College of Pharmaceutical Sciences, Zhejiang University, Hangzhou, Zhejiang, 310058, China.
School of Pharmaceutical Sciences, Zhengzhou University, 100 Kexue Avenue, Zhengzhou, 450001, China.
Eur J Med Chem. 2022 Nov 5;241:114658. doi: 10.1016/j.ejmech.2022.114658. Epub 2022 Aug 8.
Estrogen governs the regulations of various pathological and physiological actions throughout the body in both males and females. Generally, 17β-estradiol an endogenous estrogen is responsible for different health problems in pre and postmenopausal women. The major activities of endogenous estrogen are executed by nuclear estrogen receptors (ERs) ERα and ERβ while non-genomic cytoplasmic pathways also govern cell growth and apoptosis. Estrogen accomplished a fundamental role in the formation and progression of breast cancer. In this review, we have hyphenated different studies regarding ERs and a thorough and detailed study of estrogen receptors is presented. This review highlights different aspects of estrogens ranging from receptor types, their isoforms, structures, signaling pathways of ERα, ERβ and GPER along with their crystal structures, pathological roles of ER, ER ligands, and therapeutic strategies to overcome the resistance.
雌激素在男性和女性体内调节着各种病理和生理作用。一般来说，17β-雌二醇是一种内源性雌激素，会导致绝经前后女性出现不同的健康问题。内源性雌激素的主要作用是通过核雌激素受体（ERs）ERα和 ERβ来执行，而非基因组细胞质途径也可以控制细胞生长和凋亡。雌激素在乳腺癌的发生和发展中起着重要作用。在这篇综述中，我们结合了不同的关于 ERs 的研究，并对雌激素受体进行了全面而详细的研究。这篇综述强调了雌激素的不同方面，包括受体类型、它们的亚型、结构、ERα、ERβ 和 GPER 的信号通路，以及它们的晶体结构、ER 的病理作用、ER 配体和克服耐药性的治疗策略。
