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Inhibitor scaffolds for 2-oxoglutarate-dependent histone lysine demethylases.

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.
Publication status:
Published

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Publisher copy:
10.1021/jm800936s

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Journal:
Journal of medicinal chemistry More from this journal
Volume:
51
Issue:
22
Pages:
7053-7056
Publication date:
2008-11-01
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
Language:
English
Keywords:
Pubs id:
pubs:34433
UUID:
uuid:0b142e69-2440-4b78-92b7-583a057a631c
Local pid:
pubs:34433
Source identifiers:
34433
Deposit date:
2012-12-19

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