期刊
ACTA PHARMACOLOGICA SINICA
卷 37, 期 10, 页码 1273-1280出版社
NATURE PUBL GROUP
DOI: 10.1038/aps.2016.64
关键词
histone methyltransferases; adenosylmethionine; small molecule inhibitors; anti-cancer drugs; epigenetic modification; drug discovery
资金
- National Health and Family Planning Commission [2012ZX09304-011, 2013ZX09401003-005, 2013ZX09507001, 2013ZX09507-002, 2014ZX09507002-001]
- National Natural Science Foundation of China [21302202]
- Shanghai Science and Technology Development Fund [15DZ2291600]
- Thousand Talents Program in China
Post-translational epigenetic modification of histones is controlled by a number of histone-modifying enzymes. Such modification regulates the accessibility of DNA and the subsequent expression or silencing of a gene. Human histone methyltransferases (HMTs) constitute a large family that includes histone lysine methyltransferases (HKMTs) and histone/protein arginine methyltransferases (PRMTs). There is increasing evidence showing a correlation between HKMTs and cancer pathogenesis. Here, we present an overview of representative HKMTs, including their biological and biochemical properties as well as the profiles of small molecule inhibitors for a comprehensive understanding of HKMTs in drug discovery.
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