Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases

Nathan R. Rose, Stanley S. Ng, Jasmin Mecinović, B. M R Liénard, Simon H. Bello, Zhe Sun, Michael A. McDonough, Udo Oppermann*, Christopher J. Schofield

*Corresponding author for this work

Research output: Contribution to journalJournal articleResearchpeer-review

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.

Original languageEnglish
JournalJournal of Medicinal Chemistry
Volume51
Issue number22
Pages (from-to)7053-7056
Number of pages4
ISSN0022-2623
DOIs
Publication statusPublished - 27. Nov 2008
Externally publishedYes

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