G-protein-coupled receptor oligomerization and its potential for drug discovery

被引：496

作者：

George, SR

O'Dowd, BF

Lee, SR

机构：

[1] Univ Toronto, Dept Pharmacol, Toronto, ON M5S 1A8, Canada

[2] Univ Toronto, Dept Med, Toronto, ON M5S 1A8, Canada

[3] Ctr Addict & Mental Hlth, Toronto, ON M5T 1A8, Canada

来源：

NATURE REVIEWS DRUG DISCOVERY | 2002年 / 1卷 / 10期

基金：

加拿大健康研究院;

关键词：

D O I：

10.1038/nrd913

中图分类号：

Q81 [生物工程学（生物技术）]; Q93 [微生物学];

学科分类号：

071005 ; 0836 ; 090102 ; 100705 ;

摘要：

G-protein-coupled receptors (GPCRs) represent by far the largest class of targets for modern drugs. Virtually all therapeutics that are directed towards GPCRs have been designed using assays that presume that these receptors are monomeric. The recent realization that these receptors form homo-oligomeric and hetero-oligomeric complexes has added a new dimension to rational drug design. However, this important aspect of GPCR biology remains largely unincorporated into schemes to search for new therapeutics. This review provides a synopsis of the current thinking surrounding GPCR homo-oligomerization and hetero-oligomerization and shows how new models point towards unexplored avenues in the development of new therapies.

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收藏

页码：808 / 820

页数：13

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