-
1
-
-
57049161283
-
Enhanced antiviral efficacy for valopicitabine (NM283) plus Peg-interferon in hepatitis C patients with HCV genotype-1 infection: Results of a phase IIa multicenter trial, abstr. LB03. Abstr
-
April
-
Afdhal, N., M. Rodriguez-Torres, E. Lawitz, E. Godofsky, G. Chao, B. Fielman, S. Knox, and N. Brown. 2005. Enhanced antiviral efficacy for valopicitabine (NM283) plus Peg-interferon in hepatitis C patients with HCV genotype-1 infection: results of a phase IIa multicenter trial, abstr. LB03. Abstr. 40th Annu. Meet. Eur. Assoc. Study Liver, Paris, France, 13 to 17 April, 2005.
-
(2005)
40th Annu. Meet. Eur. Assoc. Study Liver, Paris, France, 13 to 17
-
-
Afdhal, N.1
Rodriguez-Torres, M.2
Lawitz, E.3
Godofsky, E.4
Chao, G.5
Fielman, B.6
Knox, S.7
Brown, N.8
-
2
-
-
33748617118
-
Finger loop inhibitors of the HCV NS5B polymerase: Discovery and prospects for new HCV therapy
-
Beaulieu, P. L. 2006. Finger loop inhibitors of the HCV NS5B polymerase: discovery and prospects for new HCV therapy. Curr. Opin. Drug Discov. Devel. 9:618-626.
-
(2006)
Curr. Opin. Drug Discov. Devel
, vol.9
, pp. 618-626
-
-
Beaulieu, P.L.1
-
3
-
-
34547618419
-
Non-nucleoside inhibitors of the HCV NS5B polymerase: Progress in the discovery and development of novel agents for the treatment of HCV infections
-
Beaulieu, P. L. 2007. Non-nucleoside inhibitors of the HCV NS5B polymerase: progress in the discovery and development of novel agents for the treatment of HCV infections. Curr. Opin. Investig. Drugs 8:614-634.
-
(2007)
Curr. Opin. Investig. Drugs
, vol.8
, pp. 614-634
-
-
Beaulieu, P.L.1
-
4
-
-
10744227250
-
Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: Discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency
-
Beaulieu, P. L., M. Bos, Y. Bousquet, P. DeRoy, G. Fazal, J. Gauthier, J. Gillard, S. Goulet, G. McKercher, M. A. Poupart, S. Valois, and G. Kukolj. 2004. Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency. Bioorg. Med. Chem. Lett. 14:967-971.
-
(2004)
Bioorg. Med. Chem. Lett
, vol.14
, pp. 967-971
-
-
Beaulieu, P.L.1
Bos, M.2
Bousquet, Y.3
DeRoy, P.4
Fazal, G.5
Gauthier, J.6
Gillard, J.7
Goulet, S.8
McKercher, G.9
Poupart, M.A.10
Valois, S.11
Kukolj, G.12
-
5
-
-
33747364216
-
Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: From benzimidazole to indole scaffolds
-
Beaulieu, P. L., J. Gillard, D. Bykowski, C. Brochu, N. Dansereau, J. S. Duceppe, B. Hache, A. Jakalian, L. Lagace, S. LaPlante, G. McKercher, E. Moreau, S. Perreault, T. Stammers, L. Thauvette, J. Warrington, and G. Kukolj. 2006. Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: from benzimidazole to indole scaffolds. Bioorg. Med. Chem. Lett. 16:4987-4993.
-
(2006)
Bioorg. Med. Chem. Lett
, vol.16
, pp. 4987-4993
-
-
Beaulieu, P.L.1
Gillard, J.2
Bykowski, D.3
Brochu, C.4
Dansereau, N.5
Duceppe, J.S.6
Hache, B.7
Jakalian, A.8
Lagace, L.9
LaPlante, S.10
McKercher, G.11
Moreau, E.12
Perreault, S.13
Stammers, T.14
Thauvette, L.15
Warrington, J.16
Kukolj, G.17
-
6
-
-
11144231108
-
Inhibitors of the HCV NS5B polymerase: New hope for the treatment of hepatitis C infections
-
Beaulieu, P. L., and Y. S. Tsantrizos. 2004. Inhibitors of the HCV NS5B polymerase: new hope for the treatment of hepatitis C infections. Curr. Opin. Investig. Drugs 5:838-850.
