期刊
ACTA PHARMACOLOGICA SINICA
卷 35, 期 2, 页码 161-174出版社
ACTA PHARMACOLOGICA SINICA
DOI: 10.1038/aps.2013.161
关键词
EZH2; PRC2; transcriptional repression; gene activation; anticancer drug; crystal structure; SET domain; methyltransferase inhibitor; epigenetic therapy
资金
- Jay and Betty Van Andel Foundation
- National Natural Science Foundation of China [NSFC 81123004]
- Ministry of Science and Technology (China) [2012CB910403, 2013CB910601]
- Amway (USA)
EZH2 is the catalytic subunit of the polycomb repressive complex 2 (PRC2), which is a highly conserved histone methyltransferase that methylates lysine 27 of histone 3. Overexpression of EZH2 has been found in a wide range of cancers, including those of the prostate and breast. In this review, we address the current understanding of the oncogenic role of EZH2, including its PRC2-dependent transcriptional repression and PRC2-independent gene activation. We also discuss the connections between EZH2 and other silencing enzymes, such as DNA methyltransferase and histone deacetylase. We comprehensively address the architecture of the PRC2 complex and the crucial roles of each subunit. Finally, we summarize new progress in developing EZH2 inhibitors, which could be a new epigenetic therapy for cancers.
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