Naturally occurring substitutions conferring resistance to hepatitis C virus polymerase inhibitors in treatment-naive patients infected with genotypes 1-5

Antiviral Therapy

Volumn 14, Issue 5, 2009, Pages 723-730

  Legrand Abravanel, Florence ^a,b   Henquell, Cécile ^c   Le Guillou Guillemette, Hélène ^d,e   Balan, Viorica ^d,e   Mirand, Audrey ^c   Dubois, Martine ^a,b   Lunel Fabiani, Francoise ^d,e   Payan, Christopher ^f   Izopet, Jacques ^a,b  

^a INSERM   (France)

^b CHU PURPAN   (France)

^c UNIVERSITY HOSPITAL OF CLERMONT FERRAND   (France)

^d ANGERS UNIVERSITY HOSPITAL   (France)

^e UNIVERSITÉ D'ANGERS   (France)

^f BREST UNIVERSITY HOSPITAL   (France)

Author keywords

[No Author keywords available]

Indexed keywords

BENZOFURAN DERIVATIVE; BENZOTHIAZINE DERIVATIVE; CYCLOSPORIN; NONSTRUCTURAL PROTEIN 5B; NUCLEOSIDE DERIVATIVE; RNA DIRECTED DNA POLYMERASE INHIBITOR; THIOPHENE DERIVATIVE;

ANTIVIRAL RESISTANCE; ARTICLE; CONCENTRATION RESPONSE; DRUG EXPOSURE; GENE SEQUENCE; GENOTYPE; HEPATITIS C VIRUS; HUMAN; IC 50; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; VIRAL GENETICS; VIRUS STRAIN;

EID: 69849107011     PISSN: 13596535     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (41)

