An Sheng-Jun, Zhang Yong-Xiang
Institute of Pharmacology and Toxicology, Academy of Military Medical Sciences, Beijing 100850.
Sheng Li Ke Xue Jin Zhan. 2002 Oct;33(4):309-12.
This review introduces the structure, functions, tissue distribution, physiologic roles of estrogen receptor subtypes (ER alpha and ER beta) along with transcriptional activities of estrogen receptor ligands and the mechanism of the modulatory pathway and tissue specific property of selective estrogen receptor modulators (SERMs), and phytoestrogens. This article is to provide a systemic approach for increasing the selectivity of estrogenic drug and optimizing the clinically based strategy of drug design. Differences exist between ER alpha and ER beta in structure, function, tissue distribution, physiologic roles and response to ligands, as well as the regulating effect on gene transcription, which are mainly determined by different co-regulators they recruit respectively.
本综述介绍了雌激素受体亚型（雌激素受体α和雌激素受体β）的结构、功能、组织分布、生理作用，以及雌激素受体配体的转录活性、选择性雌激素受体调节剂（SERM）和植物雌激素的调节途径机制及组织特异性特性。本文旨在提供一种系统性方法，以提高雌激素类药物的选择性，并优化基于临床的药物设计策略。雌激素受体α和雌激素受体β在结构、功能、组织分布、生理作用、对配体的反应以及对基因转录的调节作用等方面存在差异，这些差异主要由它们各自招募的不同共调节因子所决定。
