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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.
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
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: perni rb. 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 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
Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants.
Perni RB, Farmer LJ, Cottrell KM, Court JJ, Courtney LF, Deininger DD, Gates CA, Harbeson SL, Kim JL, Lin C, Lin K, Luong YP, Maxwell JP, Murcko MA, Pitlik J, Rao BG, Schairer WC, Tung RD, Van Drie JH, Wilson K, Thomson JA. Perni RB, et al. Bioorg Med Chem Lett. 2004 Apr 19;14(8):1939-42. doi: 10.1016/j.bmcl.2004.01.078. Bioorg Med Chem Lett. 2004. PMID: 15050632
35 results