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Page 1
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. ChemMedChem. 2014 Mar;9(3):580-9. doi: 10.1002/cmdc.201300259. Epub 2013 Sep 2. ChemMedChem. 2014. PMID: 24000170
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: mirguet o. J Med Chem. 2011 Jun 9;54(11):3827-38. doi: 10.1021/jm200108t. Epub 2011 May 13. J Med Chem. 2011. PMID: 21568322
From ApoA1 upregulation to BET family bromodomain inhibition: discovery of I-BET151.
Mirguet O, Lamotte Y, Donche F, Toum J, Gellibert F, Bouillot A, Gosmini R, Nguyen VL, Delannée D, Seal J, Blandel F, Boullay AB, Boursier E, Martin S, Brusq JM, Krysa G, Riou A, Tellier R, Costaz A, Huet P, Dudit Y, Trottet L, Kirilovsky J, Nicodeme E. Mirguet O, et al. Bioorg Med Chem Lett. 2012 Apr 15;22(8):2963-7. doi: 10.1016/j.bmcl.2012.01.125. Epub 2012 Feb 8. Bioorg Med Chem Lett. 2012. PMID: 22386529
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: mirguet o. J Med Chem. 2014 Oct 9;57(19):8111-31. doi: 10.1021/jm5010539. Epub 2014 Sep 24. J Med Chem. 2014. PMID: 25249180
Design and synthesis of bridged piperidine and piperazine isosteres.
Maertens G, Saavedra OM, Vece V, Reyes MAV, Hocine S, Öney E, Goument B, Mirguet O, Le Tiran A, Gloanec P, Hanessian S. Maertens G, et al. Among authors: mirguet o. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2627-2630. doi: 10.1016/j.bmcl.2018.06.038. Epub 2018 Jun 19. Bioorg Med Chem Lett. 2018. PMID: 29937060
Juniperanol: First total synthesis and evaluation in Type 2 Diabetes disease.
Carrër A, Turban S, Provost N, Caliez A, Lamarche G, Zanirato G, Beucher M, Pean C, Mirguet O, Perron-Sierra F, Michelet V. Carrër A, et al. Among authors: mirguet o. Bioorg Chem. 2019 Nov;92:103243. doi: 10.1016/j.bioorg.2019.103243. Epub 2019 Sep 5. Bioorg Chem. 2019. PMID: 31518756
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: mirguet o. 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
Comparison of soluble guanylate cyclase stimulators and activators in models of cardiovascular disease associated with oxidative stress.
Costell MH, Ancellin N, Bernard RE, Zhao S, Upson JJ, Morgan LA, Maniscalco K, Olzinski AR, Ballard VL, Herry K, Grondin P, Dodic N, Mirguet O, Bouillot A, Gellibert F, Coatney RW, Lepore JJ, Jucker BM, Jolivette LJ, Willette RN, Schnackenberg CG, Behm DJ. Costell MH, et al. Among authors: mirguet o. Front Pharmacol. 2012 Jul 5;3:128. doi: 10.3389/fphar.2012.00128. eCollection 2012. Front Pharmacol. 2012. PMID: 22783192 Free PMC article.
20 results