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First-in-Class Inhibitors of the Ribosomal Oxygenase MINA53.
Nowak RP, Tumber A, Hendrix E, Ansari MSZ, Sabatino M, Antonini L, Andrijes R, Salah E, Mautone N, Pellegrini FR, Simelis K, Kawamura A, Johansson C, Passeri D, Pellicciari R, Ciogli A, Del Bufalo D, Ragno R, Coleman ML, Trisciuoglio D, Mai A, Oppermann U, Schofield CJ, Rotili D. Nowak RP, et al. Among authors: oppermann u. J Med Chem. 2021 Dec 9;64(23):17031-17050. doi: 10.1021/acs.jmedchem.1c00605. Epub 2021 Nov 29. J Med Chem. 2021. PMID: 34843649 Free PMC article.
8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors.
Bavetsias V, Lanigan RM, Ruda GF, Atrash B, McLaughlin MG, Tumber A, Mok NY, Le Bihan YV, Dempster S, Boxall KJ, Jeganathan F, Hatch SB, Savitsky P, Velupillai S, Krojer T, England KS, Sejberg J, Thai C, Donovan A, Pal A, Scozzafava G, Bennett JM, Kawamura A, Johansson C, Szykowska A, Gileadi C, Burgess-Brown NA, von Delft F, Oppermann U, Walters Z, Shipley J, Raynaud FI, Westaway SM, Prinjha RK, Fedorov O, Burke R, Schofield CJ, Westwood IM, Bountra C, Müller S, van Montfort RL, Brennan PE, Blagg J. Bavetsias V, et al. Among authors: oppermann u. J Med Chem. 2016 Feb 25;59(4):1388-409. doi: 10.1021/acs.jmedchem.5b01635. Epub 2016 Jan 7. J Med Chem. 2016. PMID: 26741168 Free PMC article.
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: oppermann u. 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.
Human UTY(KDM6C) is a male-specific Nϵ-methyl lysyl demethylase.
Walport LJ, Hopkinson RJ, Vollmar M, Madden SK, Gileadi C, Oppermann U, Schofield CJ, Johansson C. Walport LJ, et al. Among authors: oppermann u. J Biol Chem. 2014 Jun 27;289(26):18302-13. doi: 10.1074/jbc.M114.555052. Epub 2014 May 5. J Biol Chem. 2014. PMID: 24798337 Free PMC article.
Docking and Linking of Fragments To Discover Jumonji Histone Demethylase Inhibitors.
Korczynska M, Le DD, Younger N, Gregori-Puigjané E, Tumber A, Krojer T, Velupillai S, Gileadi C, Nowak RP, Iwasa E, Pollock SB, Ortiz Torres I, Oppermann U, Shoichet BK, Fujimori DG. Korczynska M, et al. Among authors: oppermann u. J Med Chem. 2016 Feb 25;59(4):1580-98. doi: 10.1021/acs.jmedchem.5b01527. Epub 2015 Dec 23. J Med Chem. 2016. PMID: 26699912 Free PMC article.
Advances and challenges in understanding histone demethylase biology.
Nowak RP, Tumber A, Johansson C, Che KH, Brennan P, Owen D, Oppermann U. Nowak RP, et al. Among authors: oppermann u. Curr Opin Chem Biol. 2016 Aug;33:151-9. doi: 10.1016/j.cbpa.2016.06.021. Epub 2016 Jun 29. Curr Opin Chem Biol. 2016. PMID: 27371875 Review.
260 results