Fatty acid receptors as new therapeutic targets for diabetes

被引：93

作者：

Rayasam, Geetha Vani ^{[1
]}

Tulasi, Vamshi Krishna ^{[1
]}

Davis, Joseph Alex ^{[1
]}

Bansal, Vinay S. ^{[1
]}

机构：

[1] Dept Pharmacol, Res & Dev, Gurgaon, Haryana, India

来源：

EXPERT OPINION ON THERAPEUTIC TARGETS | 2007年 / 11卷 / 05期

关键词：

free unesterified fatty acids; GLP-1; glucose stimulated insulin secretion; GPCR; inflammation; obesity;

D O I：

10.1517/14728222.11.5.661

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

G-protein-coupled receptors (GPCRs) are key regulators of several physiological functions. Their roles in cellular signal transduction have made them the target for majority of all currently prescribed drugs. Additionally, there are many orphan GPCRs that provide potential novel therapeutic targets. Several GPCRs are involved in metabolic regulation and glucose homeostasis such as GLP-1 receptor, glucagon receptor, adiponectin receptor and so on. Recently, free fatty acids (FFAs) have been demonstrated as ligands for orphan GPCRs and have been proposed to play a critical role in physiological glucose homeostasis. GPR40 and GPR120 are activated by medium and long-chain FFAs, whereas GPR41 and GPR43 can be activated by short-chain FFAs. GPR40, which is preferentially expressed in pancreatic beta-cells, mediates the majority of the effects of FFAs on insulin secretion. In this review, these findings and also critical analysis of these GPCRs as novel targets for diabetes are discussed.

引用

页码：661 / 671

页数：11

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