-
(2004)
Curr. Opin. Investig. Drugs
, vol.5
, pp. 838-850
-
-
Beaulieu, P.L.1
Tsantrizos, Y.S.2
-
7
-
-
0037809239
-
Inhibition of hepatitis C virus RNA replication by 2′-modified nucleoside analogs
-
Carroll, S. S., J. E. Tomassini, M. Bosserman, K. Getty, M. W. Stahlhut, A. B. Eldrup, B. Bhat, D. Hall, A. L. Simcoe, R. LaFemina, C. A. Rutkowski, B. Wolanski, Z. Yang, G. Migliaccio, F. R. De, L. C. Kuo, M. MacCoss, and D. B. Olsen. 2003. Inhibition of hepatitis C virus RNA replication by 2′-modified nucleoside analogs. J. Biol. Chem. 278:11979-11984.
-
(2003)
J. Biol. Chem
, vol.278
, pp. 11979-11984
-
-
Carroll, S.S.1
Tomassini, J.E.2
Bosserman, M.3
Getty, K.4
Stahlhut, M.W.5
Eldrup, A.B.6
Bhat, B.7
Hall, D.8
Simcoe, A.L.9
LaFemina, R.10
Rutkowski, C.A.11
Wolanski, B.12
Yang, Z.13
Migliaccio, G.14
De, F.R.15
Kuo, L.C.16
MacCoss, M.17
Olsen, D.B.18
-
8
-
-
1642534328
-
Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 1: Sulfonamides
-
Chan, L., S. K. Das, T. J. Reddy, C. Poisson, M. Proulx, O. Pereira, M. Courchesne, C. Roy, W. Wang, A. Siddiqui, C. G. Yannopoulos, N. Nguyen-Ba, D. Labrecque, R. Bethell, M. Hamel, P. Courtemanche-Asselin, L. L'Heureux, M. David, O. Nicolas, S. Brunette, D. Bilimoria, and J. Bedard. 2004. Discovery of thiophene-2-carboxylic acids as potent inhibitors of HCV NS5B polymerase and HCV subgenomic RNA replication. Part 1: sulfonamides. Bioorg. Med. Chem. Lett. 14:793-796.
-
(2004)
Bioorg. Med. Chem. Lett
, vol.14
, pp. 793-796
-
-
Chan, L.1
Das, S.K.2
Reddy, T.J.3
Poisson, C.4
Proulx, M.5
Pereira, O.6
Courchesne, M.7
Roy, C.8
Wang, W.9
Siddiqui, A.10
Yannopoulos, C.G.11
Nguyen-Ba, N.12
Labrecque, D.13
Bethell, R.14
Hamel, M.15
Courtemanche-Asselin, P.16
L'Heureux, L.17
David, M.18
Nicolas, O.19
Brunette, S.20
Bilimoria, D.21
Bedard, J.22
more..
-
9
-
-
23944469297
-
Design, synthesis, and antiviral activity of 2′-deoxy-2′-fluoro- 2′-C-methylcytidine, a potent inhibitor of hepatitis C virus replication
-
Clark, J. L., L. Hollecker, J. C. Mason, L. J. Stuyver, P. M. Tharnish, S. Lostia, T. R. McBrayer, R. F. Schinazi, K. A. Watanabe, M. J. Otto, P. A. Furman, W. J. Stec, S. E. Patterson, and K. W. Pankiewicz. 2005. Design, synthesis, and antiviral activity of 2′-deoxy-2′-fluoro- 2′-C-methylcytidine, a potent inhibitor of hepatitis C virus replication. J. Med. Chem. 48:5504-5508.
-
(2005)
J. Med. Chem
, vol.48
, pp. 5504-5508
-
-
Clark, J.L.1
Hollecker, L.2
Mason, J.C.3
Stuyver, L.J.4
Tharnish, P.M.5
Lostia, S.6
McBrayer, T.R.7
Schinazi, R.F.8
Watanabe, K.A.9
Otto, M.J.10
Furman, P.A.11
Stec, W.J.12
Patterson, S.E.13
Pankiewicz, K.W.14
-
11
-
-
0037064091
-
-
Dhanak, D., K. J. Duffy, V. K. Johnston, J. Lin-Goerke, M. Darcy, A. N. Shaw, B. Gu, C. Silverman, A. T. Gates, M. R. Nonnemacher, D. L. Earnshaw, D. J. Casper, A. Kaura, A. Baker, C. Greenwood, L. L. Gutshall, D. Maley, A. DelVecchio, R. Macarron, G. A. Hofmann, Z. Alnoah, H. Y. Cheng, G. Chan, S. Khandekar, R. M. Keenan, and R. T. Sarisky. 2002. Identification and biological characterization of heterocyclic inhibitors of the hepatitis C virus RNA-dependent RNA polymerase. J. Biol. Chem. 277:38322-38327.
