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Updated: Jun 28, 2026

Assays for Validating Histone Acetyltransferase Inhibitors
Published on: August 6, 2020
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases
Nathan R Rose1, Stanley S Ng, Jasmin Mecinović
1The Department of Chemistry and the Oxford Centre for Integrative Systems Biology, Chemistry Research Laboratory, University of Oxford, 12 Mansfield Road, Oxford, OX1 3TA, United Kingdom.
Abstract:
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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