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G蛋白偶联受体寡聚化:对G蛋白激活和细胞信号传导的影响。

G protein-coupled receptor oligomerization: implications for G protein activation and cell signaling.

作者信息

Breitwieser Gerda E

机构信息

Department of Biology, Syracuse University, 122 Lyman Hall, 108 College Place, Syracuse, NY 13244, USA.

出版信息

Circ Res. 2004 Jan 9;94(1):17-27. doi: 10.1161/01.RES.0000110420.68526.19.

DOI:10.1161/01.RES.0000110420.68526.19
PMID:14715532
Abstract

The cardiovascular system is richly endowed with G protein-coupled receptors (GPCRs), members of the largest family of plasma membrane-localized receptors. During the last 10 years, it has become increasingly clear that many, if not all, GPCRs function in oligomeric complexes, as either homo- or hetero-oligomers. This review explores the mechanistic implications of GPCR dimerization and/or oligomerization on receptor activation and interactions with G proteins. The effects of GPCR oligomerization on receptor pharmacology, GPCR-mediated signaling, and potential contributions to GPCR crosstalk will be considered in the context of receptors important in the cardiovascular system. Our evolving understanding of the structural and functional consequences of GPCR oligomerization may provide novel and more selective sites for pharmacological tuning of cardiovascular function.

摘要

心血管系统富含G蛋白偶联受体(GPCRs),这是质膜定位受体中最大的家族成员。在过去十年中,越来越清楚的是,许多(如果不是全部的话)GPCRs在寡聚复合物中发挥作用,形成同型或异型寡聚体。本文综述探讨了GPCR二聚化和/或寡聚化对受体激活以及与G蛋白相互作用的机制影响。将在心血管系统中重要的受体背景下,考虑GPCR寡聚化对受体药理学、GPCR介导的信号传导以及对GPCR串扰潜在贡献的影响。我们对GPCR寡聚化的结构和功能后果不断发展的理解,可能为心血管功能的药理学调节提供新的、更具选择性的靶点。

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