The Plant Growth Regulator Daminozide is a Selective Inhibitor of the Human KDM2/7 Histone Demethylases

The JmjC oxygenases catalyse the N-demethylation of N(ε)-methyl lysine residues in histones and are current therapeutic targets. A set of 2-oxoglutarate analogues were screened using a unified assay platform for JmjC demethylases and related oxygenases. Results led to the finding that daminozide (N-...

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Published in:J Med Chem
Main Authors: 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
Format: Artigo
Language:Inglês
Published: 2012
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Online Access:https://ncbi.nlm.nih.gov/pmc/articles/PMC4673902/
https://ncbi.nlm.nih.gov/pubmed/22724510
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm300677j
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