1. Fried MW, Shiffman ML, Reddy KR, et al. Peginterferon alfa-2a plus ribavirin for chronic hepatitis C virus infection. N Engl J Med 2002; 347:975-982.
2. Manns MP, McHutchison JG, Gordon SC, et al. Peginterferon alfa-2b plus ribavirin compared with interferon alfa-2b plus ribavirin four initial treatment of chronic hepatitis C: a randomised trial. Lancet 2001; 358:958-965.
3. Behrens SE, Tomei L, De Francesco R. Identification and roperties of the RNA-dependent RNA polymerase of hepatitis C virus. EMBO J 1996; 15: 12-22.
4. Watashi K, Ishii N, Hijikata, M, et al. Cyclophilin B is a functional regulator of hepatitis C virus RNA polymerase. Mol Cell 2005; 19:111-122.
5. Lesburg CA, Cable MB, Ferrari E, Hong Z, Mannarino AF, Weber PC. Crystal structure of the RNA-dependent RNA polymerase from hepatitis C virus reveals a fully encircled active site. Nat Struct Biol 1999; 6:937-943.
6. Biswal BK, Cherney, MM, Wang M, et al. Crystal structures of the RNA-dependent RNA polymerase genotype 2a of hepatitis C virus reveal two conformations and suggest mechanisms of inhibition by non-nucleoside inhibitors. J Biol Chem 2005; 280:18202-18210.
7. Lin K, Hazuda DJ, Otto MJ, et al. Initial recommendations for HCV drug resistance analysis: a consensus statement from the HCV Drug Resistance Advisory Board. HEP DART: Frontiers in drug development for viral hepatitis. 9-13 December 2007, Maui, HI, USA. Abstract 28.
8. Harper S, Pacini B, Avolio S, et al. Development and preliminary optimization of indole-N-acetamide inhibitors of hepatitis C virus NS5B polymerase. J Med Chem 2005; 48: 1314-1317.
9. Tomei L, Altamura S, Bartholomew L, et al. Mechanism of action and antiviral activity of benzimidazole-based allosteric inhibitors of the hepatitis C virus RNA-dependent RNA polymerase. J Virol 2003; 77:13225-13231.
10. Chan L, Reddy TJ, Proulx M, et al. Identification of N,N-disubstituted phenylalanines as a novel class of inhibitors of hepatitis C NS5B polymerase. J Med Chem 2003; 46:1283-1285.
11. Gopalsamy A, Lim K, Ciszewski G, et al. Discovery of pyrano[3,4-b]indoles as potent and selective HCV NS5B polymerase inhibitors. J Med Chem 2004; 47:6603-6608.
12. Li H, Tatlock J, Linton A, et al. Identification and structure-based optimization of novel dihydropyrones as potent HCV RNA polymerase inhibitors. Bioorg Med Chem Lett 2006; 16:4834-4838.
13. Dhanak D, Duffy KJ, Johnston VK, et al. Identification and biological characterization of heterocyclic inhibitors of the hepatitis C virus RNA-dependent RNA polymerase. J Biol Chem 2002; 277:38322-38327.
14. Pfefferkorn JA, Greene ML, Nugent RA, et al. Inhibitors of HCV NS5B polymerase. Part 1: evaluation of the southern region of (2Z)-2-(benzoylamino)-3-(5-phenyl-2-furyl)acrylic acid. Bioorg Med Chem Lett 2005; 15:2481-2486.
15. Pfefferkorn JA, Nugent R, Gross RJ, et al. Inhibitors of HCV NS5B polymerase. Part 2: evaluation of the northern region of (2Z)-2-benzoylamino-3-(4-phenoxy-phenyl)-acrylic acid. Bioorg Med Chem Lett 2005; 15:2812-2818.
16. Gopalsamy A, Aplasca A, Ciszewski G, et al. Design and synthesis of 3,4-dihydro-1H-[1]-benzothieno[2,3-c]pyran and 3,4-dihydro-1H-pyrano[3,4-b]benzofuran derivatives as non-nucleoside inhibitors of HCV NS5B RNA dependent RNA polymerase. Bioorg Med Chem Lett 2006; 16:457-460.
17. Hopkins S, Scorneaux B, Huang Z, Murray MG, Harris R. The genetic and biochemical basis for resistance to SCY-635. 59th Annual Meeting of the American Association for the Study of the Liver Diseases. 31 October - 4 November 2008, San Francisco, CA, USA. Abstract 1814.
18. Peel M, Harris R, Huang Z, et al. The discovery of novel, non-immunosuppressive cyclosporin ethers, and thioethers with potent HCV activity. 59th Annual Meeting of the American Association for the Study of the Liver Diseases. 31 October - 4 November 2008, San Francisco, CA, USA. Abstract 1915.
19. Paeshuyse J, Kaul A, De Clercq E, et al. The non-immunosuppressive cyclosporin DEBIO-025 is a potent inhibitor of hepatitis C virus replication in vitro. Hepatology 2006; 43:761-770.
20. Ma S, Boerner JE, TiongYip C, et al. NIM811, a cyclophilin inhibitor, exhibits potent in vitro activity against hepatitis C virus alone or in combination with alpha interferon. Antimicrob Agents Chemother 2006; 50:2976-2982.
