Recent Progress in Histone Demethylase Inhibitors

被引：144

作者：

McAllister, Tom E. ^{[1
,2
]}

England, Katherine S. ^{[3
,4
]}

Hopkinson, Richard J. ^{[1
]}

Brennan, Paul E. ^{[3
,4
]}

Kawamura, Akane ^{[1
,2
]}

Schofield, Christopher J. ^{[1
]}

机构：

[1] Univ Oxford, Chem Res Lab, 12 Mansfield Rd, Oxford OX1 3TA, England

[2] Univ Oxford, Div Cardiovasc Med, Radcliffe Dept Med, Old Rd Campus,Roosevelt Dr, Headington OX3 7BN, England

[3] Univ Oxford, Struct Genom Consortium, Old Rd Campus,Roosevelt Dr, Headington OX3 7DQ, England

[4] Univ Oxford, Target Discovery Inst, NDM Res Bldg,Roosevelt Dr, Headington OX3 7FZ, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2016年 / 59卷 / 04期

基金：

英国工程与自然科学研究理事会; 英国惠康基金; 加拿大创新基金会; 英国生物技术与生命科学研究理事会; 巴西圣保罗研究基金会;

关键词：

PROTEIN LYSINE METHYLATION; LSD1; INHIBITORS; STRUCTURAL BASIS; CANCER-CELLS; CYCLOPROPYLAMINE DERIVATIVES; ASPARAGINYL HYDROXYLASE; SELECTIVE-INHIBITION; LYSYL-HYDROXYLATION; BIOLOGICAL-ACTIVITY; MENTAL-RETARDATION;

D O I：

10.1021/acs.jmedchem.5b01758

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

There is increasing interest in targeting histone N-methyl-lysine demethylases (KDMs) with small molecules both for the generation of probes for target exploration and for therapeutic purposes. Here we update on previous reviews on the inhibition of the lysine-specific demethylases (LSDs or KDM1s) and JmjC families of N-methyl-lysine demethylases (JmjC KDMs, KDM2-7), focusing on the academic and patent literature from 2014 to date. We also highlight recent biochemical, biological, and structural studies which are relevant to KDM inhibitor development.

引用

页码：1308 / 1329

页数：22

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