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Page 1
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: panchal sc. 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
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: panchal sc. 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
Fragment-Based Discovery of an Apolipoprotein E4 (apoE4) Stabilizer.
Petros AM, Korepanova A, Jakob CG, Qiu W, Panchal SC, Wang J, Dietrich JD, Brewer JT, Pohlki F, Kling A, Wilcox K, Lakics V, Bahnassawy L, Reinhardt P, Partha SK, Bodelle PM, Lake M, Charych EI, Stoll VS, Sun C, Mohler EG. Petros AM, et al. Among authors: panchal sc. J Med Chem. 2019 Apr 25;62(8):4120-4130. doi: 10.1021/acs.jmedchem.9b00178. Epub 2019 Apr 12. J Med Chem. 2019. PMID: 30933499
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: panchal sc. 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
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: panchal sc. 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
Identification and structure-based drug design of cell-active inhibitors of interleukin 17A at a novel C-terminal site.
Goedken ER, Argiriadi MA, Dietrich JD, Petros AM, Krishnan N, Panchal SC, Qiu W, Wu H, Zhu H, Adams AM, Bodelle PM, Goguen L, Richardson PL, Slivka PF, Srikumaran M, Upadhyay AK, Wu B, Judge RA, Vasudevan A, Gopalakrishnan SM, Cox PB, Stoll VS, Sun C. Goedken ER, et al. Among authors: panchal sc. Sci Rep. 2022 Aug 26;12(1):14561. doi: 10.1038/s41598-022-18760-1. Sci Rep. 2022. PMID: 36028520 Free PMC article.
The EED protein-protein interaction inhibitor A-395 inactivates the PRC2 complex.
He Y, Selvaraju S, Curtin ML, Jakob CG, Zhu H, Comess KM, Shaw B, The J, Lima-Fernandes E, Szewczyk MM, Cheng D, Klinge KL, Li HQ, Pliushchev M, Algire MA, Maag D, Guo J, Dietrich J, Panchal SC, Petros AM, Sweis RF, Torrent M, Bigelow LJ, Senisterra G, Li F, Kennedy S, Wu Q, Osterling DJ, Lindley DJ, Gao W, Galasinski S, Barsyte-Lovejoy D, Vedadi M, Buchanan FG, Arrowsmith CH, Chiang GG, Sun C, Pappano WN. He Y, et al. Among authors: panchal sc. Nat Chem Biol. 2017 Apr;13(4):389-395. doi: 10.1038/nchembio.2306. Epub 2017 Jan 30. Nat Chem Biol. 2017. PMID: 28135237
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: panchal sc. Nature. 2020 Feb;578(7794):306-310. doi: 10.1038/s41586-020-1930-8. Epub 2020 Jan 22. Nature. 2020. PMID: 31969702
33 results