Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.
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A novel antidiabetic drug, fasiglifam/TAK-875, acts as an ago-allosteric modulator of FFAR1Defining the molecular basis for the first potent and selective orthosteric agonists of the FFA2 free fatty acid receptorGPR120 is an omega-3 fatty acid receptor mediating potent anti-inflammatory and insulin-sensitizing effectsPotential roles of GPR120 and its agonists in the management of diabetesOmega-3 Fatty Acids and FFAR4The role of omega-3 fatty acid receptor GPR120 in insulin resistanceExclusive photorelease of signalling lipids at the plasma membrane.GPR40 is necessary but not sufficient for fatty acid stimulation of insulin secretion in vivo.The action and mode of binding of thiazolidinedione ligands at free fatty acid receptor 1Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice.AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodentsThe Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptorsFatty acid 16:4(n-3) stimulates a GPR120-induced signaling cascade in splenic macrophages to promote chemotherapy resistance.Increased glucose metabolism and glycerolipid formation by fatty acids and GPR40 receptor signaling underlies the fatty acid potentiation of insulin secretionDocosahexaenoic acid, G protein-coupled receptors, and melanoma: is G protein-coupled receptor 40 a potential therapeutic target?Activation of GPR40 attenuates chronic inflammation induced impact on pancreatic β-cells health and function.Lipid receptors and islet function: therapeutic implications?Alteration of the glucagon axis in GPR120 (FFAR4) knockout mice: a role for GPR120 in glucagon secretion.Mercaptoacetate and fatty acids exert direct and antagonistic effects on nodose neurons via GPR40 fatty acid receptorsBacMam technology and its application to drug discovery.A potent class of GPR40 full agonists engages the enteroinsular axis to promote glucose control in rodents.Viral-mediated gene delivery for cell-based assays in drug discovery.Linoleic acid stimulates [Ca2+]i increase in rat pancreatic beta-cells through both membrane receptor- and intracellular metabolite-mediated pathways.Treatment with CNX-011-67, a novel GPR40 agonist, delays onset and progression of diabetes and improves beta cell preservation and function in male ZDF ratsOmega-3 fatty acids and other FFA4 agonists inhibit growth factor signaling in human prostate cancer cells.GPR40 (FFAR1) - Combined Gs and Gq signaling in vitro is associated with robust incretin secretagogue action ex vivo and in vivoHypothalamic GPR40 signaling activated by free long chain fatty acids suppresses CFA-induced inflammatory chronic pain.Attenuation of inflammatory and neuropathic pain behaviors in mice through activation of free fatty acid receptor GPR40.Differential Gene Expression in GPR40-Overexpressing Pancreatic β-cells Treated with Linoleic Acid.CNX-011-67, a novel GPR40 agonist, enhances glucose responsiveness, insulin secretion and islet insulin content in n-STZ rats and in islets from type 2 diabetic patients.GPR40/FFA1 and neutral sphingomyelinase are involved in palmitate-boosted inflammatory response of microvascular endothelial cells to LPS.Functional analysis of free fatty acid receptor GPR120 in human eosinophils: implications in metabolic homeostasis.Cloning, identification and functional characterization of bovine free fatty acid receptor-1 (FFAR1/GPR40) in neutrophils.Free fatty acid receptors: structural models and elucidation of ligand binding interactions.Simvastatin Impairs Insulin Secretion by Multiple Mechanisms in MIN6 Cells.Discovery of novel FFA4 (GPR120) receptor agonists with β-arrestin2-biased characteristics.G protein-coupled receptors and insulin secretion: 119 and countingDifferential intracellular calcium influx, nitric oxide production, ICAM-1 and IL8 expression in primary bovine endothelial cells exposed to nonesterified fatty acidsEndogenously generated omega-3 fatty acids attenuate vascular inflammation and neointimal hyperplasia by interaction with free fatty acid receptor 4 in mice.Fatty acid-related modulations of membrane fluidity in cells: detection and implications.
P2860
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P2860
Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules.
description
2006 nî lūn-bûn
@nan
2006年の論文
@ja
2006年論文
@yue
2006年論文
@zh-hant
2006年論文
@zh-hk
2006年論文
@zh-mo
2006年論文
@zh-tw
2006年论文
@wuu
2006年论文
@zh
2006年论文
@zh-cn
name
Pharmacological regulation of ...... nd antagonist small molecules.
@en
type
label
Pharmacological regulation of ...... nd antagonist small molecules.
@en
prefLabel
Pharmacological regulation of ...... nd antagonist small molecules.
@en
P2093
P2860
P356
P1476
Pharmacological regulation of ...... nd antagonist small molecules.
@en
P2093
Aaron S Goetz
Andrew J Peat
Carina Ammala
Celia P Briscoe
David C McCoy
David F Corbett
Diane M Ignar
James A Fornwald
John L Andrews
Stephen C McKeown
P2860
P304
P356
10.1038/SJ.BJP.0706770
P407
P577
2006-05-15T00:00:00Z