- 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.
- Journal of medicinal chemistry
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- Wellcome Trust and Biotechnology and Biological Sciences Research Council
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Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
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