›› 2013, Vol. 33 ›› Issue (2): 225-.doi: 10.3969/j.issn.1674-8115.2013.02.020

• 综述 • 上一篇    下一篇

GPER:雌激素相关疾病治疗的新靶点

王 洁1,2, 阿吉艾克拜尔·艾萨2, 马海蓉2, 王振华1   

  1. 1.石河子大学药学院 新疆特种植物药资源教育部重点实验室, 石河子 832002; 2.中国科学院 新疆理化技术研究所干旱地区植物资源化学重点实验室, 乌鲁木齐 830011
  • 出版日期:2013-02-28 发布日期:2013-03-07
  • 通讯作者: 马海蓉, 电子信箱: mahr@ms.xjb.ac.cn; 王振华, 电子信箱: zhenhuawang@tom.com。
  • 作者简介:王 洁(1987—), 女, 硕士生; 电子信箱: wodepencil@sina.com
  • 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

WANG Jie1,2, Haji Akber AISA2, MA Hai-rong2, WANG Zhen-hua1   

  1. 1.Key Laboratory of Xinjiang Endemic Phytomedicine Resources, College of Pharmacy, Shihezi University, Shihezi 832002, China; 2.Key Laboratory of Plant Resources and Natural Products Chemistry of Arid Zone, Xinjiang Technical Institute of Physics and Chemistry, Chinese Academy of Sciences, Urumqi 830011, China
  • Online:2013-02-28 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

摘要:

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

Abstract:

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