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Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.

Abstract:

The JmjC oxygenases catalyze the N-demethylation of N(ε)-methyl lysine residues in histones and are current therapeutic targets. A set of human 2-oxoglutarate analogues were screened using a unified assay platform for JmjC demethylases and related oxygenases. Results led to the finding that daminozide (N-(dimethylamino)succinamic acid, 160 Da), a plant growth regulator, selectively inhibits the KDM2/7 JmjC subfamily. Kinetic and crystallographic studies reveal that daminozide chelates the act...

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Publication status:
Published

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Publisher copy:
10.1021/jm300677j

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Journal:
Journal of medicinal chemistry
Volume:
55
Issue:
14
Pages:
6639-6643
Publication date:
2012-07-05
DOI:
EISSN:
1520-4804
ISSN:
0022-2623
URN:
uuid:c67ca6f0-9687-4806-8a9d-18ad921b832a
Source identifiers:
341091
Local pid:
pubs:341091

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