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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.


Journal article


Journal of medicinal chemistry

Publication Date





7053 - 7056


The 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.


Humans, Ketoglutaric Acids, Oxidoreductases, N-Demethylating, Enzyme Inhibitors, Crystallography, X-Ray, Molecular Structure, Protein Structure, Tertiary, Structure-Activity Relationship, Dose-Response Relationship, Drug, Stereoisomerism, Models, Molecular