雌激素受体GPR30研究进展

Advances on novel estrogen receptor GPR30

G蛋白偶联受体30(G protein-coupled receptor 30,GPR30)是上世纪90年代发现的一种膜相关雌激素受体(estrogen receptor,ER),其作用模式和效应与传统核受体ERα、β均有不同,且与二者并没有同源性,是又一种具有独立作用的新型ER。GPR30广泛表达于全身多个系统及多种肿瘤细胞,主要定位于内质网,通过转活表皮生长因子受体(epidermal growth factor receptor,EGFR)及第二信使等介导雌激素样物质快速反应和转录调节,参与多种疾病及肿瘤生物学过程,可能与ERα具有协同作用,在乳腺癌等重大疾病的治疗中具有较好的应用前景。

G protein-coupled receptor 30 （GPR30） was a novel estrogen receptor identified as membrane associated receptor in the late 1990s. This new member of estrogen receptors was independent of the classic nuclear estrogen receptor α and β due to the low homology and significant difference between them. It was reported that GPR30 localized endoplasmic reticulum predominantly, which was expressed in diverse cancer cells and a wide range of systems throughout the body. The rapid non-genetic response, partially at least, transcription regulation of estrogenic effects were mediated by the novel receptor via transactivation of epidermal growth factor receptor and modulation of second messengers such as cyclic adenosine monophosphate （cAMP） and Ca^2＋. These pathways, possibly coordinate with ERα, were involved in various physiological, physiopathological and carcinogenesis process. Theoretically, GPR30 would be a novel therapeutic target in estrogen-related diseases such as breast carcinoma.