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多功能雌激素受体α F结构域。

The multifunctional estrogen receptor-alpha F domain.

作者信息

Skafar Debra F, Zhao Changqing

机构信息

Department of Physiology, Wayne State University School of Medicine, 540 E. Canfield, Detroit, MI, 48201, USA.

出版信息

Endocrine. 2008 Feb;33(1):1-8. doi: 10.1007/s12020-008-9054-1. Epub 2008 Mar 25.

Abstract

The members of the nuclear receptor superfamily act as transcriptional regulatory factors and exhibit a multidomain structure characterized as domains A-E/F. This review focuses on a small, relatively understudied region at the extreme carboxy-terminus of the estrogen receptor (ER) alpha, the F domain. The F domain contributes to differences in the activity of ER alpha and beta subtypes; it is required for tamoxifen's agonist activity on an estrogen response element, and it modifies the receptor's interactions with coregulators including steroid receptor coactivator-1. The differences between the F domains of the ER alpha and beta subtypes and among the other members of the nuclear hormone receptor superfamily may offer opportunities for selective control of the activity of these proteins.

摘要

核受体超家族成员作为转录调节因子,呈现出具有A - E/F结构域特征的多结构域结构。本综述聚焦于雌激素受体(ER)α极端羧基末端一个相对研究较少的小区域,即F结构域。F结构域导致ERα和β亚型在活性上存在差异;它是他莫昔芬对雌激素反应元件产生激动剂活性所必需的,并且它会改变受体与包括类固醇受体共激活因子-1在内的共调节因子之间的相互作用。ERα和β亚型的F结构域之间以及核激素受体超家族其他成员之间的差异,可能为选择性控制这些蛋白质的活性提供机会。

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