Free fatty acid receptor 1 (FFAR1), also known as G-protein coupled receptor 40 (GPR40), is a rhodopsin-like G-protein coupled receptor [5] that is coded (i.e., its synthesis is directed) by the FFAR1 gene. [6] This gene is located on the short (i.e., "q") arm of chromosome 19 at position 13.12 (location notated as 19q13.12). [7]

Recently, certain novel GPR40 agonists have been identified that regulate glucose-stimulated insulin secretion, leading to the development of new drugs for the treatment of type 2 diabetes. In this review, we focus on progress in the physiological role of GPR40 and potential drugs targeting GPR40 over the past decade.

GPR40 is a class A G-protein coupled receptor (GPCR) mainly expressed in pancreas, intestine, and brain. Its endogenous ligand is long-chain fatty acids, which activate GPR40 after meal ingestion to induce secretion of incretins in the gut, including GLP-1, GIP, and PYY, the latter control appetite and glucose metabolism.

2018年4月25日 · Nature Communications - GPR40 is a G-protein coupled receptor that binds to free fatty acids, mediating insulin and incretin secretion. Here, the authors present the crystal structure of...

GPR40 is a GPCR that is highly expressed in pancreatic beta cells and involved in insulin secretion in rodents and humans. Hence, GPR40 is a potential therapeutic target in diabetes, which can lead to the development of oral drugs with fewer hypoglycemic side effects.

GPR40 (also known as FFA receptor 1) is primarily expressed in pancreatic .-cells and is activated by medium-chain and long-chain FFAs. GPR40 has been shown to augment glucose dependent insulin secretion (GDIS) from pancreatic .-cells and is widely studied drug discovery target for the treatment of type 2 diabetes mellitus (T2DM) and other ...

OBJECTIVE— The G-protein–coupled receptor GPR40 is expressed in pancreatic β-cells and is activated by long-chain fatty acids. Gene deletion studies have shown that GPR40 mediates, at least in part, fatty acid–amplification of glucose-induced insulin secretion (GSIS) but is not implicated in GSIS itself.

2014年7月20日 · Human GPR40 receptor (hGPR40), also known as free fatty-acid receptor 1 (FFAR1), is a G-protein-coupled receptor that binds long-chain free fatty acids to enhance glucose-dependent insulin...

2017年6月5日 · We report the 3.2-Å crystal structure of human GPR40 (hGPR40) in complex with both the partial agonist MK-8666 and an AgoPAM, which exposes a novel lipid-facing AgoPAM-binding pocket outside the...

摘要： G蛋白偶联受体40(G protein-coupled receptor 40, GPR40)是一种具有7个跨膜α螺旋结构的G蛋白偶联受体, 主要分布于胰腺细胞和神经系统细胞。它能与机体内游离的中长链脂肪酸结合, 激活细胞内信号通路, 从而调节其生理功能。在胰岛细胞中, GPR40可被游离脂肪酸 ...