College of Animal Science and Technology, China Agricultural University, Beijing 100193, China.
Institute of Laboratory Animal Sciences, Chinese Academy of Medical Sciences, Ministry of Health, Beijing 100021, China.
Cells. 2021 Feb 21;10(2):459. doi: 10.3390/cells10020459.
Female infertility is mainly caused by ovulation disorders, which affect female reproduction and pregnancy worldwide, with polycystic ovary syndrome (PCOS) being the most prevalent of these. PCOS is a frequent endocrine disease that is associated with abnormal function of the female sex hormone estrogen and estrogen receptors (ERs). Estrogens mediate genomic effects through ERα and ERβ in target tissues. The G-protein-coupled estrogen receptor (GPER) has recently been described as mediating the non-genomic signaling of estrogen. Changes in estrogen receptor signaling pathways affect cellular activities, such as ovulation; cell cycle phase; and cell proliferation, migration, and invasion. Over the years, some selective estrogen receptor modulators (SERMs) have made substantial strides in clinical applications for subfertility with PCOS, such as tamoxifen and clomiphene, however the role of ER in PCOS still needs to be understood. This article focuses on the recent progress in PCOS caused by the abnormal expression of estrogen and ERs in the ovaries and uterus, and the clinical application of related targeted small-molecule drugs.
女性不孕主要由排卵障碍引起，影响全球女性的生殖和妊娠，其中多囊卵巢综合征（PCOS）最为常见。PCOS 是一种常见的内分泌疾病，与女性性激素雌激素和雌激素受体（ERs）的异常功能有关。雌激素通过靶组织中的 ERα 和 ERβ 介导基因组效应。最近描述了 G 蛋白偶联雌激素受体（GPER）介导雌激素的非基因组信号。雌激素受体信号通路的变化会影响细胞活动，如排卵、细胞周期阶段和细胞增殖、迁移和侵袭。多年来，一些选择性雌激素受体调节剂（SERMs）在治疗 PCOS 引起的不孕方面取得了重大进展，如他莫昔芬和氯米酚，但 ER 在 PCOS 中的作用仍有待了解。本文重点介绍了卵巢和子宫中雌激素和 ERs 异常表达引起的 PCOS 的最新进展，以及相关靶向小分子药物的临床应用。
