Inhibitor Scaffolds for 2-Oxoglutarate-Dependent Histone Lysine Demethylases

被引：196

作者：

Rose, Nathan R. ^{[2
,3
]}

Ng, Stanley S. ^{[1
,4
]}

Mecinovic, Jasmin ^{[2
,3
]}

Lienard, Benoit M. R. ^{[2
,3
]}

Bello, Simon H. ^{[2
,3
]}

Sun, Zhe ^{[1
,4
]}

McDonough, Michael A. ^{[2
,3
]}

Oppermann, Udo ^{[1
,4
]}

Schofield, Christopher J. ^{[2
,3
]}

机构：

[1] Univ Oxford, Struct Genom Consortium, Headington OX3 7DQ, England

[2] Univ Oxford, Dept Chem, Oxford OX1 3TA, England

[3] Univ Oxford, Oxford Ctr Integrat Syst Biol, Chem Res Lab, Oxford OX1 3TA, England

[4] Botnar Res Ctr, Oxford Biomed Res Unit, Oxford OX3 7LD, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2008年 / 51卷 / 22期

基金：

英国惠康基金; 英国生物技术与生命科学研究理事会;

关键词：

D O I：

10.1021/jm800936s

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The dynamic methylation of histone lysyl residues plays an important role in biology by regulating transcription, maintaining genomic integrity, and by contributing to epigenetic effects. Here we describe a variety of inhibitor scaffolds that inhibit the human 2-oxoglutarate-dependent JMJD2 subfamily of histone demethylases. Combined with structural data, these chemical starting points will be useful to generate small-molecule probes to analyze the physiological roles of these enzymes in epigenetic signaling.

引用

收藏

页码：7053 / 7056

页数：4

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