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1)Briscoe CP, Tadayyon M, Andrews JL, et al. The orphan G protein-coupled receptor GPR40 is activated by medium and long chain fatty acids. J Biol Chem. 2003; 278 : 11303-11
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2)Itoh Y, Kawamata Y, Harada M, et al. Free fatty acids regulate insulin secretion from pancreatic beta cells through GPR40. Nature. 2003; 422: 173-6
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3)Nagasumi K, Esaki R, Iwachidow K, et al. Overexpression of GPR40 in pancreatic beta-cells augments glucose-stimulated insulin secretion and improves glucose tolerance in normal and diabetic mice. Diabetes. 2009; 58 : 1067-76
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4)Alquier T, Poitout V. GPR40: good cop, bad cop? Diabetes. 2009; 58: 1035-6
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5)Edfalk S, Steneberg P, Edlund H. Gpr40 is expressed in enteroendocrine cells and mediates free fatty acid stimulation of incretin secretion. Diabetes. 2008; 57: 2280-7
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6)Briscoe CP, Peat AJ, McKeown SC, et al. Pharmacological regulation of insulin secretion in MIN6 cells through the fatty acid receptor GPR40: identification of agonist and antagonist small molecules. Br J Pharmacol. 2006; 148(5): 619-28
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7)Tan CP, Feng Y, Zhou YP, et al. Selective small-molecule agonists of G protein-coupled receptor 40 promote glucose-dependent insulin secretion and reduce blood glucose in mice. Diabetes. 2008; 57(8): 2211-9
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8)Lin DC, Zhang J, Zhuang R, et al. AMG 837: a novel GPR40/FFA1 agonist that enhances insulin secretion and lowers glucose levels in rodents. PLoS One. 2011; 6(11): e27270
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9)Bharate SB, Nemmani KVS, Vishwakarma RA. Progress in the discovery and development of small-molecule modulators of G-protein-coupled receptor 40 (GPR40/FFA1/FFAR1):an emerging target for type 2 diabetes. Expert Opin Ther Patents. 2009; 19: 237-64
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10)Negoro N, Sasaki S, Mikami S, et al. Discovery of TAK-875: a potent, selective, and orally bioavailable GPR40 agonist. ACS Med Chem Lett. 2010; 1: 290-4
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11)Tsujihata Y, Ito R, Suzuki M, et al. 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; 339: 228-37
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12)Yashiro H, Tsujihata Y, Takeuchi K, et al. The Effects of TAK-875, a selective G protein-coupled receptor 40/free fatty acid 1 agonist, on insulin and glucagon secretion in isolated rat and human islets. J Pharmacol Exp Ther. 2012; 340(2) : 483-9
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13)Flodgren E, Olde B, Meidute-Abaraviciene S, et al. GPR40 is expressed in glucagon producing cells and affects glucagon secretion. Biochem Biophys Res Commun. 2007; 354(1): 240-5
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14)Sako Y, Grill VE. A 48-hour lipid infusion in the rat time-dependently inhibits glucose-induced insulin secretion and B cell oxidation through a process likely coupled to fatty oxidation. Endocrinology. 1990; 127: 1580-9
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15)Negoro N, Sasaki S, Mikami S, et al. Optimization of (2,3-dihydro-1-benzofuran-3-yl)acetic acids: discovery of a non-free fatty acid-like, highly bioavailable G protein-coupled receptor 40/free fatty acid receptor 1 agonist as a glucose-dependent insulinotropic agent. J Med Chem. 2012; 55(8): 3960-74
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16)Ito R, Tsujihata Y, Suzuki M, et al. TAK-875, a GPR40 agonist, improves postprandial hyperglycemia additively with sulfonylurea and is effective with sulfonylurea failure. Diabetes. 2012; 60 Supple 1: 294
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17)Ito R, Tsujihata Y, Nagasumi K, et al. TAK-875, a GPR40 agonist, in combination with metformin improves glycemic control and β-cell function in Zucker diabetic fatty rats. Diabetes. 2011; 60 Supple 1: 275
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18)Araki T, Hirayama M, Hiroi S, et al. Gpr40-induced insulin secretion by novel agonist TAK-875: first clinical findings in patients with type 2 diabetes. Diabetes Obes Metab. 2012; 14(3): 271-8
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19)Burant CF, Viswanathan P, Marcinak J, et al. TAK-875 versus placebo or glimepiride in type 2 diabetes mellitus: a phase 2, randomised, double-blind, placebo-controlled trial. Lancet. 2012; 379(9824): 1403-11
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