药学学报, 2015, 50(6): 658-667
引用本文:
蔡金亚, 李俊豪, 丁石荟, 张娟, 刘桂霞, 李卫华, 唐赟. 雌激素受体β选择性配体的研究进展[J]. 药学学报, 2015, 50(6): 658-667.
CAI Jin-ya, LI Jun-hao, DING Shi-hui, ZHANG Juan, LIU Gui-xia, LI Wei-hua, TANG Yun. Progress in study of selective ERβ ligands[J]. Acta Pharmaceutica Sinica, 2015, 50(6): 658-667.

雌激素受体β选择性配体的研究进展
蔡金亚, 李俊豪, 丁石荟, 张娟, 刘桂霞, 李卫华, 唐赟
华东理工大学药学院, 上海市新药设计重点实验室, 上海 200237
摘要:
雌激素受体 (estrogen receptors, ERs) 属于核受体家族, 与癌症、炎症、骨质疏松等多种疾病密切相关.雌激素受体有αβ两种亚型, 在人体内有不同的功能和组织分布.选择性靶向ERβ的配体能调节相关受体功能且避免作用于ERα引起的不良反应, 因而近年来成为研究的热点.本文主要综述了近年来报道的不同类型的ERβ选择性配体及其构效关系分析的研究进展.
关键词:    雌激素受体β      选择性      配体      构效关系     
Progress in study of selective ERβ ligands
CAI Jin-ya, LI Jun-hao, DING Shi-hui, ZHANG Juan, LIU Gui-xia, LI Wei-hua, TANG Yun
Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China
Abstract:
Estrogen receptors (ERs) are members of nuclear receptors and related to several diseases such as cancer, inflammation and osteoporosis. ERs have two forms, ERα and ERβ, which have different functions and organism distributions. Compounds selectively targeting ERβ can regulate important physiological functions and avoid the side effects caused by targeting ERα. Therefore, selective ERβ ligands have received considerable research interest in recent years. In this article, different kinds of selective ERβ ligands were summarized and their structure-activity relationships were also analyzed.
Key words:    estrogen receptor β    selectivity    ligand    structure-activity relationship   
收稿日期: 2014-12-23
基金项目: 国家自然科学基金资助项目 (21072059); 教育部基本科研业务费资助项目 (WY1113007).
通讯作者: 唐赟
Email: ytang234@ecust.edu.cn
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