《生命科学》 2006, 18(5):

一个潜在的糖尿病新靶标 ——GPR40

龚　珍，贺凌燕，柳　红，刘景根，朱维良^*，陈凯先，蒋华良

中国科学院上海生命科学研究院上海药物研究所药物发现与设计中心，上海201203

摘　要：摘　要：G蛋白偶联受体40(GPR40)是典型的七次跨膜受体，在游离脂肪酸的刺激下，它能起到放大葡萄糖刺激的胰岛素分泌效应，是一种潜在的治疗糖尿病药物的靶标。另外，GPR40还被认为和一些神经类疾病以及某些癌症有关。本文着重叙述了游离脂肪酸经由GPR40放大葡萄糖刺激的胰岛素分泌机制，同时也介绍了GPR40的其他一些生理功能。
关键词：糖尿病；胰岛素；GPR40；自由脂肪酸

GPR40 --a potential target for diebete mellitus

GONG Zhen, HE Ling-Yan, LIU Hong, LIU Jing-Gen, ZHU Wei-Liang^*, CHEN Kai-Xian, JIANG Hua-Liang

Drug Discovery and Design Centre, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China

Abstract: Abstract: GTP-binding protein coupling receptor 40(GPR40), which belongs to GPCR superfamily with seven transmembrane spanning helical bundles, is a potential drug target for diabetes mellitus. It was found that the receptor can amplify the glucose stimulated insulin secretion (GSIS) by free fatty acid (FFA), and is related to some neural diseases and cancers. Agonists and antagonists of GPR40 are under research with the aim to develop new drugs. In the present article, a proceeding of the recent researches on GPR40 has been reviewed, especially about the molecular mechanism of FFA amplifying GSIS. Furthermore, some other physiological functions of GPR40 have also been discussed.
Key words: diabetes; insulin; GPR40; free fatty acid