A human cell surface receptor activated by free fatty acids and thiazolidinedione drugs

被引：307

作者：

Kotarsky, K ^{[1
]}

Nilsson, NE ^{[1
]}

Flodgren, E ^{[1
]}

Owman, C ^{[1
]}

Olde, B ^{[1
]}

机构：

[1] Wallenberg Neurosci Ctr, Div Mol Neurobiol, SE-22184 Lund, Sweden

来源：

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS | 2003年 / 301卷 / 02期

关键词：

receptor; cell surface; GPR40; fatty acid; thiazolidinediones; diabetes; obesity; arteriosclerosis; reverse pharmacology; drug evaluation; preclinical;

D O I：

10.1016/S0006-291X(02)03064-4

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Fatty acids, which are essential nutritional components, are also involved in cardiovascular and metabolic diseases. Here we report a human cell surface receptor that we name free fatty acid receptor (FFAR), because it is specifically activated by medium to long-chain free fatty acids. The receptor belongs to the class of seven-transmembrane, G-protein coupled receptors (GPCRs) and also mediates responses to antidiabetic drugs of the thiazolidinedione type. It is expressed in skeletal muscle, heart, liver, and pancreatic beta-cells. Stimulation of FFAR increases the intracellular calcium concentration in cells expressing the receptor in a native (pancreatic beta-cell line) or in a recombinant form. In view of the nature of the activating substances, their physiological role in the body, and the tissue distribution of FFAR we suggest the term "nutrient sensing receptor" for receptors acting at the interface between dietary components and signalling molecules. (C) 2003 Elsevier Science (USA). All rights reserved.

引用

页码：406 / 410

页数：5

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