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https://doi.org/10.1021/jm300677j
| 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. https://doi.org/10.1021/jm300677j | 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 | URI: | http://scholarbank.nus.edu.sg/handle/10635/125028 | ISSN: | 00222623 | DOI: | 10.1021/jm300677j |
| Appears in Collections: | Staff Publications |
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