- Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.
Journal of medicinal chemistry (2008-10-24)
Nathan R Rose, Stanley S Ng, Jasmin Mecinović, Benoît M R Liénard, Simon H Bello, Zhe Sun, Michael A McDonough, Udo Oppermann, Christopher J Schofield
PMID18942826
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.
MATERIALS
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Succinic acid, BioReagent, BioRenewable, suitable for cell culture, suitable for insect cell culture