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Title: Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases
Authors: Rose, N.R.
Woon, E.C.Y. 
Tumber, A.
Walport, L.J.
Chowdhury, R.
Li, X.S.
King, O.N.F.
Lejeune, C.
Ng, S.S.
Krojer, T.
Chan, M.C.
Rydzik, A.M.
Hopkinson, R.J.
Che, K.H.
Daniel, M.
Strain-Damerell, C.
Gileadi, C.
Kochan, G.
Leung, I.K.H.
Dunford, J.
Yeoh, K.K.
Ratcliffe, P.J.
Burgess-Brown, N.
Von Delft, F.
Muller, S.
Marsden, B.
Brennan, P.E.
McDonough, M.A.
Oppermann, U.
Klose, R.J.
Schofield, C.J.
Kawamura, A.
Issue Date: 26-Jul-2012
Citation: Rose, N.R., Woon, E.C.Y., Tumber, A., Walport, L.J., Chowdhury, R., Li, X.S., King, O.N.F., Lejeune, C., Ng, S.S., Krojer, T., Chan, M.C., Rydzik, A.M., Hopkinson, R.J., Che, K.H., Daniel, M., Strain-Damerell, C., Gileadi, C., Kochan, G., Leung, I.K.H., Dunford, J., Yeoh, K.K., Ratcliffe, P.J., Burgess-Brown, N., Von Delft, F., Muller, S., Marsden, B., Brennan, P.E., McDonough, M.A., Oppermann, U., Klose, R.J., Schofield, C.J., Kawamura, A. (2012-07-26). Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases. Journal of Medicinal Chemistry 55 (14) : 6639-6643. ScholarBank@NUS Repository.
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 active site metal via its hydrazide carbonyl and dimethylamino groups. © 2012 American Chemical Society.
Source Title: Journal of Medicinal Chemistry
ISSN: 00222623
DOI: 10.1021/jm300677j
Appears in Collections:Staff Publications

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