Regulation of estrogen receptor beta activity and implications in health and disease

Abstract

Together with the estrogen receptor (ER) alpha, estrogen receptor beta (ERbeta) mediates many of the physiological effects of estrogens. As ERbeta is crucially involved in a variety of important physiological processes, its activity should be tightly regulated. ERbeta regulation is achieved by hormone binding as well as by posttranslational modifications of the receptor. Furthermore, ERbeta expression levels are under circadian control and can be regulated by DNA methylation of the ERbeta promoter region. There are also a number of factors that can interfere with ERbeta activity, such as phytoestrogens, endocrine disruptive chemicals, and growth factors. In this article, we outline different mechanisms of ERbeta regulation and how they are implicated in various diseases. We also discuss how these insights might help to specifically target ERbeta in drug design. 2009 Birkhauser Verlag, Basel/Switzerland.