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Development of Orally Efficacious Allosteric Inhibitors of TNFα via Fragment-Based Drug Design.
Dietrich JD, Longenecker KL, Wilson NS, Goess C, Panchal SC, Swann SL, Petros AM, Hobson AD, Ihle D, Song D, Richardson P, Comess KM, Cox PB, Dombrowski A, Sarris K, Donnelly-Roberts DL, Duignan DB, Gomtsyan A, Jung P, Krueger AC, Mathieu S, McClure A, Stoll VS, Wetter J, Mankovich JA, Hajduk PJ, Vasudevan A, Stoffel RH, Sun C. Dietrich JD, et al. Among authors: longenecker kl. J Med Chem. 2021 Jan 14;64(1):417-429. doi: 10.1021/acs.jmedchem.0c01280. Epub 2020 Dec 30. J Med Chem. 2021. PMID: 33378180
Fragment-based discovery of a potent NAMPT inhibitor.
Korepanova A, Longenecker KL, Pratt SD, Panchal SC, Clark RF, Lake M, Gopalakrishnan SM, Raich D, Sun C, Petros AM. Korepanova A, et al. Among authors: longenecker kl. Bioorg Med Chem Lett. 2018 Feb 1;28(3):437-440. doi: 10.1016/j.bmcl.2017.12.023. Epub 2017 Dec 12. Bioorg Med Chem Lett. 2018. PMID: 29287958
SAR and characterization of non-substrate isoindoline urea inhibitors of nicotinamide phosphoribosyltransferase (NAMPT).
Curtin ML, Heyman HR, Clark RF, Sorensen BK, Doherty GA, Hansen TM, Frey RR, Sarris KA, Aguirre AL, Shrestha A, Tu N, Woller K, Pliushchev MA, Sweis RF, Cheng M, Wilsbacher JL, Kovar PJ, Guo J, Cheng D, Longenecker KL, Raich D, Korepanova AV, Soni NB, Algire MA, Richardson PL, Marin VL, Badagnani I, Vasudevan A, Buchanan FG, Maag D, Chiang GG, Tse C, Michaelides MR. Curtin ML, et al. Among authors: longenecker kl. Bioorg Med Chem Lett. 2017 Aug 1;27(15):3317-3325. doi: 10.1016/j.bmcl.2017.06.018. Epub 2017 Jun 14. Bioorg Med Chem Lett. 2017. PMID: 28610984
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: longenecker kl. 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
Aryl uracil inhibitors of hepatitis C virus NS5B polymerase: synthesis and characterization of analogs with a fused 5,6-bicyclic ring motif.
Krueger AC, Randolph JT, DeGoey DA, Donner PL, Flentge CA, Hutchinson DK, Liu D, Motter CE, Rockway TW, Wagner R, Beno DW, Koev G, Lim HB, Beyer JM, Mondal R, Liu Y, Kati WM, Longenecker KL, Molla A, Stewart KD, Maring CJ. Krueger AC, et al. Among authors: longenecker kl. Bioorg Med Chem Lett. 2013 Jun 15;23(12):3487-90. doi: 10.1016/j.bmcl.2013.04.057. Epub 2013 May 1. Bioorg Med Chem Lett. 2013. PMID: 23664214
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. Nature. 2020 Feb;578(7794):306-310. doi: 10.1038/s41586-020-1930-8. Epub 2020 Jan 22. Nature. 2020. PMID: 31969702
Structure-based optimization of MurF inhibitors.
Stamper GF, Longenecker KL, Fry EH, Jakob CG, Florjancic AS, Gu YG, Anderson DD, Cooper CS, Zhang T, Clark RF, Cia Y, Black-Schaefer CL, Owen McCall J, Lerner CG, Hajduk PJ, Beutel BA, Stoll VS. Stamper GF, et al. Among authors: longenecker kl. Chem Biol Drug Des. 2006 Jan;67(1):58-65. doi: 10.1111/j.1747-0285.2005.00317.x. Chem Biol Drug Des. 2006. PMID: 16492149
46 results