Sensitivity of NS3 serine proteases from hepatitis C virus genotypes 2 and 3 to the inhibitor BILN 2061

Journal of Virology

Volumn 78, Issue 14, 2004, Pages 7352-7359

  Thibeault, Diane ^a   Bousquet, Christiane ^a   Gingras, Rock ^a   Lagacé, Lisette ^a   Maurice, Roger ^a   White, Peter W ^a   Lamarre, Daniel ^a,b  

^a BOEHRINGER INGELHEIM CANADA LTD   (Canada)

^b CENTRE HOSPITALIER DE L UNIVERSITÉ DE MONTRÉAL   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIVIRUS AGENT; CILUPREVIR; NS3 SERINE PROTEASE; SERINE PROTEINASE; UNCLASSIFIED DRUG;

ARTICLE; CONCENTRATION RESPONSE; DRUG BINDING SITE; DRUG POTENCY; GENETIC VARIABILITY; HEPATITIS C VIRUS; IN VITRO STUDY; NONHUMAN; PRIORITY JOURNAL; SENSITIVITY ANALYSIS; VIRUS GENOME; VIRUS STRAIN;

EID: 3142700044     PISSN: 0022538X     EISSN: None     Source Type: Journal    
DOI: 10.1128/JVI.78.14.7352-7359.2004     Document Type: Article

References (33)

