free fatty acid receptor 1 ; Rattus norvegicus






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1 15914509 Oleic acid interacts with GPR40 to induce Ca2+ signaling in rat islet beta-cells: mediation by PLC and L-type Ca2+ channel and link to insulin release. Am J Physiol Endocrinol Metab 2005 Oct 4
2 16214394 GPR40, a free fatty acid receptor on pancreatic beta cells, regulates insulin secretion. Hepatol Res 2005 Oct 1
3 16254037 Reduction in voltage-gated K+ currents in primary cultured rat pancreatic beta-cells by linoleic acids. Endocrinology 2006 Feb 2
4 17101212 Free fatty acids increase cytosolic free calcium and stimulate insulin secretion from beta-cells through activation of GPR40. Mol Cell Endocrinol 2007 Jan 15 5
5 17240142 Solid phase synthesis and SAR of small molecule agonists for the GPR40 receptor. Bioorg Med Chem Lett 2007 Mar 15 1
6 18477808 Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice. Diabetes 2008 Aug 2
7 19217448 Acute administration of GPR40 receptor agonist potentiates glucose-stimulated insulin secretion in vivo in the rat. Metabolism 2009 Mar 8
8 19346127 Synthesis and SAR of 1,2,3,4-tetrahydroisoquinolin-1-ones as novel G-protein-coupled receptor 40 (GPR40) antagonists. Bioorg Med Chem Lett 2009 May 1 4
9 19815053 Sulfonylureas uncouple glucose-dependence for GPR40-mediated enhancement of insulin secretion from INS-1E cells. Mol Cell Endocrinol 2010 Feb 5 6
10 20211608 DHA promotes the neuronal differentiation of rat neural stem cells transfected with GPR40 gene. Brain Res 2010 May 12 7
11 20888730 DC260126, a small-molecule antagonist of GPR40, improves insulin tolerance but not glucose tolerance in obese Zucker rats. Biomed Pharmacother 2010 Nov 3
12 21319751 Design, synthesis, and biological activity of potent and orally available G protein-coupled receptor 40 agonists. J Med Chem 2011 Mar 10 8
13 21339298 Conjugated linoleic acids mediate insulin release through islet G protein-coupled receptor FFA1/GPR40. J Biol Chem 2011 Apr 8 1
14 21565851 Acute stimulation of glucagon secretion by linoleic acid results from GPR40 activation and [Ca2+]i increase in pancreatic islet {alpha}-cells. J Endocrinol 2011 Aug 2
15 21752941 TAK-875, an orally available G protein-coupled receptor 40/free fatty acid receptor 1 agonist, enhances glucose-dependent insulin secretion and improves both postprandial and fasting hyperglycemia in type 2 diabetic rats. J Pharmacol Exp Ther 2011 Oct 1
16 22087278 AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One 2011 3
17 22242551 Identification of fused-ring alkanoic acids with improved pharmacokinetic profiles that act as G protein-coupled receptor 40/free fatty acid receptor 1 agonists. J Med Chem 2012 Feb 23 4
18 22332921 Long-term in vitro treatment of INS-1 rat pancreatic β-cells by unsaturated free fatty acids protects cells against gluco- and lipotoxicities via activation of GPR40 receptors. Clin Exp Pharmacol Physiol 2012 May 7
19 22734209 Linoleic acid activates GPR40/FFA1 and phospholipase C to increase [Ca2+]i release and insulin secretion in islet beta-cells. Chin Med Sci J 2012 Mar 2
20 23372643 PPAR-γ activation increases insulin secretion through the up-regulation of the free fatty acid receptor GPR40 in pancreatic β-cells. PLoS One 2013 1
21 23520164 Fatty acid receptor Gpr40 mediates neuromicrovascular degeneration induced by transarachidonic acids in rodents. Arterioscler Thromb Vasc Biol 2013 May 3
22 23628491 GW9508 inhibits insulin secretion by activating ATP-sensitive potassium channels in rat pancreatic β-cells. J Mol Endocrinol 2013 2
23 23817296 Evidence for the involvement of GPR40 and NADPH oxidase in palmitic acid-induced superoxide production and insulin secretion. Islets 2013 Jul-Aug 13
24 23848179 TAK-875, a GPR40/FFAR1 agonist, in combination with metformin prevents progression of diabetes and β-cell dysfunction in Zucker diabetic fatty rats. Br J Pharmacol 2013 Oct 2
