Department of Biosciences and Nutrition, Karolinska Institute, Hälsovägen 7, 141 57 Huddinge, Sweden.
Cell Mol Life Sci. 2009 Dec;66(24):3873-94. doi: 10.1007/s00018-009-0118-z.
Together with the estrogen receptor (ER) alpha, estrogen receptor beta (ER beta ) mediates many of the physiological effects of estrogens. As ER beta is crucially involved in a variety of important physiological processes, its activity should be tightly regulated. ER beta regulation is achieved by hormone binding as well as by posttranslational modifications of the receptor. Furthermore, ER beta expression levels are under circadian control and can be regulated by DNA methylation of the ER beta promoter region. There are also a number of factors that can interfere with ER beta activity, such as phytoestrogens, endocrine disruptive chemicals, and growth factors. In this article, we outline different mechanisms of ER beta regulation and how they are implicated in various diseases. We also discuss how these insights might help to specifically target ER beta in drug design.
与雌激素受体 (ER) alpha 一起，雌激素受体 beta (ER beta) 介导雌激素的许多生理作用。由于 ER beta 对于各种重要的生理过程至关重要，因此其活性应该受到严格调节。ER beta 的调节是通过激素结合以及受体的翻译后修饰来实现的。此外，ER beta 的表达水平受昼夜节律控制，并可通过 ER beta 启动子区域的 DNA 甲基化来调节。还有许多因素可以干扰 ER beta 的活性，例如植物雌激素、内分泌干扰化学物质和生长因子。在本文中，我们概述了 ER beta 调节的不同机制，以及它们如何与各种疾病相关。我们还讨论了这些见解如何帮助在药物设计中专门针对 ER beta。
