雌激素受体β选择性配体的研究进展

Progress in study of selective ERβ ligands

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α和β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。

Estrogen receptors （ERs） are members of nuclear receptors and related to several diseases such as cancer, inflammation and osteoporosis. ERs have two forms, ERa 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 ERa. Therefore, selective ERfl 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.