Recent progress in developing selective inhibitors of protein methyltransferases

被引:37
作者
Kaniskan, H. Umit [1 ]
Jin, Jian [1 ,2 ]
机构
[1] Icahn Sch Med Mt Sinai, Dept Pharmacol Sci, New York, NY 10029 USA
[2] Icahn Sch Med Mt Sinai, Dept Oncol Sci, New York, NY 10029 USA
基金
美国国家卫生研究院;
关键词
SMALL-MOLECULE INHIBITORS; REPRESSIVE COMPLEX 2; LYSINE METHYLTRANSFERASE; DOT1L INHIBITORS; COMPETITIVE INHIBITOR; STRUCTURAL BASIS; DRUG DISCOVERY; BINDING POCKET; IN-VIVO; CARM1;
D O I
10.1016/j.cbpa.2017.06.013
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Mounting evidence suggests that protein methyltransferases (PMTs), which catalyze methylation of histones as well as nonhistone proteins, play a crucial role in diverse biological pathways and human diseases. In particular, PMTs have been recognized as major players in regulating gene expression and chromatin state. There has been an increasingly growing interest in these enzymes as potential therapeutic targets and over the past two years tremendous progress has been made in the discovery of selective, small molecule inhibitors of protein lysine and arginine methyltransferases. Inhibitors of PMTs have been used extensively in oncology studies as tool compounds, and inhibitors of EZH2, DOT1 L and PRMT5 are currently in clinical trials.
引用
收藏
页码:100 / 108
页数:9
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