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Page 1
Discovery and Characterization of Novel Nonsubstrate and Substrate NAMPT Inhibitors.
Wilsbacher JL, Cheng M, Cheng D, Trammell SAJ, Shi Y, Guo J, Koeniger SL, Kovar PJ, He Y, Selvaraju S, Heyman HR, Sorensen BK, Clark RF, Hansen TM, Longenecker KL, Raich D, Korepanova AV, Cepa S, Towne DL, Abraham VC, Tang H, Richardson PL, McLoughlin SM, Badagnani I, Curtin ML, Michaelides MR, Maag D, Buchanan FG, Chiang GG, Gao W, Rosenberg SH, Brenner C, Tse C. Wilsbacher JL, et al. Among authors: longenecker kl. Mol Cancer Ther. 2017 Jul;16(7):1236-1245. doi: 10.1158/1535-7163.MCT-16-0819. Epub 2017 May 3. Mol Cancer Ther. 2017. PMID: 28468779
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
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
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. 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
The HPK1 Inhibitor A-745 Verifies the Potential of Modulating T Cell Kinase Signaling for Immunotherapy.
Malchow S, Korepanova A, Panchal SC, McClure RA, Longenecker KL, Qiu W, Zhao H, Cheng M, Guo J, Klinge KL, Trusk P, Pratt SD, Li T, Kurnick MD, Duan L, Shoemaker AR, Gopalakrishnan SM, Warder SE, Shotwell JB, Lai A, Sun C, Osuma AT, Pappano WN. Malchow S, et al. Among authors: longenecker kl. ACS Chem Biol. 2022 Mar 18;17(3):556-566. doi: 10.1021/acschembio.1c00819. Epub 2022 Feb 21. ACS Chem Biol. 2022. PMID: 35188729
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
Balancing Properties with Carboxylates: A Lead Optimization Campaign for Selective and Orally Active CDK9 Inhibitors.
Tong Y, Florjancic AS, Clark RF, Lai C, Mastracchio A, Zhu GD, Smith ML, Kovar PJ, Shaw B, Albert DH, Qiu W, Longenecker KL, Liu X, Olson AM, Osterling DJ, Tahir SK, Phillips DC, Leverson JD, Souers AJ, Penning TD. Tong Y, et al. Among authors: longenecker kl. ACS Med Chem Lett. 2021 Jun 22;12(7):1108-1115. doi: 10.1021/acsmedchemlett.1c00161. eCollection 2021 Jul 8. ACS Med Chem Lett. 2021. PMID: 34267880 Free PMC article.
46 results