small Intestine. Cell Mol Gastroenterol Hepatol; 2017 May;3(3):422-446
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] GATA4 Is Sufficient to Establish Jejunal Versus Ileal Identity in the Small Intestine.
  • BACKGROUND & AIMS: Patterning of the small intestinal epithelium along its cephalocaudal axis establishes three functionally distinct regions: duodenum, jejunum, and ileum.
  • Efficient nutrient assimilation and growth depend on the proper spatial patterning of specialized digestive and absorptive functions performed by duodenal, jejunal, and ileal enterocytes.
  • When enterocyte function is disrupted by disease or injury, intestinal failure can occur.
  • One approach to alleviate intestinal failure would be to restore lost enterocyte functions.
  • The molecular mechanisms determining regionally defined enterocyte functions, however, are poorly delineated.
  • We previously showed that GATA binding protein 4 (GATA4) is essential to define jejunal enterocytes.
  • The goal of this study was to test the hypothesis that GATA4 is sufficient to confer jejunal identity within the intestinal epithelium.
  • METHODS: To test this hypothesis, we generated a novel <i>Gata4</i> conditional knock-in mouse line and expressed GATA4 in the ileum, where it is absent.
  • RESULTS: We found that GATA4-expressing ileum lost ileal identity.
  • The global gene expression profile of GATA4-expressing ileal epithelium aligned more closely with jejunum and duodenum rather than ileum.
  • Focusing on jejunal vs ileal identity, we defined sets of jejunal and ileal genes likely to be regulated directly by GATA4 to suppress ileal identity and promote jejunal identity.
  • Furthermore, our study implicates GATA4 as a transcriptional repressor of <i>fibroblast growth factor 15 (Fgf15)</i>, which encodes an enterokine that has been implicated in an increasing number of human diseases.
  • CONCLUSIONS: Overall, this study refines our understanding of an important GATA4-dependent molecular mechanism to pattern the intestinal epithelium along its cephalocaudal axis by elaborating on GATA4's function as a crucial dominant molecular determinant of jejunal enterocyte identity.
  • Microarray data from this study have been deposited into NCBI Gene Expression Omnibus (http://www.ncbi.nlm.nih.gov/geo) and are accessible through GEO series accession number GSE75870.

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  • (PMID = 28462382.001).
  • [ISSN] 2352-345X
  • [Journal-full-title] Cellular and molecular gastroenterology and hepatology
  • [ISO-abbreviation] Cell Mol Gastroenterol Hepatol
  • [Language] eng
  • [Grant] United States / NIDDK NIH HHS / DK / R01 DK047987; United States / NIDDK NIH HHS / DK / R01 DK087873; United States / NIDDK NIH HHS / DK / R29 DK047987; United States / NIDDK NIH HHS / DK / R56 DK087873
  • [Publication-type] Journal Article
  • [Publication-country] United States
  • [Keywords] NOTNLM ; Cyp7a1, cytochrome P450 family 7 subfamily A member 1 / E, embryonic day / EMSA, electrophoretic mobility shift assay / Enterohepatic Signaling / FXR / FXR, farnesoid X receptor / Fabp6, fatty acid binding protein 6 / Fgf, fibroblast growth factor / Fgf15 / Jejunal Identity / OSTα/β, organic solute transporter α/β / PCR, polymerase chain reaction / SBS, short-bowel syndrome / Slc, solute carrier / TSS, transcription start site / Transcriptional Regulation / bio-ChIP-seq, biotin-mediated chromatin immunoprecipitation with high-throughput sequencing / bp, base pair / cDNA, complementary DNA / cKI, conditional knock-in / cKO, conditional knockout / dATP, deoxyadenosine triphosphate / lnl, loxP-flanked PGK-Neo-3xSV40 polyadenylation sequence / mRNA, messenger RNA / pA, polyadenylation / qRT, quantitative reverse-transcription / xiFABP, Xenopus I-FABP
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93. Giambartolomei GH, Arriola Benitez PC, Delpino MV: &lt;i&gt;Brucella&lt;/i&gt; and Osteoarticular Cell Activation: Partners in Crime. Front Microbiol; 2017;8:256

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] <i>Brucella</i> and Osteoarticular Cell Activation: Partners in Crime.
  • The molecular mechanisms implicated in bone damage have been recently elucidated. <i>B. abortus</i> induces bone damage through diverse mechanisms in which TNF-α and the receptor activator of nuclear factor kappa-B ligand (RANKL)-the natural modulator of bone homeostasis are involved.
  • These bacteria inhibit bone matrix deposition by osteoblasts (the only bone cells involved in bone deposition), and modify the phenotype of these cells to produce matrix metalloproteinases (MMPs) and cytokine secretion, contributing to bone matrix degradation. <i>B. abortus</i> also affects osteoclasts (cells naturally involved in bone resorption) by inducing an increase in osteoclastogenesis and osteoclast activation; thus, increasing mineral and organic bone matrix resorption, contributing to bone damage.
  • The analysis of <i>B. abortus</i>-infected synoviocytes indicated that bacteria also replicate in their reticulum suggesting that they could use this cell type for intracellular replication during the osteoarticular localization of the disease.

