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In vitro resistance studies of hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061: structural analysis indicates different resistance mechanisms.
Lin C, Lin K, Luong YP, Rao BG, Wei YY, Brennan DL, Fulghum JR, Hsiao HM, Ma S, Maxwell JP, Cottrell KM, Perni RB, Gates CA, Kwong AD. Lin C, et al. Among authors: wei yy. J Biol Chem. 2004 Apr 23;279(17):17508-14. doi: 10.1074/jbc.M313020200. Epub 2004 Feb 6. J Biol Chem. 2004. PMID: 14766754 Free article.
Inhibitors of hepatitis C virus NS3.4A protease 1. Non-charged tetrapeptide variants.
Perni RB, Britt SD, Court JC, Courtney LF, Deininger DD, Farmer LJ, Gates CA, Harbeson SL, Kim JL, Landro JA, Levin RB, Luong YP, O'Malley ET, Pitlik J, Rao BG, Schairer WC, Thomson JA, Tung RD, Van Drie JH, Wei Y. Perni RB, et al. Bioorg Med Chem Lett. 2003 Nov 17;13(22):4059-63. doi: 10.1016/j.bmcl.2003.08.050. Bioorg Med Chem Lett. 2003. PMID: 14592508
Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization.
Perni RB, Pitlik J, Britt SD, Court JJ, Courtney LF, Deininger DD, Farmer LJ, Gates CA, Harbeson SL, Levin RB, Lin C, Lin K, Moon YC, Luong YP, O'Malley ET, Rao BG, Thomson JA, Tung RD, Van Drie JH, Wei Y. Perni RB, et al. Bioorg Med Chem Lett. 2004 Mar 22;14(6):1441-6. doi: 10.1016/j.bmcl.2004.01.022. Bioorg Med Chem Lett. 2004. PMID: 15006379
Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease.
Perni RB, Almquist SJ, Byrn RA, Chandorkar G, Chaturvedi PR, Courtney LF, Decker CJ, Dinehart K, Gates CA, Harbeson SL, Heiser A, Kalkeri G, Kolaczkowski E, Lin K, Luong YP, Rao BG, Taylor WP, Thomson JA, Tung RD, Wei Y, Kwong AD, Lin C. Perni RB, et al. Antimicrob Agents Chemother. 2006 Mar;50(3):899-909. doi: 10.1128/AAC.50.3.899-909.2006. Antimicrob Agents Chemother. 2006. PMID: 16495249 Free PMC article.
Novel dual-targeting benzimidazole urea inhibitors of DNA gyrase and topoisomerase IV possessing potent antibacterial activity: intelligent design and evolution through the judicious use of structure-guided design and structure-activity relationships.
Charifson PS, Grillot AL, Grossman TH, Parsons JD, Badia M, Bellon S, Deininger DD, Drumm JE, Gross CH, LeTiran A, Liao Y, Mani N, Nicolau DP, Perola E, Ronkin S, Shannon D, Swenson LL, Tang Q, Tessier PR, Tian SK, Trudeau M, Wang T, Wei Y, Zhang H, Stamos D. Charifson PS, et al. J Med Chem. 2008 Sep 11;51(17):5243-63. doi: 10.1021/jm800318d. Epub 2008 Aug 9. J Med Chem. 2008. PMID: 18690678
337 results