The ins and outs of GPR30: A transmembrane estrogen receptor
The ins and outs of GPR30: A transmembrane estrogen receptor
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DOI：
10.1016/j.jsbmb.2008.03.006
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发表时间：
2008-04-01
影响因子：
4.1
通讯作者：
Arterburn, Jeffrey B.
中科院分区：
文献类型：
--
作者：
Prossnitz, Eric R.;Oprea, Tudor I.;Arterburn, Jeffrey B.
雌激素是人类生理学中一种重要的激素。它既通过转录调节起作用，也通过第二信使对细胞内信号传导进行调节而起作用。尽管雌激素的转录效应是通过经典的核类固醇受体（ERs）产生的，但近期研究揭示存在一种新型的7次跨膜G蛋白偶联受体GPR30，它对雌激素和他莫昔芬的刺激有反应，能产生快速的细胞信号传导，包括细胞外调节蛋白激酶（ERK）激活、磷脂酰肌醇 - 3 - 激酶（PI3K）激活、钙动员以及环磷腺苷酸（cAMP）生成。为了区分由ER和GPR30介导的信号传导，我们已经确定了一种对GPR30具有高度特异性的新型GPR30激动剂。在这篇综述中，我们将描述近期的研究工作，以进一步加深我们对GPR30在雌激素生物学中作用的理解。（C）2008爱思唯尔有限公司。保留所有权利。
Estrogen is an important hormone in human physiology. It acts both via transcriptional regulation as well as via modulation of intracellular signaling through second messengers. Although estrogen's transcriptional effects occur through classical nuclear steroid receptors (ERs) recent studies reveal the existence of, a novel 7-transmembrane G protein-coupled receptor, GPR30, which responds to estrogen and tamoxifen stimulation with rapid cellular signaling including ERK activation, PI3K activation, calcium mobilization and cAMP production. To distinguish between ER- and GPR30-mediated signaling, we have identified a novel GPR30 agonist that exhibits high specificity for GPR30. In this review, we will describe recent work to further our understanding of the role of GPR30 in estrogen biology. (C) 2008 Elsevier Ltd. All rights reserved.