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Page 1
Selective inhibition of the BD2 bromodomain of BET proteins in prostate cancer.
Faivre EJ, McDaniel KF, Albert DH, Mantena SR, Plotnik JP, Wilcox D, Zhang L, Bui MH, Sheppard GS, Wang L, Sehgal V, Lin X, Huang X, Lu X, Uziel T, Hessler P, Lam LT, Bellin RJ, Mehta G, Fidanze S, Pratt JK, Liu D, Hasvold LA, Sun C, Panchal SC, Nicolette JJ, Fossey SL, Park CH, Longenecker K, Bigelow L, Torrent M, Rosenberg SH, Kati WM, Shen Y. Faivre EJ, et al. Among authors: pratt jk. Nature. 2020 Feb;578(7794):306-310. doi: 10.1038/s41586-020-1930-8. Epub 2020 Jan 22. Nature. 2020. PMID: 31969702
Methylpyrrole inhibitors of BET bromodomains.
Hasvold LA, Sheppard GS, Wang L, Fidanze SD, Liu D, Pratt JK, Mantei RA, Wada CK, Hubbard R, Shen Y, Lin X, Huang X, Warder SE, Wilcox D, Li L, Buchanan FG, Smithee L, Albert DH, Magoc TJ, Park CH, Petros AM, Panchal SC, Sun C, Kovar P, Soni NB, Elmore SW, Kati WM, McDaniel KF. Hasvold LA, et al. Among authors: pratt jk. Bioorg Med Chem Lett. 2017 May 15;27(10):2225-2233. doi: 10.1016/j.bmcl.2017.02.057. Epub 2017 Feb 24. Bioorg Med Chem Lett. 2017. PMID: 28268136
Discovery of N-(4-(2,4-Difluorophenoxy)-3-(6-methyl-7-oxo-6,7-dihydro-1H-pyrrolo[2,3-c]pyridin-4-yl)phenyl)ethanesulfonamide (ABBV-075/Mivebresib), a Potent and Orally Available Bromodomain and Extraterminal Domain (BET) Family Bromodomain Inhibitor.
McDaniel KF, Wang L, Soltwedel T, Fidanze SD, Hasvold LA, Liu D, Mantei RA, Pratt JK, Sheppard GS, Bui MH, Faivre EJ, Huang X, Li L, Lin X, Wang R, Warder SE, Wilcox D, Albert DH, Magoc TJ, Rajaraman G, Park CH, Hutchins CW, Shen JJ, Edalji RP, Sun CC, Martin R, Gao W, Wong S, Fang G, Elmore SW, Shen Y, Kati WM. McDaniel KF, et al. Among authors: pratt jk. J Med Chem. 2017 Oct 26;60(20):8369-8384. doi: 10.1021/acs.jmedchem.7b00746. Epub 2017 Oct 12. J Med Chem. 2017. PMID: 28949521
Discovery of N-Ethyl-4-[2-(4-fluoro-2,6-dimethyl-phenoxy)-5-(1-hydroxy-1-methyl-ethyl)phenyl]-6-methyl-7-oxo-1H-pyrrolo[2,3-c]pyridine-2-carboxamide (ABBV-744), a BET Bromodomain Inhibitor with Selectivity for the Second Bromodomain.
Sheppard GS, Wang L, Fidanze SD, Hasvold LA, Liu D, Pratt JK, Park CH, Longenecker K, Qiu W, Torrent M, Kovar PJ, Bui M, Faivre E, Huang X, Lin X, Wilcox D, Zhang L, Shen Y, Albert DH, Magoc TJ, Rajaraman G, Kati WM, McDaniel KF. Sheppard GS, et al. Among authors: pratt jk. J Med Chem. 2020 May 28;63(10):5585-5623. doi: 10.1021/acs.jmedchem.0c00628. Epub 2020 May 7. J Med Chem. 2020. PMID: 32324999
Preclinical Characterization of BET Family Bromodomain Inhibitor ABBV-075 Suggests Combination Therapeutic Strategies.
