Signaling property study of adhesion G-protein-coupled receptors

被引：84

作者：

Gupte, Jamila ^{[1
]}

Swaminath, Gayathri ^{[1
]}

Danao, Jay ^{[1
]}

Tian, Hui ^{[1
]}

Li, Yang ^{[1
]}

Wu, Xinle ^{[1
]}

机构：

[1] Amgen Inc, San Francisco, CA 94080 USA

来源：

FEBS LETTERS | 2012年 / 586卷 / 08期

关键词：

Adhesion; G-protein-coupled receptor; GPR97; CD97;

D O I：

10.1016/j.febslet.2012.03.014

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：

Adhesion G-protein-coupled receptors (GPCR) are special members of GPCRs with long N-termini containing multiple domains. We overexpressed our collection of receptors together with G-proteins in mammalian cell lines and measured the concentrations of intracellular signaling molecules, such as inositol phosphate and cAMP. Our results show that a subset of tested adhesion GPCRs has constitutive activities and is capable of coupling to a variety of G-proteins. In addition, we have identified a small molecule compound that specifically activates one of the subfamily members, GPR97, and the activation was confirmed by an independent GTP gamma S assay. These findings suggest classical GPCR screening assays could be applied to de-orphanize these receptors, and provide pharmacological tools to improve understanding of the physiological functions of these receptors. (C) 2012 Federation of European Biochemical Societies. Published by Elsevier B. V. All rights reserved.

引用

页码：1214 / 1219

页数：6

共 15 条

[1] The human and mouse repertoire of the adhesion family of G-protein-coupled receptors [J].