25 23911664 GPR40 protein levels are crucial to the regulation of stimulated hormone secretion in pancreatic islets. Lessons from spontaneous obesity-prone and non-obese type 2 diabetes in rats. Mol Cell Endocrinol 2013 Dec 5 8
26 24666736 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. BMC Pharmacol Toxicol 2014 Mar 25 6
27 24675078 Increased glucose metabolism and glycerolipid formation by fatty acids and GPR40 receptor signaling underlies the fatty acid potentiation of insulin secretion. J Biol Chem 2014 May 9 12
28 24760994 Mercaptoacetate and fatty acids exert direct and antagonistic effects on nodose neurons via GPR40 fatty acid receptors. Am J Physiol Regul Integr Comp Physiol 2014 Jul 1 7
29 24835985 Discovery of 3-aryl-3-ethoxypropanoic acids as orally active GPR40 agonists. Bioorg Med Chem Lett 2014 Jul 1 5
30 24900210 Discovery of TAK-875: A Potent, Selective, and Orally Bioavailable GPR40 Agonist. ACS Med Chem Lett 2010 Sep 9 2
31 24974801 Activation of GPR40 attenuates chronic inflammation induced impact on pancreatic β-cells health and function. BMC Cell Biol 2014 Jun 30 2
32 25092426 Activation of G-protein-coupled receptor 40 attenuates the cisplatin-induced apoptosis of human renal proximal tubule epithelial cells. Int J Mol Med 2014 Oct 2
33 25446111 Opposite effects of GPR120 and GPR40 on cell motile activity induced by ethionine in liver epithelial cells. Biochem Biophys Res Commun 2015 Jan 2 6
34 25701750 Insulinotropic effect of Chikusetsu saponin IVa in diabetic rats and pancreatic β-cells. J Ethnopharmacol 2015 Apr 22 6
35 25729276 Differential Gene Expression in GPR40-Overexpressing Pancreatic β-cells Treated with Linoleic Acid. Korean J Physiol Pharmacol 2015 Mar 10
36 25792236 Activation of extracellular signal-regulated protein kinases 1 and 2 (ERK1/2) by free fatty acid receptor 1 (FFAR1/GPR40) protects from palmitate-induced beta cell death, but plays no role in insulin secretion. Cell Physiol Biochem 2015 10
37 25815144 Discovery of DS-1558: A Potent and Orally Bioavailable GPR40 Agonist. ACS Med Chem Lett 2015 Mar 12 3
38 25925080 H₂O₂-Activated Mitochondrial Phospholipase iPLA₂γ Prevents Lipotoxic Oxidative Stress in Synergy with UCP2, Amplifies Signaling via G-Protein-Coupled Receptor GPR40, and Regulates Insulin Secretion in Pancreatic β-Cells. Antioxid Redox Signal 2015 Oct 20 4
39 26234904 Optimization of 3-aryl-3-ethoxypropanoic acids and discovery of the potent GPR40 agonist DS-1558. Bioorg Med Chem 2015 Sep 1 2
40 26381015 Vascular, but not luminal, activation of FFAR1 (GPR40) stimulates GLP-1 secretion from isolated perfused rat small intestine. Physiol Rep 2015 Sep 2
41 26417688 Yhhu4488, a novel GPR40 agonist, promotes GLP-1 secretion and exerts anti-diabetic effect in rodent models. Biochem Biophys Res Commun 2015 Oct 30 7
42 26791830 Mercaptoacetate blocks fatty acid-induced GLP-1 secretion in male rats by directly antagonizing GPR40 fatty acid receptors. Am J Physiol Regul Integr Comp Physiol 2016 Apr 15 2
43 26813930 Fasiglifam/TAK-875, a Selective GPR40 Agonist, Improves Hyperglycemia in Rats Unresponsive to Sulfonylureas and Acts Additively with Sulfonylureas. J Pharmacol Exp Ther 2016 Apr 1
44 26968637 Diverse effects of G-protein-coupled free fatty acid receptors on the regulation of cellular functions in lung cancer cells. Exp Cell Res 2016 Mar 15 2
45 27990751 Curcumin improves glucose tolerance via stimulation of glucagon-like peptide-1 secretion. Mol Nutr Food Res 2017 Mar 2
46 27994752 Identification of an Orally Efficacious GPR40/FFAR1 Receptor Agonist. ACS Med Chem Lett 2016 Dec 8 7
47 28197316 Design and Synthesis of Novel, Selective GPR40 AgoPAMs. ACS Med Chem Lett 2017 Feb 9 2
48 28206647 Fasiglifam (TAK-875): Mechanistic Investigation and Retrospective Identification of Hazards for Drug Induced Liver Injury. Toxicol Sci 2018 Jun 1 1
49 28542610 GPR40 partial agonist MK-2305 lower fasting glucose in the Goto Kakizaki rat via suppression of endogenous glucose production. PLoS One 2017 4
50 28583918 GPR120 suppresses adipose tissue lipolysis and synergizes with GPR40 in antidiabetic efficacy. J Lipid Res 2017 Aug 3