-
Dhanak, D., K. J. Duffy, V. K. Johnston, J. Lin-Goerke, M. Darcy, A. N. Shaw, B. Gu, C. Silverman, A. T. Gates, M. R. Nonnemacher, D. L. Earnshaw, D. J. Casper, A. Kaura, A. Baker, C. Greenwood, L. L. Gutshall, D. Maley, A. DelVecchio, R. Macarron, G. A. Hofmann, Z. Alnoah, H. Y. Cheng, G. Chan, S. Khandekar, R. M. Keenan, and R. T. Sarisky. 2002. Identification and biological characterization of heterocyclic inhibitors of the hepatitis C virus RNA-dependent RNA polymerase. J. Biol. Chem. 277:38322-38327.
-
-
-
-
12
-
-
33845247515
-
General catalytic deficiency of hepatitis C virus RNA polymerase with an S282T mutation and mutually exclusive resistance towards 2′-modified nucleotide analogues
-
Dutartre, H., C. Bussetta, J. Boretto, and B. Canard. 2006. General catalytic deficiency of hepatitis C virus RNA polymerase with an S282T mutation and mutually exclusive resistance towards 2′-modified nucleotide analogues. Antimicrob. Agents Chemother. 50:4161-4169.
-
(2006)
Antimicrob. Agents Chemother
, vol.50
, pp. 4161-4169
-
-
Dutartre, H.1
Bussetta, C.2
Boretto, J.3
Canard, B.4
-
13
-
-
34247565001
-
Antiviral activity of telaprevir (VX-950) and peginterferon alfa-2a in patients with hepatitis C
-
Forestier, N., H. W. Reesink, C. J. Weegink, L. McNair, T. L. Kieffer, H. M. Chu, S. Purdy, P. L. Jansen, and S. Zeuzem. 2007. Antiviral activity of telaprevir (VX-950) and peginterferon alfa-2a in patients with hepatitis C. Hepatology 46:640-648.
-
(2007)
Hepatology
, vol.46
, pp. 640-648
-
-
Forestier, N.1
Reesink, H.W.2
Weegink, C.J.3
McNair, L.4
Kieffer, T.L.5
Chu, H.M.6
Purdy, S.7
Jansen, P.L.8
Zeuzem, S.9
-
14
-
-
0034773129
-
Advances in therapy for chronic hepatitis C
-
Fried, M. W. 2001. Advances in therapy for chronic hepatitis C. Clin. Liver Dis. 5:1009-1023.
-
(2001)
Clin. Liver Dis
, vol.5
, pp. 1009-1023
-
-
Fried, M.W.1
-
15
-
-
0037179698
-
Peginterferon alfa-2a plus ribavirin for chronic hepatitis C virus infection
-
Fried, M. W., M. L. Shiffman, K. R. Reddy, C. Smith, G. Marinos, F. L. Goncales, Jr., D. Haussinger, M. Diago, G. Carosi, D. Dhumeaux, A. Craxi, A. Lin, J. Hoffman, and J. Yu. 2002. Peginterferon alfa-2a plus ribavirin for chronic hepatitis C virus infection. N. Engl. J. Med. 347:975-982.
-
(2002)
N. Engl. J. Med
, vol.347
, pp. 975-982
-
-
Fried, M.W.1
Shiffman, M.L.2
Reddy, K.R.3
Smith, C.4
Marinos, G.5
Goncales Jr., F.L.6
Haussinger, D.7
Diago, M.8
Carosi, G.9
Dhumeaux, D.10
Craxi, A.11
Lin, A.12
Hoffman, J.13
Yu, J.14
-
16
-
-
2942635076
-
Differences in epidemiology, liver disease and treatment response among HCV genotypes
-
Hadziyannis, S. J., and J. S. Koskinas. 2004. Differences in epidemiology, liver disease and treatment response among HCV genotypes. Hepatol. Res. 29:129-135.