Bui MH, Lin X, Albert DH, Li L, Lam LT, Faivre EJ, Warder SE, Huang X, Wilcox D, Donawho CK, Sheppard GS, Wang L, Fidanze S, Pratt JK, Liu D, Hasvold L, Uziel T, Lu X, Kohlhapp F, Fang G, Elmore SW, Rosenberg SH, McDaniel KF, Kati WM, Shen Y. Bui MH, et al. Among authors: pratt jk. Cancer Res. 2017 Jun 1;77(11):2976-2989. doi: 10.1158/0008-5472.CAN-16-1793. Epub 2017 Apr 17. Cancer Res. 2017. PMID: 28416490
Discovery and optimization of novel constrained pyrrolopyridone BET family inhibitors.
Fidanze SD, Liu D, Mantei RA, Hasvold LA, Pratt JK, Sheppard GS, Wang L, Holms JH, Dai Y, Aguirre A, Bogdan A, Dietrich JD, Marjanovic J, Park CH, Hutchins CW, Lin X, Bui MH, Huang X, Wilcox D, Li L, Wang R, Kovar P, Magoc TJ, Rajaraman G, Albert DH, Shen Y, Kati WM, McDaniel KF. Fidanze SD, et al. Among authors: pratt jk. Bioorg Med Chem Lett. 2018 Jun 1;28(10):1804-1810. doi: 10.1016/j.bmcl.2018.04.020. Epub 2018 Apr 11. Bioorg Med Chem Lett. 2018. PMID: 29678460
Fragment-Based, Structure-Enabled Discovery of Novel Pyridones and Pyridone Macrocycles as Potent Bromodomain and Extra-Terminal Domain (BET) Family Bromodomain Inhibitors.
Wang L, Pratt JK, Soltwedel T, Sheppard GS, Fidanze SD, Liu D, Hasvold LA, Mantei RA, Holms JH, McClellan WJ, Wendt MD, Wada C, Frey R, Hansen TM, Hubbard R, Park CH, Li L, Magoc TJ, Albert DH, Lin X, Warder SE, Kovar P, Huang X, Wilcox D, Wang R, Rajaraman G, Petros AM, Hutchins CW, Panchal SC, Sun C, Elmore SW, Shen Y, Kati WM, McDaniel KF. Wang L, et al. Among authors: pratt jk. J Med Chem. 2017 May 11;60(9):3828-3850. doi: 10.1021/acs.jmedchem.7b00017. Epub 2017 Apr 21. J Med Chem. 2017. PMID: 28368119
Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability.
Randolph JT, Krueger AC, Donner PL, Pratt JK, Liu D, Motter CE, Rockway TW, Tufano MD, Wagner R, Lim HB, Beyer JM, Mondal R, Panchal NS, Colletti L, Liu Y, Koev G, Kati WM, Hernandez LE, Beno DWA, Longenecker KL, Stewart KD, Dumas EO, Molla A, Maring CJ. Randolph JT, et al. Among authors: pratt jk. J Med Chem. 2018 Feb 8;61(3):1153-1163. doi: 10.1021/acs.jmedchem.7b01630. Epub 2018 Jan 25. J Med Chem. 2018. PMID: 29342358
Discovery of ABT-267, a pan-genotypic inhibitor of HCV NS5A.
DeGoey DA, Randolph JT, Liu D, Pratt J, Hutchins C, Donner P, Krueger AC, Matulenko M, Patel S, Motter CE, Nelson L, Keddy R, Tufano M, Caspi DD, Krishnan P, Mistry N, Koev G, Reisch TJ, Mondal R, Pilot-Matias T, Gao Y, Beno DW, Maring CJ, Molla A, Dumas E, Campbell A, Williams L, Collins C, Wagner R, Kati WM. DeGoey DA, et al. J Med Chem. 2014 Mar 13;57(5):2047-57. doi: 10.1021/jm401398x. Epub 2014 Jan 15. J Med Chem. 2014. PMID: 24400777
31 results