- 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...
Expand abstract - Publication status:
- Published
- 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
- Copyright date:
- 2012
Journal article
Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
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