Please use this identifier to cite or link to this item: https://doi.org/10.1021/jm300677j
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dc.titlePlant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases
dc.contributor.authorRose, N.R.
dc.contributor.authorWoon, E.C.Y.
dc.contributor.authorTumber, A.
dc.contributor.authorWalport, L.J.
dc.contributor.authorChowdhury, R.
dc.contributor.authorLi, X.S.
dc.contributor.authorKing, O.N.F.
dc.contributor.authorLejeune, C.
dc.contributor.authorNg, S.S.
dc.contributor.authorKrojer, T.
dc.contributor.authorChan, M.C.
dc.contributor.authorRydzik, A.M.
dc.contributor.authorHopkinson, R.J.
dc.contributor.authorChe, K.H.
dc.contributor.authorDaniel, M.
dc.contributor.authorStrain-Damerell, C.
dc.contributor.authorGileadi, C.
dc.contributor.authorKochan, G.
dc.contributor.authorLeung, I.K.H.
dc.contributor.authorDunford, J.
dc.contributor.authorYeoh, K.K.
dc.contributor.authorRatcliffe, P.J.
dc.contributor.authorBurgess-Brown, N.
dc.contributor.authorVon Delft, F.
dc.contributor.authorMuller, S.
dc.contributor.authorMarsden, B.
dc.contributor.authorBrennan, P.E.
dc.contributor.authorMcDonough, M.A.
dc.contributor.authorOppermann, U.
dc.contributor.authorKlose, R.J.
dc.contributor.authorSchofield, C.J.
dc.contributor.authorKawamura, A.
dc.date.accessioned2016-06-02T10:29:58Z
dc.date.available2016-06-02T10:29:58Z
dc.date.issued2012-07-26
dc.identifier.citationRose, 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
dc.identifier.issn00222623
dc.identifier.urihttp://scholarbank.nus.edu.sg/handle/10635/125028
dc.description.abstractThe 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.
dc.description.urihttp://libproxy1.nus.edu.sg/login?url=http://dx.doi.org/10.1021/jm300677j
dc.sourceScopus
dc.typeArticle
dc.contributor.departmentPHARMACY
dc.description.doi10.1021/jm300677j
dc.description.sourcetitleJournal of Medicinal Chemistry
dc.description.volume55
dc.description.issue14
dc.description.page6639-6643
dc.description.codenJMCMA
dc.identifier.isiut000306764600036
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