Signaling property study of adhesion G-protein-coupled receptors
Signaling property study of adhesion G-protein-coupled receptors
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DOI：
10.1016/j.febslet.2012.03.014
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发表时间：
2012-04-24
期刊：
影响因子：
3.5
通讯作者：
Wu, Xinle
中科院分区：
文献类型：
--
作者：
Gupte, Jamila;Swaminath, Gayathri;Wu, Xinle
粘附G蛋白偶联受体（GPCR）是一类特殊的GPCR成员，其N端含有多个结构域。我们在哺乳动物细胞系中过表达我们收集的受体和G蛋白，并测量细胞内信号分子的浓度，如磷酸肌醇和cAMP。我们的研究结果表明，测试的粘附GPCR的子集具有组成性活动，并能够耦合到各种G蛋白。此外，我们已经鉴定了一种小分子化合物，其特异性激活亚家族成员之一GPR97，并且通过独立的GTP γ S测定证实了该激活。这些研究结果表明，经典的GPCR筛选试验可以应用于这些受体的去乙酰化，并提供药理学工具，以提高对这些受体的生理功能的理解。(C)2012年欧洲生物化学学会联合会。由Elsevier B出版。V.保留所有权利。
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.