21. Kuntzen T, Timm J, Berical A, et al. Naturally occurring dominant resistance mutations to hepatitis C virus protease and polymerase inhibitors in treatment-naive patients. Hepatology 2008; 48:1769-1778.
22. Le Pogam S, Seshaadri A, Kosaka A, et al. Existence of hepatitis C virus NS5B variants naturally resistant to non-nucleoside, but not to nucleoside, polymerase inhibitors amon untreated patients. J Antimicrob Chemother 2008; 61:1205-1216.
23. Sandres-Saune K, Deny P, Pasquier C, Thibaut V, Duverlie G, Izopet J. Determining hepatitis C genotype by analyzing the sequence of the NS5b region. J Virol Methods 2001; 109:187-193.
24. Smith DB, Martin JA, Klumpp K, et al. Design, synthesis, and antiviral properties of 4′-substituted ribonucleosides as inhibitors of hepatitis C virus replication: the discovery of R1479. Bioorg Med Chem Lett 2007; 17:2570-2576.
25. Le Pogam S, Jiang WR, Leveque V, et al. In vitro selected Con1 subgenomic replicons resistant to 2′-C-methyl-cytidine or to R1479 show lack of cross resistance. Virology 2006; 351:349-359.
26. Murakami E, Bao H, Ramesh M, et al. Mechanism of activation of β-D-2′-deoxy-2′-fluoro-2′-C-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. Antimicrob Agents Chemother 2007; 51:503-509.
27. Pawlotsky JM, Chevaliez S, McHutchison JG. The hepatitis C virus life cycle as a target for new antiviral therapies. Gastroenterology 2007; 132:1979-1998.
28. Kukolj G, McGibbon GA, McKercher G, et al. Binding site characterization ana resistance to a class of non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase. J Biol Chem 2005; 280:39260-39267.
29. Marquis M, Deterding K, Erhardt A, et al. Genotypic and phenotypic analysis of hepatitis C virus NS5B polymerase variants to BILB-1941 inhibition. 59th Annual Meeting of the American Association for the Study of the Liver Diseases. 31 October - 4 November 2008, San Francisco, CA, USA. Abstract 1897.
30. Le Pogam S, Kang H, Harris SF, et al. Selection and characterization of replicon variants dually resistant to thumb- and palm-binding nonnucleoside polymerase inhibitors of the hepatitis C virus. J Virol 2006; 80:6146-6154.
31. Herlihy KJ, Graham JP, Kumpf R, Patick AK, Duggal R, Shi ST. Development of intergenotypic chimeric replicons to determine the broad-spectrum antiviral activities of hepatitis C virus polymerase inhibitors. Antimicrob Agents Chemother 2008; 52:3523-3531.
32. Howe AY, Cheng H, Thompson I, et al. Molecular mechanism of a thumb domain hepatitis C virus nonnucleoside RNA-dependent RNA polymerase inhibitor. Antimicrob Agents Chemother 2006; 50:4103-4113.
33. Shi ST, Herlihy KJ, Graham JP, et al. In vitro resistance study of AG-021541, a nove nonnucleoside inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. Antimicrob Agents Chemother 2008; 52:675-683.
34. Mo H, Lu L, Pilot-Matias T, et al. Mutations conferring resistance to a hepatitis C virus (HCV) RNA-dependent RNA polymerase inhibitor alone or in combination with an HCV serine protease inhibitor in vitro. Antimicrob Agents Chemother 2005; 49:4305-4314.
35. Lu L, Dekhtyar T, Masse S, et al. Identification and characterization of mutations conferring resistance to an HCV RNA-dependent RNA polymerase inhibitor in vitro. Antiviral Res 2007; 76:93-97.
36. Howe AY, Cheng H, Johann S, et al. Molecular mechanism of hepatitis C virus replicon variants with reduced susceptibility to a benzofuran inhibitor, HCV-796. Antimicrob Agents Chemother 2008; 52:3327-3338.
37. Fernandes F, Poole DS, Hoover S, et al. Sensitivity of hepatitis C virus to cyclosporine A depends on nonstructural proteins NS5A and NS5B. Hepatology 2007; 46:1026-1033.
38. Robida JM, Netson HB, Liu Z, Tanp H. Characterization of hepatitis C virus subgenomic replicon resistance to cyclosporine in vitro. J Virol 2007; 81:5829-5840.
39. Payan C, Roudot-Thoraval F, Marcellin P, et al. Changing of hepatitis C virus genotype patterns in France at the beginning the third millenium: the GEMHEP GenoCII Study. J Viral Hepat 2005; 12:405-413.
40. Pauwels F, Mostmans W, Quirynen LM, et al. Binding-site identification and genotypic profiling of hepatitis C virus polymerase inhibitors. J Virol 2007; 81:6909-6919.
41. Bartels DJ, Zhou Y, Zhang EZ, et al. Natural prevalence of hepatitis C virus variants with decreased sensitivity to NS3.4A protease inhibitors in treatment-naive subjects. J Infect Dis 2008; 198:800-807.