Estrogen-Receptor Expression and Function in Female Reproductive Disease

Abstract

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.

Fenton Reaction-Induced Oxidative Damage to Membrane Lipids and Protective Effects of 17β-Estradiol in Porcine Ovary and Thyroid Homogenates

“…It is known that high levels of 17β-estradiol are associated with a higher risk of estrogen-dependent cancer, such as breast and endometrial cancer [ 31 , 32 ]. In agreement with that, exogenous estrogens can increase oxidative damage in different tissues under experimental conditions [ 15 , 33 ], and even induce polycystic ovary syndrome [ 34 ].…”

Oestrogenic Endocrine Disruptors in the Placenta and the Fetus

“…Phytoestrogens are a plant component with biological activity similar to animal estrogen, with a wide range of effects on hormone-related diseases, and they exert a weak estrogen-like effect by binding to the ER with low affinity. ERs are present in different tissues, including the reproductive tract, bones, placenta, and mammary gland, suggesting that phytoestrogens may play a tissue-specific hormonal role [116,117]. ERα is perceived to promote cell growth, whereas ERβ does the opposite, mainly promoting apoptosis [118].…”

The oxytocin receptor signalling system and breast cancer: a critical review

“…OTR also interacts with other proteins, some of which are highly relevant and dysregulated in breast cancer, such as the oestrogen receptors (ERs), which are present in approximately 75% of all breast cancer cases. ERs include two subtypes, ERα and ERβ, encoded by ESR1 and ESR2, respectively, which can function at the membrane or within the nucleus [128]. ERα is the most studied subtype due to its clinical significance, while the clinical relevance of ERβ remains obscure [129].…”