Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
نویسندگان
چکیده
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 active site metal via its hydrazide carbonyl and dimethylamino groups.
منابع مشابه
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عنوان ژورنال:
- Journal of medicinal chemistry
دوره 55 14 شماره
صفحات -
تاریخ انتشار 2012