-
(2004)
Hepatol. Res
, vol.29
, pp. 129-135
-
-
Hadziyannis, S.J.1
Koskinas, J.S.2
-
17
-
-
22244435560
-
Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase
-
Harper, S., S. Avolio, B. Pacini, F. M. Di, S. Altamura, L. Tomei, G. Paonessa, M. S. Di, A. Carfi, C. Giuliano, J. Padron, F. Bonelli, G. Migliaccio, F. R. De, R. Laufer, M. Rowley, and F. Narjes. 2005. Potent inhibitors of subgenomic hepatitis C virus RNA replication through optimization of indole-N-acetamide allosteric inhibitors of the viral NS5B polymerase. J. Med. Chem. 48:4547-4557.
-
(2005)
J. Med. Chem
, vol.48
, pp. 4547-4557
-
-
Harper, S.1
Avolio, S.2
Pacini, B.3
Di, F.M.4
Altamura, S.5
Tomei, L.6
Paonessa, G.7
Di, M.S.8
Carfi, A.9
Giuliano, C.10
Padron, J.11
Bonelli, F.12
Migliaccio, G.13
De, F.R.14
Laufer, R.15
Rowley, M.16
Narjes, F.17
-
18
-
-
9644290930
-
-
Howe, A. Y., J. Bloom, C. J. Baldick, C. A. Benetatos, H. Cheng, J. S. Christensen, S. K. Chunduru, G. A. Coburn, B. Feld, A. Gopalsamy, W. P. Gorczyca, S. Herrmann, S. Johann, X. Jiang, M. L. Kimberland, G. Krisnamurthy, M. Olson, M. Orlowski, S. Swanberg, I. Thompson, M. Thorn, V. A. Del, D. C. Young, Z. M. van, J. W. Ellingboe, J. Upeslacis, M. Collett, T. S. Mansour, and J. F. O'Connell. 2004. Novel nonnucleoside inhibitor of hepatitis C virus RNA-dependent RNA polymerase. Antimicrob. Agents Chemother. 48:4813-4821.
-
Howe, A. Y., J. Bloom, C. J. Baldick, C. A. Benetatos, H. Cheng, J. S. Christensen, S. K. Chunduru, G. A. Coburn, B. Feld, A. Gopalsamy, W. P. Gorczyca, S. Herrmann, S. Johann, X. Jiang, M. L. Kimberland, G. Krisnamurthy, M. Olson, M. Orlowski, S. Swanberg, I. Thompson, M. Thorn, V. A. Del, D. C. Young, Z. M. van, J. W. Ellingboe, J. Upeslacis, M. Collett, T. S. Mansour, and J. F. O'Connell. 2004. Novel nonnucleoside inhibitor of hepatitis C virus RNA-dependent RNA polymerase. Antimicrob. Agents Chemother. 48:4813-4821.
-
-
-
-
19
-
-
33845251587
-
Molecular mechanism of a thumb domain hepatitis C virus nonnucleoside RNA-dependent RNA polymerase inhibitor
-
Howe, A. Y., H. Cheng, I. Thompson, S. K. Chunduru, S. Herrmann, J. O'Connell, A. Agarwal, R. Chopra, and A. M. Del Vecchio. 2006. Molecular mechanism of a thumb domain hepatitis C virus nonnucleoside RNA-dependent RNA polymerase inhibitor. Antimicrob. Agents Chemother. 50: 4103-4113.
-
(2006)
Antimicrob. Agents Chemother
, vol.50
, pp. 4103-4113
-
-
Howe, A.Y.1
Cheng, H.2
Thompson, I.3
Chunduru, S.K.4
Herrmann, S.5
O'Connell, J.6
Agarwal, A.7
Chopra, R.8
Del Vecchio, A.M.9
-
20
-
-
34548758435
-
Telaprevir and pegylated interferon-alpha-2a inhibit wild-type and resistant genotype 1 hepatitis C virus replication in patients
-
Kieffer, T. L., C. Sarrazin, J. S. Miller, M. W. Welker, N. Forestier, H. W. Reesink, A. D. Kwong, and S. Zeuzem. 2007. Telaprevir and pegylated interferon-alpha-2a inhibit wild-type and resistant genotype 1 hepatitis C virus replication in patients. Hepatology 46:631-639.
