Histone lysine methyltransferases as anti-cancer targets for drug discovery  

作　　者：Qing LIU Ming-wei WANG 

机构地区：[1]The CAS Key Laboratory of Receptor Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China [2]The National Center for Drug Screening, Shanghai 201203, China [3]School of Pharmacy, Fudan University, Shanghai 201203, China

出　　处：《Acta Pharmacologica Sinica》2016年第10期1273-1280,共8页中国药理学报（英文版）

基　　金：Acknowledgements We gratefully acknowledge the financial support from the National Health and Family Planning Commission （2012ZX09304-011, 2013ZX09401003-005, 2013ZX09507001, 2013ZX09507-002, and 2014ZX09507002-001）, the National Natural Science Foundation of China （21302202）, Shanghai Science and Technology Development Fund （15DZ2291600）, and the Thousand Talents Program in China.

摘　　要：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.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.

关 键 词：histone methyltransferases adenosylmethionine small molecule inhibitors anti-cancer drugs epigenetic modification drugdiscovery 

分 类 号：R[医药卫生]