Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 51, Issue 22, Pages 7053-7056Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm800936s
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Funding
- Commonwealth Scholarship Commission
- The Wellcome Trust
- BBSRC
- Structural Genomics Consortium [1097737]
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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.
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