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Inhibition of 2-oxoglutarate dependent oxygenases.
Rose NR, McDonough MA, King ON, Kawamura A, Schofield CJ. Rose NR, et al. Among authors: kawamura a. Chem Soc Rev. 2011 Aug;40(8):4364-97. doi: 10.1039/c0cs00203h. Epub 2011 Mar 10. Chem Soc Rev. 2011. PMID: 21390379 Review.
The oncometabolite 2-hydroxyglutarate inhibits histone lysine demethylases.
Chowdhury R, Yeoh KK, Tian YM, Hillringhaus L, Bagg EA, Rose NR, Leung IK, Li XS, Woon EC, Yang M, McDonough MA, King ON, Clifton IJ, Klose RJ, Claridge TD, Ratcliffe PJ, Schofield CJ, Kawamura A. Chowdhury R, et al. Among authors: kawamura a. EMBO Rep. 2011 May;12(5):463-9. doi: 10.1038/embor.2011.43. Epub 2011 Apr 1. EMBO Rep. 2011. PMID: 21460794 Free PMC article.
A photoreactive small-molecule probe for 2-oxoglutarate oxygenases.
Rotili D, Altun M, Kawamura A, Wolf A, Fischer R, Leung IKH, Mackeen MM, Tian YM, Ratcliffe PJ, Mai A, Kessler BM, Schofield CJ. Rotili D, et al. Among authors: kawamura a. Chem Biol. 2011 May 27;18(5):642-654. doi: 10.1016/j.chembiol.2011.03.007. Chem Biol. 2011. PMID: 21609845 Free PMC article.
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: kawamura a. 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.
Plant growth regulator daminozide is a selective inhibitor of human KDM2/7 histone demethylases.
Rose NR, Woon EC, Tumber A, Walport LJ, Chowdhury R, Li XS, King ON, Lejeune C, Ng SS, Krojer T, Chan MC, Rydzik AM, Hopkinson RJ, Che KH, Daniel M, Strain-Damerell C, Gileadi C, Kochan G, Leung IK, Dunford J, Yeoh KK, Ratcliffe PJ, Burgess-Brown N, von Delft F, Muller S, Marsden B, Brennan PE, McDonough MA, Oppermann U, Klose RJ, Schofield CJ, Kawamura A. Rose NR, et al. Among authors: kawamura a. J Med Chem. 2012 Jul 26;55(14):6639-43. doi: 10.1021/jm300677j. Epub 2012 Jul 11. J Med Chem. 2012. PMID: 22724510 Free PMC article.
Dual-action inhibitors of HIF prolyl hydroxylases that induce binding of a second iron ion.
Yeoh KK, Chan MC, Thalhammer A, Demetriades M, Chowdhury R, Tian YM, Stolze I, McNeill LA, Lee MK, Woon ECY, Mackeen MM, Kawamura A, Ratcliffe PJ, Mecinović J, Schofield CJ. Yeoh KK, et al. Among authors: kawamura a. Org Biomol Chem. 2013 Feb 7;11(5):732-745. doi: 10.1039/c2ob26648b. Epub 2012 Nov 15. Org Biomol Chem. 2013. PMID: 23151668 Free PMC article.
Reporter ligand NMR screening method for 2-oxoglutarate oxygenase inhibitors.
Leung IK, Demetriades M, Hardy AP, Lejeune C, Smart TJ, Szöllössi A, Kawamura A, Schofield CJ, Claridge TD. Leung IK, et al. Among authors: kawamura a. J Med Chem. 2013 Jan 24;56(2):547-55. doi: 10.1021/jm301583m. Epub 2013 Jan 4. J Med Chem. 2013. PMID: 23234607 Free PMC article.
1,229 results