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

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Abstrakt

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.

OriginalsprogEngelsk
TidsskriftJournal of Medicinal Chemistry
Vol/bind51
Udgave nummer22
Sider (fra-til)7053-7056
Antal sider4
ISSN0022-2623
DOI
StatusUdgivet - 27. nov. 2008
Udgivet eksterntJa

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