GPER:雌激素相关疾病治疗的新靶点
网络出版日期: 2013-03-07
基金资助
国家自然科学基金(81102890);国家自然科学基金杰出青年学者基金 (30925045);教育部新世纪优秀人才支持计划 (NCET-10-0967)
GPER: a novel target in treatment of estrogen-related diseases
Online published: 2013-03-07
Supported by
National Natural Science Foundation of China, 81102890, 30925045;Foundation of the Ministry of Education of China, NCET-10-0967
G蛋白耦联雌激素受体 (GPER)是一种G蛋白偶联受体家族的新型雌激素受体,可与雌二醇等雌激素结合,但其信号途径及作用机制与经典核雌激素受体(ERα和ERβ)不同,是一种既能够介导非基因型快速反应也可通过第二信使系统发挥间接转录调控作用的膜性受体。由于GPER可能与雌激素相关疾病的发生、发展密切相关,很可能成为治疗相关疾病的新靶点,近年来备受关注。本文就GPER的发现、结构、亚细胞定位、配体、信号转导途径及与相关疾病之间的关系等方面进行阐述。
关键词: G蛋白偶联雌激素受体; 基因表达; 肿瘤
王 洁, 阿吉艾克拜尔·艾萨, 马海蓉, 等 . GPER:雌激素相关疾病治疗的新靶点[J]. 上海交通大学学报(医学版), 2013 , 33(2) : 225 . DOI: 10.3969/j.issn.1674-8115.2013.02.020
G protein-coupled estrogen receptor 1 (GPER) is a novel receptor, which belongs to the family of G protein-coupled receptors, to many of the rapid biological responses to estrogen. Different from the two classical nuclear estrogen receptors, ERα and ERβ, GPER modulates both rapid non-genomic reaction and genomic transcriptional events of estrogen. In this regard, GPER may be considered as a valuable target toward novel therapeutic strategy for many estrogen-related diseases. The intrinsic appearance of GPER, including structure, subcellular localization, ligands, signal transduction pathway and relationship with diseases is reviewed in this paper.
Key words: G protein-coupled estrogen receptor 1; gene expression; cancer
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