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Discovery of Potent Cyclophilin Inhibitors Based on the Structural Simplification of Sanglifehrin A.
Steadman VA, Pettit SB, Poullennec KG, Lazarides L, Keats AJ, Dean DK, Stanway SJ, Austin CA, Sanvoisin JA, Watt GM, Fliri HG, Liclican AC, Jin D, Wong MH, Leavitt SA, Lee YJ, Tian Y, Frey CR, Appleby TC, Schmitz U, Jansa P, Mackman RL, Schultz BE. Steadman VA, et al. Among authors: schultz be. J Med Chem. 2017 Feb 9;60(3):1000-1017. doi: 10.1021/acs.jmedchem.6b01329. Epub 2017 Jan 31. J Med Chem. 2017. PMID: 28075591
Biochemical characterization and structure determination of a potent, selective antibody inhibitor of human MMP9.
Appleby TC, Greenstein AE, Hung M, Liclican A, Velasquez M, Villaseñor AG, Wang R, Wong MH, Liu X, Papalia GA, Schultz BE, Sakowicz R, Smith V, Kwon HJ. Appleby TC, et al. Among authors: schultz be. J Biol Chem. 2017 Apr 21;292(16):6810-6820. doi: 10.1074/jbc.M116.760579. Epub 2017 Feb 24. J Biol Chem. 2017. PMID: 28235803 Free PMC article.
Discovery of a Potent and Orally Bioavailable Cyclophilin Inhibitor Derived from the Sanglifehrin Macrocycle.
Mackman RL, Steadman VA, Dean DK, Jansa P, Poullennec KG, Appleby T, Austin C, Blakemore CA, Cai R, Cannizzaro C, Chin G, Chiva JC, Dunbar NA, Fliri H, Highton AJ, Hui H, Ji M, Jin H, Karki K, Keats AJ, Lazarides L, Lee YJ, Liclican A, Mish M, Murray B, Pettit SB, Pyun P, Sangi M, Santos R, Sanvoisin J, Schmitz U, Schrier A, Siegel D, Sperandio D, Stepan G, Tian Y, Watt GM, Yang H, Schultz BE. Mackman RL, et al. Among authors: schultz be. J Med Chem. 2018 Nov 8;61(21):9473-9499. doi: 10.1021/acs.jmedchem.8b00802. Epub 2018 Aug 22. J Med Chem. 2018. PMID: 30074795
Discovery of the pan-genotypic hepatitis C virus NS3/4A protease inhibitor voxilaprevir (GS-9857): A component of Vosevi®.
Taylor JG, Zipfel S, Ramey K, Vivian R, Schrier A, Karki KK, Katana A, Kato D, Kobayashi T, Martinez R, Sangi M, Siegel D, Tran CV, Yang ZY, Zablocki J, Yang CY, Wang Y, Wang K, Chan K, Barauskas O, Cheng G, Jin D, Schultz BE, Appleby T, Villaseñor AG, Link JO. Taylor JG, et al. Among authors: schultz be. Bioorg Med Chem Lett. 2019 Aug 15;29(16):2428-2436. doi: 10.1016/j.bmcl.2019.03.037. Epub 2019 Mar 26. Bioorg Med Chem Lett. 2019. PMID: 31133531
Biochemical characterization of tirabrutinib and other irreversible inhibitors of Bruton's tyrosine kinase reveals differences in on - and off - target inhibition.
Liclican A, Serafini L, Xing W, Czerwieniec G, Steiner B, Wang T, Brendza KM, Lutz JD, Keegan KS, Ray AS, Schultz BE, Sakowicz R, Feng JY. Liclican A, et al. Among authors: schultz be. Biochim Biophys Acta Gen Subj. 2020 Apr;1864(4):129531. doi: 10.1016/j.bbagen.2020.129531. Epub 2020 Jan 15. Biochim Biophys Acta Gen Subj. 2020. PMID: 31953125 Free article.
Discovery of Potent and Selective MTH1 Inhibitors for Oncology: Enabling Rapid Target (In)Validation.
Farand J, Kropf JE, Blomgren P, Xu J, Schmitt AC, Newby ZE, Wang T, Murakami E, Barauskas O, Sudhamsu J, Feng JY, Niedziela-Majka A, Schultz BE, Schwartz K, Viatchenko-Karpinski S, Kornyeyev D, Kashishian A, Fan P, Chen X, Lansdon EB, Ports MO, Currie KS, Watkins WJ, Notte GT. Farand J, et al. Among authors: schultz be. ACS Med Chem Lett. 2019 Nov 19;11(3):358-364. doi: 10.1021/acsmedchemlett.9b00420. eCollection 2020 Mar 12. ACS Med Chem Lett. 2019. PMID: 32184970 Free PMC article.
Key Metabolic Enzymes Involved in Remdesivir Activation in Human Lung Cells.
Li R, Liclican A, Xu Y, Pitts J, Niu C, Zhang J, Kim C, Zhao X, Soohoo D, Babusis D, Yue Q, Ma B, Murray BP, Subramanian R, Xie X, Zou J, Bilello JP, Li L, Schultz BE, Sakowicz R, Smith BJ, Shi PY, Murakami E, Feng JY. Li R, et al. Among authors: schultz be. Antimicrob Agents Chemother. 2021 Aug 17;65(9):e0060221. doi: 10.1128/AAC.00602-21. Epub 2021 Aug 17. Antimicrob Agents Chemother. 2021. PMID: 34125594 Free PMC article.
41 results