| Literature DB >> 23239736 |
Kexin Xu1, Zhenhua Jeremy Wu, Anna C Groner, Housheng Hansen He, Changmeng Cai, Rosina T Lis, Xiaoqiu Wu, Edward C Stack, Massimo Loda, Tao Liu, Han Xu, Laura Cato, James E Thornton, Richard I Gregory, Colm Morrissey, Robert L Vessella, Rodolfo Montironi, Cristina Magi-Galluzzi, Philip W Kantoff, Steven P Balk, X Shirley Liu, Myles Brown.
Abstract
Epigenetic regulators represent a promising new class of therapeutic targets for cancer. Enhancer of zeste homolog 2 (EZH2), a subunit of Polycomb repressive complex 2 (PRC2), silences gene expression via its histone methyltransferase activity. We found that the oncogenic function of EZH2 in cells of castration-resistant prostate cancer is independent of its role as a transcriptional repressor. Instead, it involves the ability of EZH2 to act as a coactivator for critical transcription factors including the androgen receptor. This functional switch is dependent on phosphorylation of EZH2 and requires an intact methyltransferase domain. Hence, targeting the non-PRC2 function of EZH2 may have therapeutic efficacy for treating metastatic, hormone-refractory prostate cancer.Entities:
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Year: 2012 PMID： 23239736 PMCID： PMC3625962 DOI： 10.1126/science.1227604
Source DB: PubMed Journal: Science ISSN： 0036-8075 Impact factor: 47.728