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  • (PMID = 28265268.001).
  • [ISSN] 1664-302X
  • [Journal-full-title] Frontiers in microbiology
  • [ISO-abbreviation] Front Microbiol
  • [Language] eng
  • [Publication-type] Journal Article; Review
  • [Publication-country] Switzerland
  • [Keywords] NOTNLM ; B and T cells and Brucella / osteoarticular brucellosis / osteoblast / osteoclastogenesis / synoviocyte
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94. Taylor A, Schenkel LC, Yokich M, Bakovic M: Adaptations to excess choline in insulin resistant and Pcyt2 deficient skeletal muscle. Biochem Cell Biol; 2017 Apr;95(2):223-231
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [MeSH-minor] Administration, Oral. Animals. Antigens, CD95 / genetics. Antigens, CD95 / metabolism. Carnitine O-Palmitoyltransferase / genetics. Carnitine O-Palmitoyltransferase / metabolism. Diacylglycerol O-Acyltransferase / genetics. Diacylglycerol O-Acyltransferase / metabolism. Fatty Acids / metabolism. Gene Expression Regulation. Glucose / metabolism. Insulin Receptor Substrate Proteins / genetics. Insulin Receptor Substrate Proteins / metabolism. Mice. Mice, Knockout. Microtubule-Associated Proteins / genetics. Microtubule-Associated Proteins / metabolism. Muscle, Skeletal. Organic Cation Transport Proteins / genetics. Organic Cation Transport Proteins / metabolism. PPAR alpha / genetics. PPAR alpha / metabolism. Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha / genetics. Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha / metabolism. Signal Transduction. Stearoyl-CoA Desaturase / genetics. Stearoyl-CoA Desaturase / metabolism. Sterol Regulatory Element Binding Protein 1 / genetics. Sterol Regulatory Element Binding Protein 1 / metabolism. Triglycerides / metabolism

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  • (PMID = 28068143.001).
  • [ISSN] 1208-6002
  • [Journal-full-title] Biochemistry and cell biology = Biochimie et biologie cellulaire
  • [ISO-abbreviation] Biochem. Cell Biol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Canada
  • [Chemical-registry-number] 0 / Antigens, CD95; 0 / CTL1 protein, mouse; 0 / Fas protein, mouse; 0 / Fatty Acids; 0 / Insulin Receptor Substrate Proteins; 0 / Irs1 protein, mouse; 0 / MAP1LC3 protein, mouse; 0 / Microtubule-Associated Proteins; 0 / Organic Cation Transport Proteins; 0 / PPAR alpha; 0 / Peroxisome Proliferator-Activated Receptor Gamma Coactivator 1-alpha; 0 / Ppargc1a protein, mouse; 0 / Srebf1 protein, mouse; 0 / Sterol Regulatory Element Binding Protein 1; 0 / Triglycerides; EC 1.14.19.1 / Scd1 protein, mouse; EC 1.14.19.1 / Stearoyl-CoA Desaturase; EC 2.3.1.20 / DGAT2 protein, mouse; EC 2.3.1.20 / Dgat1 protein, mouse; EC 2.3.1.20 / Diacylglycerol O-Acyltransferase; EC 2.3.1.21 / CPT1B protein, mouse; EC 2.3.1.21 / Carnitine O-Palmitoyltransferase; EC 2.7.7.- / RNA Nucleotidyltransferases; EC 2.7.7.14 / Ethanolamine-phosphate cytidylyltransferase; IY9XDZ35W2 / Glucose; N91BDP6H0X / Choline
  • [Keywords] NOTNLM ; Pcyt2 / choline / insulin resistance / muscle squelettique / résistance à l’insuline / skeletal muscle / triglycerides / triglycérides
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95. Giordano C, Rovito D, Barone I, Mancuso R, Bonofiglio D, Giordano F, Catalano S, Gabriele B, Andò S: Benzofuran-2-acetic ester derivatives induce apoptosis in breast cancer cells by upregulating p21&lt;sup&gt;Cip/WAF1&lt;/sup&gt; gene expression in p53-independent manner. DNA Repair (Amst); 2017 Mar;51:20-30
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • We observed that benzofuran compounds bearing a phenyl or tert-butyl substituent α to the methoxycarbonyl group significantly inhibited anchorage-dependent and -independent cell growth, and induced G0/G1 cell cycle arrest in human estrogen receptor alpha positive (MCF-7 and T47D) and in triple negative MDA-MB-231 breast cancer cells, without affecting growth of MCF-10A normal breast epithelial cells.
  • Overall, we provide evidence that the newly tested benzofuran derivatives showed antiproliferative and pro-apoptotic activities against breast cancer cells regardless estrogen receptor status, suggesting their possible clinical development as anticancer agents.
  • [MeSH-minor] Antineoplastic Agents / pharmacology. Cell Cycle Checkpoints / drug effects. Cell Line, Tumor. Esters / pharmacology. Female. Gene Expression Regulation, Neoplastic. Humans. Hydrolysis. Poly(ADP-ribose) Polymerases / metabolism. Tumor Suppressor Protein p53

