The fatty acid receptor FFA1/GPR40 a decade later: how much do we know?

被引：129

作者：

Mancini, Arturo D.

Poitout, Vincent ^{[1
]}

机构：

[1] Ctr Hosp Univ Montreal CRCHUM, Ctr Rech, Montreal Diabet Res Ctr, Montreal, PQ, Canada

来源：

TRENDS IN ENDOCRINOLOGY AND METABOLISM | 2013年 / 24卷 / 08期

基金：

加拿大健康研究院;

关键词：

GPR40/FFA1; type; 2; diabetes; pancreatic beta cell; insulin secretion; biased agonism; STIMULATED INSULIN-SECRETION; PANCREATIC BETA-CELLS; BIOAVAILABLE GPR40 AGONIST; PROTEIN-KINASE D1; GLUCAGON-SECRETION; DOUBLE-BLIND; IN-VIVO; GENE-EXPRESSION; LINOLEIC-ACID; ISOLATED RAT;

D O I：

10.1016/j.tem.2013.03.003

中图分类号：

R5 [内科学];

学科分类号：

1002 ; 100201 ;

摘要：

Glucose homeostasis requires the highly coordinated regulation of insulin secretion by pancreatic beta cells. This is primarily mediated by glucose itself, but other nutrients, including free fatty acids (FFAs), potentiate the insulinotropic capacity of glucose. A decade ago, the seven-transmembrane domain receptor (7TMR) GPR40 was demonstrated to be predominantly expressed in beta cells and activated by long-chain FFAs. This discovery added a new dimension to our understanding of FFA-mediated control of glucose homeostasis. Furthermore, GPR40 has drawn considerable interest as a novel therapeutic target to enhance insulin secretion in type 2 diabetes. However, our understanding of the biology of GPR40 remains incomplete and its physiological role controversial. Here we summarize the current state of knowledge and emerging concepts regarding the role of GPR40 in regulating glucose homeostasis.

引用

页码：398 / 407

页数：10

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