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82 results

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Page 1
Selective targeting of BD1 and BD2 of the BET proteins in cancer and immunoinflammation.
Gilan O, Rioja I, Knezevic K, Bell MJ, Yeung MM, Harker NR, Lam EYN, Chung CW, Bamborough P, Petretich M, Urh M, Atkinson SJ, Bassil AK, Roberts EJ, Vassiliadis D, Burr ML, Preston AGS, Wellaway C, Werner T, Gray JR, Michon AM, Gobbetti T, Kumar V, Soden PE, Haynes A, Vappiani J, Tough DF, Taylor S, Dawson SJ, Bantscheff M, Lindon M, Drewes G, Demont EH, Daniels DL, Grandi P, Prinjha RK, Dawson MA. Gilan O, et al. Among authors: bamborough p. Science. 2020 Apr 24;368(6489):387-394. doi: 10.1126/science.aaz8455. Epub 2020 Mar 19. Science. 2020. PMID: 32193360 Free PMC article.
Discovery and characterization of small molecule inhibitors of the BET family bromodomains.
Chung CW, Coste H, White JH, Mirguet O, Wilde J, Gosmini RL, Delves C, Magny SM, Woodward R, Hughes SA, Boursier EV, Flynn H, Bouillot AM, Bamborough P, Brusq JM, Gellibert FJ, Jones EJ, Riou AM, Homes P, Martin SL, Uings IJ, Toum J, Clement CA, Boullay AB, Grimley RL, Blandel FM, Prinjha RK, Lee K, Kirilovsky J, Nicodeme E. Chung CW, et al. Among authors: bamborough p. J Med Chem. 2011 Jun 9;54(11):3827-38. doi: 10.1021/jm200108t. Epub 2011 May 13. J Med Chem. 2011. PMID: 21568322
Selectivity of kinase inhibitor fragments.
Bamborough P, Brown MJ, Christopher JA, Chung CW, Mellor GW. Bamborough P, et al. J Med Chem. 2011 Jul 28;54(14):5131-43. doi: 10.1021/jm200349b. Epub 2011 Jun 23. J Med Chem. 2011. PMID: 21699136
Identification of a novel series of BET family bromodomain inhibitors: binding mode and profile of I-BET151 (GSK1210151A).
Seal J, Lamotte Y, Donche F, Bouillot A, Mirguet O, Gellibert F, Nicodeme E, Krysa G, Kirilovsky J, Beinke S, McCleary S, Rioja I, Bamborough P, Chung CW, Gordon L, Lewis T, Walker AL, Cutler L, Lugo D, Wilson DM, Witherington J, Lee K, Prinjha RK. Seal J, et al. Among authors: bamborough p. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2968-72. doi: 10.1016/j.bmcl.2012.02.041. Epub 2012 Feb 24. Bioorg Med Chem Lett. 2012. PMID: 22437115
Naphthyridines as novel BET family bromodomain inhibitors.
Mirguet O, Lamotte Y, Chung CW, Bamborough P, Delannée D, Bouillot A, Gellibert F, Krysa G, Lewis A, Witherington J, Huet P, Dudit Y, Trottet L, Nicodeme E. Mirguet O, et al. Among authors: bamborough p. ChemMedChem. 2014 Mar;9(3):580-9. doi: 10.1002/cmdc.201300259. Epub 2013 Sep 2. ChemMedChem. 2014. PMID: 24000170
Discovery of epigenetic regulator I-BET762: lead optimization to afford a clinical candidate inhibitor of the BET bromodomains.
Mirguet O, Gosmini R, Toum J, Clément CA, Barnathan M, Brusq JM, Mordaunt JE, Grimes RM, Crowe M, Pineau O, Ajakane M, Daugan A, Jeffrey P, Cutler L, Haynes AC, Smithers NN, Chung CW, Bamborough P, Uings IJ, Lewis A, Witherington J, Parr N, Prinjha RK, Nicodème E. Mirguet O, et al. Among authors: bamborough p. J Med Chem. 2013 Oct 10;56(19):7501-15. doi: 10.1021/jm401088k. Epub 2013 Sep 25. J Med Chem. 2013. PMID: 24015967
The discovery of I-BET726 (GSK1324726A), a potent tetrahydroquinoline ApoA1 up-regulator and selective BET bromodomain inhibitor.
Gosmini R, Nguyen VL, Toum J, Simon C, Brusq JM, Krysa G, Mirguet O, Riou-Eymard AM, Boursier EV, Trottet L, Bamborough P, Clark H, Chung CW, Cutler L, Demont EH, Kaur R, Lewis AJ, Schilling MB, Soden PE, Taylor S, Walker AL, Walker MD, Prinjha RK, Nicodème E. Gosmini R, et al. Among authors: bamborough p. J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24. J Med Chem. 2014. PMID: 25249180
1,3-Dimethyl Benzimidazolones Are Potent, Selective Inhibitors of the BRPF1 Bromodomain.
Demont EH, Bamborough P, Chung CW, Craggs PD, Fallon D, Gordon LJ, Grandi P, Hobbs CI, Hussain J, Jones EJ, Le Gall A, Michon AM, Mitchell DJ, Prinjha RK, Roberts AD, Sheppard RJ, Watson RJ. Demont EH, et al. Among authors: bamborough p. ACS Med Chem Lett. 2014 Sep 10;5(11):1190-5. doi: 10.1021/ml5002932. eCollection 2014 Nov 13. ACS Med Chem Lett. 2014. PMID: 25408830 Free PMC article.
82 results