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

Journal article

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

Authors: Rose, N; Woon, E; Tumber, A; Walport, L; Chowdhury, R

• Publication status: Published
• Journal: Journal of medicinal chemistry
• Volume: 55
• Issue: 14
• Pages: 6639-6643
• Publication date: 2012-07-01
• DOI: 10.1021/jm300677j
• EISSN: 1520-4804
• ISSN: 0022-2623
• Language: English
• Keywords: Protein Conformation; Succinates; Substrate Specificity; Inhibitory Concentration 50; Models, Molecular; Enzyme Inhibitors; Humans; Jumonji Domain-Containing Histone Demethylases; Plant Growth Regulators