1. Beyer, B. M., R. Zhang, Z. Hong, V. Madison, and B. A. Malcolm. 2001. Effect of naturally occurring active site mutations on hepatitis C virus NS3 protease specificity. Proteins 43:82-88.
2. Bianchi, E., C. Steinkühler, M. Taliani, A. Urbani, R. De Francesco, and A. Pessi. 1996. Synthetic depsipeptide substrates for the assay of human hepatitis C virus protease. Anal. Biochem. 237:239-244.
3. Bodansky, M. 1993. Peptide chemistry, 2nd ed. Springer-Verlag, Berlin, Germany.
4. Di Bisceglie, A. M., and J. H. Hoofnagle. 2002. Optimal therapy of hepatitis C. Hepatology 36:S121-S127.
5. Domingo, E., C. M. Ruiz-Jarabo, S. Sierra, A. Arias, N. Pariente, E. Baranowski, and C. Escarmís. 2002. Emergence and selection of RNA virus variants: memory and extinction. Virus Res. 82:39-44.
6. Drake, J. W., and J. J. Holland. 1999. Mutation rates among RNA viruses. Proc. Natl. Acad. Sci. USA 96:13910-13913.
7. Hoofnagle, J. H. 2002. Course and outcome of hepatitis C. Hepatology 36:S21-S29.
8. Kakiuchi, N., M. Hijikata, Y. Komoda, Y. Tanji, Y. Hirowatari, and K. Shimotohno. 1995. Bacterial expression and analysis of cleavage activity of HCV serine proteinase using recombinant and synthetic substrate. Biochem. Biophys. Res. Commun. 210:1059-1065.
9. Kim, J. L., K. A. Morgenstern, C. Lin, T. Fox, M. D. Dwyer, J. A. Landro, S. P. Chambers, W. Markland, C. A. Lepre, E. T. O'Malley, S. L. Harbeson, C. M. Rice, M. A. Murcko, P. R. Caron, and J. A. Thomson. 1996. Crystal structure of the hepatitis C virus NS3 protease domain complexed with a synthetic NS4A cofactor peptide. Cell 87:343-355.
10. Koch, U., G. Biasiol, M. Brunetti, D. Fattori, M. Pallaoro, and C. Steinkühler. 2001. Role of charged residues in the catalytic mechanism of hepatitis C virus NS3 protease: electrostatic precollision guidance and transilion-state stabilization. Biochemistry 40:631-640.
11. Kolykhalov, A. A., K. Mihalik, S. M. Feinstone, and C. M. Rice. 2000. Hepatitis C virus-encoded enzymatic activities and conserved RNA elements in the 3′ nontranslated region are essential for virus replication in vivo. J. Virol. 74:2046-2051.
12. Lamarre, D., P. C. Anderson, M. Bailey, P. Beaulieu, G. Bolger, P. Bonneau, M. Bös, D. R. Cameron, M. Cartier, M. G. Cordingley, A.-M. Faucher, N. Goudreau, S. Kawai, G. Kukolj, L. Lagacé, S. R. LaPlante, H. Narjes, M.-A. Poupart, J. Rancourt, R. E. Sentjens, R. St. George, B. Simoneau, G. Steinmann, D. Thibeault, Y. S. Tsantrizos, S. M. Weldon, C.-L. Yong, and M. Llinàs-Brunet. 2003. An NS3 protease inhibitor with antiviral proof-of-concept in humans infected with hepatitis C virus. Nature 426:186-189.
13. LaPlante, S. R., D. R. Cameron, N. Aubry, S. Lefebvre, G. Kukolj, R. Maurice, D. Thibeault, D. Lamarre, and M. Llinàs-Brunet. 1999. Solution structure of substrate-based ligands when bound to hepatitis C virus NS3 protease domain. J. Biol. Chem. 274:18618-18624.
14. Lin, C., J. A. Thomson, and C. M. Rice. 1995. A central region in the hepatitis C virus NS4A protein allows formation of an active NS3-NS4A serine proteinase complex in vivo and in vitro. J. Virol. 69:4373-4380.
15. Llinàs-Brunet, M., M. Bailey, R. Déziel, G. Fazal, V. Gorys, S. Goulet, T. Halmos, R. Maurice, M. Poirier, M.-A. Poupart, J. Rancourt, D. Thibeault, D. Wernic, and D. Lamarre. 1998. Studies on the C-terminal of hexapeptide inhibitors of the hepatitis C virus serine protease. Bioorg. Med. Chem. Lett. 8:2719-2724.
16. Llinàs-Brunet, M., M. Bailey, G. Fazal, E. Ghiro, V. Gorys, S. Goulet, T. Halmos, R. Maurice, M. Poirier, M.-A. Poupart, J. Rancourt, D. Thibeault, D. Wernic, and D. Lamarre. 2000. Highly potent and selective peptide-based inhibitors of the hepatitis C virus serine protease: towards smaller inhibitors. Bioorg. Med. Chem. Lett. 10:2267-2270.
17. Llinàs-Brunet, M., M. Bailey, G. Fazal, S. Goulet, T. Halmos, S. R. LaPlante, R. Maurice, M. Poirier, M.-A. Poupart, D. Thibeault, D. Wernic, and D. Lamarre. 1998. Peptide-based inhibitors of the hepatitis C virus serine protease. Bioorg. Med. Chem. Lett. 8:1713-1718.
18. Mondelli, M. U., and E. Silini. 1999. Clinical significance of hepatitis C virus genotypes. J. Hepatol. 31(Suppl. 1):65-70.
19. Muzammil, S., P. Ross, and E. Freire. 2003. A major role for a set of non-active site mutations in the development of HIV-1 protease drug resistance. Biochemistry 42:631-638.
20. Neumann, A. U., N. P. Lam, H. Dahari, D. R. Gretch, T. E. Wiley, T. J. Laydent, and A. S. Perelson. 1998. Hepatitis C viral dynamics in vivo and the antiviral efficacy of interferon-alpha therapy. Science 282:103-107.
21. Pause, A., G. Kukolj, M. Bailey, M. Brault, F. Dô, T. Halmos, L. Lagacé, R. Maurice, M. Marquis, G. McKercher, C. Pellerin, L. Pilote, D. Thibeault, and D. Lamarre. 2003. An NS3 serine protease inhibitor abrogates replication of subgenomic hepatitis C virus RNA. J. Biol. Chem. 278:20374-20380.
22. Pawlotsky, J.-M. 2003. Hepatitis C virus genetic variability: pathogenic and clinical implications. Clin. Liver Dis. 7:45-66.
23. Reed, K. E., and C. M. Rice. 2000. Overview of hepatitis C virus genome structure, polyprotein processing, and protein properties. Curr. Top. Microbiol. Immunol. 242:55-84.
24. Simmonds, P. 1999. Viral heterogeneity of the hepatitis C virus. J. Hepatol. 31(Suppl. 1):54-60.
25. Simmonds, P. 2001. The origin and evolution of hepatitis viruses in humans. J. Gen. Virol. 82:693-712.
26. Steinhühler, C., U. Koch, F. Narjes, and V. G. Matassa. 2001. Hepatitis C virus serine protease inhibitors: current progress and future challenges. Curr. Med. Chem. 8:919-932.
27. Taliani, M., E. Bianchi, F. Narjes, M. Fossatelli, A. Urbani, C. Steinkühler, R. De Francesco, and A. Pessi. 1996. A continuous assay of hepatitis C virus protease based on resonance energy transfer depsipeptide substrates. Anal. Biochem. 240:60-67.
28. Trozzi, C., L. Bartholomew, A. Ceccacci, G. Biasiol, L. Pacini, S. Altamura, F. Narjes, E. Muraglia, G. Paonessa, U. Koch, R. De Francesco, C. Steinkühler, and G. Migliaccio. 2003. In vitro selection and characterization of hepatitis C virus serine protease variants resistant to an active-site peptide inhibitor. J. Virol. 77:3669-3779.
29. Tsantrizos, Y. S., G. Bolger, P. Bonneau, D. R. Cameron, N. Goudreau, G. Kukolj, S. R. LaPlante, M. Llinàs-Brunet, H. Nar, and D. Lamarre. 2003. Macrocyclic inhibitors of the NS3 protease as potential therapeutic agents of hepatitis C virus infection. Angew. Chem. Int. Ed. 42:1355-1360.
30. Tsantrizos, Y. S., D. R. Cameron, A.-M. Faucher, É. Ghiro, N. Goudreau, T. Halmos, and M. Llinàs-Brunet. August 2003. Macrocyclic peptides active against hepatitis C virus. U.S. patent 6,608,027 B1.
31. Webster, G., E. Barnes, D. Brown, and G. Dusheiko. 2000. HCV genotypes-role in pathogenesis of disease and response to therapy. Baíllière's Clin. Gastroenterol. 14:229-240.
32. Wright-Minogue, J., N. Yao, R. Zhang, N. Butkiewicz, B. M. Baroudy, J. Y. N. Lau, and Z. Hong. 2000. Cross-genotypic interaction between hepatitis C virus NS3 protease domains and NS4A cofactors. J. Hepatol. 32:497-504.
33. Yan, Y., Y. Li, S. Munshi, V. Sardana, J. L. Cole, M. Sardana, C. Steinkühler, L. Tomei, R. De Francesco, L. C. Kuo, and Z. Chen. 1998. Complex of NS3 protease and NS4A peptide of BK strain hepatitis C virus: a 2.2 Å resolution structure in a hexagonal crystal form. Protein Sci. 7:837-847.