雌激素膜性受体GPR30/GPER的研究现状

Research Progress of Membranous Estrogen Receptor GPR30/GPER

雌激素对女性生理变化或病理改变都起到重大的作用。传统理论认为,雌激素通过经典受体ERα/β调控转录反应或介导细胞信号转导。G蛋白耦联受体30(GPR30),又称G蛋白耦联雌激素受体(GPER),是一种新型的雌激素受体,能与雌激素或其衍生物、拮抗剂特异性结合并发挥生物学效应。近期发现在恶性肿瘤,如乳腺癌、子宫内膜癌、卵巢癌中有GPR30过表达。研究GPR30与恶性肿瘤发生发展的关系,以期在雌激素相关疾病尤其是肿瘤中寻找新的治疗靶点。

Estrogen,as the most important sexual hormone of female,plays a significant role in women＇s physiological functions or pathologic status changing procedure.Traditional theory holds that estrogen regulates transcription reaction or mediates signal transduction through the classical estrogen receptor ER α/β.GPR30 （also known as GPER） is a novel estrogen receptor,which has the ability to specially bind with estrogen or its derivatives,antagonists,and then leads to biological effect.Recently,in malignant tumors such as breast carcinoma,endometrial carcinoma or ovarian carcinoma,there were found over-expression of GPR30.Scholars studied the relationship between GPR30 and the occurrence and development of malignant tumors,in order to search for novel therapeutic targets in estrogen-related diseases,especially cancers.