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  • [Copyright] Copyright © 2017 Elsevier B.V. All rights reserved.
  • (PMID = 28108275.001).
  • [ISSN] 1568-7856
  • [Journal-full-title] DNA repair
  • [ISO-abbreviation] DNA Repair (Amst.)
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Netherlands
  • [Chemical-registry-number] 0 / Antineoplastic Agents; 0 / Benzofurans; 0 / CDKN1A protein, human; 0 / Cyclin-Dependent Kinase Inhibitor p21; 0 / Esters; 0 / Tumor Suppressor Protein p53; EC 2.4.2.30 / Poly(ADP-ribose) Polymerases
  • [Keywords] NOTNLM ; Anticancer activity / Benzofurans / Breast cancer / p21Cip/WAF1
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96. 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 Sep 19;

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] Multiple organic cation transporters contribute to the renal transport of sulpiride.
  • Sulpiride, a selective dopamine D2 receptor blocker, is widely used for treatment of schizophrenia, depression, and gastric/duodenal ulcers.
  • Our results demonstrated 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 basolateral (BL) to 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] This article is protected by copyright. All rights reserved.
  • (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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97. 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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98. 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
  • [Keywords] NOTNLM ; abnormalities / benzene / gene expression / mortality / naphthalene / naphthalin
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99. Kirpotina LN, Schepetkin IA, Khlebnikov AI, Ruban OI, Ge Y, Ye RD, Kominsky DJ, Quinn MT: 4-Aroyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-ones as N-formyl peptide receptor 1 (FPR1) antagonists. Biochem Pharmacol; 2017 Oct 15;142:120-132
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  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • [Title] 4-Aroyl-3-hydroxy-5-phenyl-1H-pyrrol-2(5H)-ones as N-formyl peptide receptor 1 (FPR1) antagonists.

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  • [Copyright] Copyright © 2017 Elsevier Inc. All rights reserved.
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  • (PMID = 28690139.001).
  • [ISSN] 1873-2968
  • [Journal-full-title] Biochemical pharmacology
  • [ISO-abbreviation] Biochem. Pharmacol.
  • [Language] eng
  • [Grant] United States / NIGMS NIH HHS / GM / P30 GM110732
  • [Publication-type] Journal Article
  • [Publication-country] England
  • [Keywords] NOTNLM ; 1H-pyrrol-2(5H)-one / Antagonist / Formyl peptide receptor / Molecular modeling / Neutrophil
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100. Starick L, Riano F, Karunakaran MM, Kunzmann V, Li J, Kreiss M, Amslinger S, Scotet E, Olive D, De Libero G, Herrmann T: Butyrophilin 3A (BTN3A, CD277)-specific antibody 20.1 differentially activates Vγ9Vδ2 TCR clonotypes and interferes with phosphoantigen activation. Eur J Immunol; 2017 Jun;47(6):982-992

  • [Source] The source of this record is MEDLINE®, a database of the U.S. National Library of Medicine.
  • This study provides novel perspectives on the physiological mechanism of Vγ9Vδ2 T-cell activation, and highlights the complex mode of action of BTN3A-specific antibodies as agents in cancer immunotherapy.
  • [MeSH-major] Antibodies, Monoclonal / immunology. Antigens, CD / immunology. Butyrophilins / immunology. Lymphocyte Activation. Receptors, Antigen, T-Cell, gamma-delta / immunology. T-Lymphocytes / immunology
  • [MeSH-minor] Animals. Cell Line. HEK293 Cells. Humans. Mice

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  • [Copyright] © 2017 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
  • (PMID = 28386905.001).
  • [ISSN] 1521-4141
  • [Journal-full-title] European journal of immunology
  • [ISO-abbreviation] Eur. J. Immunol.
  • [Language] eng
  • [Publication-type] Journal Article
  • [Publication-country] Germany
  • [Chemical-registry-number] 0 / Antibodies, Monoclonal; 0 / Antigens, CD; 0 / BTN3A1 protein, human; 0 / Butyrophilins; 0 / Receptors, Antigen, T-Cell, gamma-delta
  • [Keywords] NOTNLM ; Butyrophilin / Human γδ T cells / Phosphoantigen / T-cell activation / T-cell receptor
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