Department of Microbiology, University of Virginia, Charlottesville, Virginia, USA.
Mol Cell Endocrinol. 2012 Apr 16;352(1-2):70-8. doi: 10.1016/j.mce.2011.07.004. Epub 2011 Jul 24.
Regulation of the androgen receptor (AR) by its cognate ligand is well established, but how post-translational modification modulates AR activity is only emerging. The AR is subject to modification by phosphorylation, acetylation, methylation, SUMOylation, and ubiquitination. As several of the enzymes that modify the AR are altered in prostate cancer, defining the context and physiological effects of these modifications could provide insight into mechanisms that underpin human disease. Here, we review how post-translational modification contributes to AR function as a transcription factor with particular emphasis on phosphorylation and dephosphorylation mechanisms.
雄激素受体(AR)与其同源配体的调节作用已得到充分证实,但翻译后修饰如何调节 AR 活性尚在研究之中。AR 可发生磷酸化、乙酰化、甲基化、SUMO 化和泛素化等翻译后修饰。由于几种修饰 AR 的酶在前列腺癌中发生了改变,因此确定这些修饰的作用背景和生理效应可以深入了解支持人类疾病的机制。在这里,我们回顾了翻译后修饰如何作为转录因子促进 AR 功能,特别强调了磷酸化和去磷酸化机制。