Regulation of G protein-coupled receptor kinases
Regulation of G protein-coupled receptor kinases
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DOI：
10.1016/s1050-1738(00)00053-0
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发表时间：
2000-02-01
影响因子：
9.3
通讯作者：
Benovic, JL
中科院分区：
文献类型：
--
作者：
Penn, RB;Pronin, AN;Benovic, JL
G蛋白偶联受体激酶(GRKs)与激动剂激活形式的G蛋白偶联受体(GPCRs)特异性地相互作用，影响受体的磷酸化和脱敏。最近的研究表明，GRK功能是一个高度调控的过程，也许正是通过这种方式，少数GRK(迄今已发现7个)能够以协调的方式调节给定细胞类型中的许多GPCR的反应性。调节GRK活性的机制可分为3类：1)亚细胞定位；2)内源性激酶活性的改变；3)GRK表达水平的改变。这篇综述将总结我们目前对这些调控过程的理解，并解释这些机制如何在不同的生理条件下影响GPCRs的调控。(《心脏医学趋势》2000；10：81-89)。(C)2000年，爱思唯尔科学公司。
G protein-coupled receptor kinases (GRKs) specifically interact with the agonist-activated form of G protein-coupled receptors (GPCRs) to effect receptor phosphorylation and desensitization. Recent studies demonstrate that GRK function is a highly regulated process, and it is perhaps in this manner that a handful of GRKs (7 have been identified to date) are able to regulate the responsiveness of numerous GPCRs in a given cell type in a coordinated manner. The mechanisms by which GRK activity is regulated can be divided into 3 categories: 1) subcellular localization; 2) alterations in intrinsic kinase activity; and 3) alterations in GRK expression levels. This review, will summarize our current understanding of each of these regulatory processes, and offer explanations as to how such mechanisms influence GPCR regulation under various physiologic conditions. (Trends Cardiovasc Med 2000; 10:81-89). (C) 2000, Elsevier Science Inc.