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Quantitative high-throughput screening identifies 8-hydroxyquinolines as cell-active histone demethylase inhibitors.
King ON, Li XS, Sakurai M, Kawamura A, Rose NR, Ng SS, Quinn AM, Rai G, Mott BT, Beswick P, Klose RJ, Oppermann U, Jadhav A, Heightman TD, Maloney DJ, Schofield CJ, Simeonov A. King ON, et al. Among authors: oppermann u. PLoS One. 2010 Nov 23;5(11):e15535. doi: 10.1371/journal.pone.0015535. PLoS One. 2010. PMID: 21124847 Free PMC article.
Assessing histone demethylase inhibitors in cells: lessons learned.
Hatch SB, Yapp C, Montenegro RC, Savitsky P, Gamble V, Tumber A, Ruda GF, Bavetsias V, Fedorov O, Atrash B, Raynaud F, Lanigan R, Carmichael L, Tomlin K, Burke R, Westaway SM, Brown JA, Prinjha RK, Martinez ED, Oppermann U, Schofield CJ, Bountra C, Kawamura A, Blagg J, Brennan PE, Rossanese O, Müller S. Hatch SB, et al. Among authors: oppermann u. Epigenetics Chromatin. 2017 Mar 1;10:9. doi: 10.1186/s13072-017-0116-6. eCollection 2017. Epigenetics Chromatin. 2017. PMID: 28265301 Free PMC article.
Crystal structures of histone demethylase JMJD2A reveal basis for substrate specificity.
Ng SS, Kavanagh KL, McDonough MA, Butler D, Pilka ES, Lienard BM, Bray JE, Savitsky P, Gileadi O, von Delft F, Rose NR, Offer J, Scheinost JC, Borowski T, Sundstrom M, Schofield CJ, Oppermann U. Ng SS, et al. Among authors: oppermann u. Nature. 2007 Jul 5;448(7149):87-91. doi: 10.1038/nature05971. Epub 2007 Jun 24. Nature. 2007. PMID: 17589501
Linking of 2-oxoglutarate and substrate binding sites enables potent and highly selective inhibition of JmjC histone demethylases.
Woon EC, Tumber A, Kawamura A, Hillringhaus L, Ge W, Rose NR, Ma JH, Chan MC, Walport LJ, Che KH, Ng SS, Marsden BD, Oppermann U, McDonough MA, Schofield CJ. Woon EC, et al. Among authors: oppermann u. Angew Chem Int Ed Engl. 2012 Feb 13;51(7):1631-4. doi: 10.1002/anie.201107833. Epub 2012 Jan 12. Angew Chem Int Ed Engl. 2012. PMID: 22241642 No abstract available.
257 results