SERMs: how do they work?

Abstract

characterisation of distinct ER subtypes. Most notable is the identification of the ER-alpha and ER-beta subtypes, but additional ER species, as well as receptor mechanisms via non-classical pathways, have been suggested by recent work. Dimerisation of the ER, an essential element of the ‘classical’ ER action pathway, has recently been shown to occur not only with ERalpha and ER-beta homodimers, but also with heterodimers involving both receptor subtypes. The distribution through various body tissues of ER subtypes adds an additional layer of complexity to the situation. A level of complexity that is just beginning to emerge involves ER regulatory proteins. Classical ER action involves a number of cellular regulatory proteins, many of which bind to ER complexes. Alterations of ER conformation lead to alterations of such interactions. This pathway clearly contributes to alterations in ER mechanistic pathways, in ways that have thus far been characterised in only a few instances.