Beijing Key Laboratory for Animal Genetic Improvement, National Engineering Laboratory for Animal Breeding, Key Laboratory of Animal Genetics and Breeding of the Ministry of Agriculture, College of Animal Science and Technology, China Agricultural University, Beijing 100193, China.
CAS Key Laboratory of Genome Sciences and Information, Beijing Institute of Genomics, Chinese Academy of Sciences, Beijing 100101, China.
Cells. 2019 Sep 21;8(10):1123. doi: 10.3390/cells8101123.
Estrogen receptors (ER) include ER alpha, ER beta and new membrane receptor G protein-coupled receptor 30 (GPR30). Estrogen receptors are key receptors to maintain ovarian granulosa cell differentiation, follicle and oocyte growth and development, and ovulation function. The abnormal functions of estrogen, its receptors, and estradiol synthesis-related enzymes are closely related to clinical reproductive endocrine diseases, such as polycystic ovary syndrome (PCOS) and endometriosis (EMS). At present, hormone therapy is the main treatment for ovarian-related diseases, and a stable hormone environment is established by regulating ovarian function. In recent years, some estrogen-related drugs have made great progress, such as clomiphene, which is a nonsteroidal antiestrogen drug in clinical application. This article elaborates on the regulatory role of estrogen and its nuclear receptors and membrane receptors in oocyte development, especially female reproductive diseases related to the abnormal expression of estrogen and its receptors. We also highlighted the latest advances of treatment strategy for these diseases and the application of related targeted small molecule drugs in clinical research and treatment, so as to provide reference for the treatment of female reproductive diseases.
雌激素受体(ER)包括 ERα、ERβ和新的膜受体 G 蛋白偶联受体 30(GPR30)。雌激素受体是维持卵巢颗粒细胞分化、卵泡和卵母细胞生长发育以及排卵功能的关键受体。雌激素、其受体和雌二醇合成相关酶的异常功能与临床生殖内分泌疾病密切相关,如多囊卵巢综合征(PCOS)和子宫内膜异位症(EMS)。目前,激素治疗是卵巢相关疾病的主要治疗方法,通过调节卵巢功能来建立稳定的激素环境。近年来,一些与雌激素相关的药物取得了很大进展,如临床上应用的非甾体类抗雌激素药物氯米酚。本文详细阐述了雌激素及其核受体和膜受体在卵母细胞发育中的调节作用,特别是与雌激素及其受体异常表达相关的女性生殖疾病。我们还强调了这些疾病治疗策略的最新进展以及相关靶向小分子药物在临床研究和治疗中的应用,为女性生殖疾病的治疗提供参考。