6079-88-5Relevant articles and documents
Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases
Rose, Nathan R.,Woon, Esther C. Y.,Tumber, Anthony,Walport, Louise J.,Chowdhury, Rasheduzzaman,Li, Xuan Shirley,King, Oliver N. F.,Lejeune, Clarisse,Ng, Stanley S.,Krojer, Tobias,Chan, Mun Chiang,Rydzik, Anna M.,Hopkinson, Richard J.,Che, Ka Hing,Daniel, Michelle,Strain-Damerell, Claire,Gileadi, Carina,Kochan, Grazyna,Leung, Ivanhoe K. H.,Dunford, James,Yeoh, Kar Kheng,Ratcliffe, Peter J.,Burgess-Brown, Nicola,Von Delft, Frank,Muller, Susanne,Marsden, Brian,Brennan, Paul E.,McDonough, Michael A.,Oppermann, Udo,Klose, Robert J.,Schofield, Christopher J.,Kawamura, Akane
supporting information; experimental part, p. 6639 - 6643 (2012/09/22)
The JmjC oxygenases catalyze the N-demethylation of Nε- 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.
