Chromatin proteins and modifications as drug targets

被引：335

作者：

Helin, Kristian ^{[1
,2
,3
]}

Dhanak, Dashyant ^{[4
]}

机构：

[1] Univ Copenhagen, Biotech Res & Innovat Ctr, DK-2200 Copenhagen, Denmark

[2] Univ Copenhagen, Ctr Epigenet, DK-2200 Copenhagen, Denmark

[3] Univ Copenhagen, Danish Stem Cell Ctr, DK-2200 Copenhagen, Denmark

[4] Janssen Res & Dev, Spring House, PA 19477 USA

来源：

NATURE | 2013年 / 502卷 / 7472期

基金：

欧洲研究理事会; 新加坡国家研究基金会;

关键词：

HISTONE METHYLTRANSFERASE EZH2; SMALL-MOLECULE INHIBITOR; THERAPEUTIC STRATEGY; SOMATIC MUTATIONS; CHEMICAL PROBE; SELECTIVE-INHIBITION; DEMETHYLASE GENE; HDAC INHIBITORS; CANCER-CELLS; LYSINE; 27;

D O I：

10.1038/nature12751

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

A plethora of groundbreaking studies have demonstrated the importance of chromatin-associated proteins and post-translational modifications of histones, proteins and DNA (so-called epigenetic modifications) for transcriptional control and normal development. Disruption of epigenetic control is a frequent event in disease, and the first epigenetic-based therapies for cancer treatment have been approved. A generation of new classes of potent and specific inhibitors for several chromatin-associated proteins have shown promise in preclinical trials. Although the biology of epigenetic regulation is complex, new inhibitors such as these will hopefully be of clinical use in the coming years.

引用

页码：480 / 488

页数：9

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