Histone lysine methyltransferases as anti-cancer targets for drug discovery

被引：0

作者：

Qing Liu

Ming-wei Wang

机构：

[1] The CAS Key Laboratory of Receptor Research,

[2] Shanghai Institute of Materia Medica,undefined

[3] Chinese Academy of Sciences,undefined

[4] The National Center for Drug Screening,undefined

[5] School of Pharmacy,undefined

[6] Fudan University,undefined

来源：

Acta Pharmacologica Sinica | 2016年 / 37卷

关键词：

histone methyltransferases; adenosylmethionine; small molecule inhibitors; anti-cancer drugs; epigenetic modification; drug discovery;

D O I：

暂无

中图分类号：

学科分类号：

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.

引用

页码：1273 / 1280

页数：7

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