-
(2007)
Hepatology
, vol.46
, pp. 631-639
-
-
Kieffer, T.L.1
Sarrazin, C.2
Miller, J.S.3
Welker, M.W.4
Forestier, N.5
Reesink, H.W.6
Kwong, A.D.7
Zeuzem, S.8
-
21
-
-
38349194473
-
2′-Deoxy-4′-azido nucleoside analogs are highly potent inhibitors of hepatitis C virus replication despite the lack of 2′-alpha-hydroxyl groups
-
Klumpp, K., G. Kalayanov, H. Ma, P. S. Le, V. Leveque, W. R. Jiang, N. Inocencio, W. A. De, S. Rajyaguru, E. Tai, S. Chanda, M. R. Irwin, C. Sund, A. Winqist, T. Maltseva, S. Eriksson, E. Usova, M. Smith, A. Alker, I. Najera, N. Cammack, J. A. Martin, N. G. Johansson, and D. B. Smith. 2008. 2′-Deoxy-4′-azido nucleoside analogs are highly potent inhibitors of hepatitis C virus replication despite the lack of 2′-alpha-hydroxyl groups. J. Biol. Chem. 283:2167-2175.
-
(2008)
J. Biol. Chem
, vol.283
, pp. 2167-2175
-
-
Klumpp, K.1
Kalayanov, G.2
Ma, H.3
Le, P.S.4
Leveque, V.5
Jiang, W.R.6
Inocencio, N.7
De, W.A.8
Rajyaguru, S.9
Tai, E.10
Chanda, S.11
Irwin, M.R.12
Sund, C.13
Winqist, A.14
Maltseva, T.15
Eriksson, S.16
Usova, E.17
Smith, M.18
Alker, A.19
Najera, I.20
Cammack, N.21
Martin, J.A.22
Johansson, N.G.23
Smith, D.B.24
more..
-
22
-
-
33645232568
-
The novel nucleoside analog R1479 (4′-azidocytidine) is a potent inhibitor of NS5B-dependent RNA synthesis and hepatitis C virus replication in cell culture
-
Klumpp, K., V. Leveque, P. S. Le, H. Ma, W. R. Jiang, H. Kang, C. Granycome, M. Singer, C. Laxton, J. Q. Hang, K. Sarma, D. B. Smith, D. Heindl, C. J. Hobbs, J. H. Merrett, J. Symons, N. Cammack, J. A. Martin, R. Devos, and I. Najera. 2006. The novel nucleoside analog R1479 (4′-azidocytidine) is a potent inhibitor of NS5B-dependent RNA synthesis and hepatitis C virus replication in cell culture. J. Biol. Chem. 281:3793-3799.
-
(2006)
J. Biol. Chem
, vol.281
, pp. 3793-3799
-
-
Klumpp, K.1
Leveque, V.2
Le, P.S.3
Ma, H.4
Jiang, W.R.5
Kang, H.6
Granycome, C.7
Singer, M.8
Laxton, C.9
Hang, J.Q.10
Sarma, K.11
Smith, D.B.12
Heindl, D.13
Hobbs, C.J.14
Merrett, J.H.15
Symons, J.16
Cammack, N.17
Martin, J.A.18
Devos, R.19
Najera, I.20
more..
-
23
-
-
33744910421
-
In vitro selected Con1 subgenomic replicons resistant to 2′-C-methyl-cytidine or to R1479 show lack of cross resistance
-
Le Pogam, S., W. R. Jiang, V. Leveque, S. Rajyaguru, H. Ma, H. Kang, S. Jiang, M. Singer, S. Ali, K. Klumpp, D. Smith, J. Symons, N. Cammack, and I. Najera. 2006. In vitro selected Con1 subgenomic replicons resistant to 2′-C-methyl-cytidine or to R1479 show lack of cross resistance. Virology 351:349-359.
-
(2006)
Virology
, vol.351
, pp. 349-359
-
-
Le Pogam, S.1
Jiang, W.R.2
Leveque, V.3
Rajyaguru, S.4
Ma, H.5
Kang, H.6
Jiang, S.7
Singer, M.8
Ali, S.9
Klumpp, K.10
Smith, D.11
Symons, J.12
Cammack, N.13
Najera, I.14
-
24
-
-
33744930847
-
Selection and characterization of replicon variants dually resistant to thumb- and palm-binding nonnucleoside polymerase inhibitors of the hepatitis C virus
-
Le Pogam, S., H. Kang, S. F. Harris, V. Leveque, A. M. Giannetti, S. Ali, W. R. Jiang, S. Rajyaguru, G. Tavares, C. Oshiro, T. Hendricks, K. Klumpp, J. Symons, M. F. Browner, N. Cammack, and I. Najera. 2006. Selection and characterization of replicon variants dually resistant to thumb- and palm-binding nonnucleoside polymerase inhibitors of the hepatitis C virus. J. Virol. 80:6146-6154.
-
(2006)
J. Virol
, vol.80
, pp. 6146-6154
-
-
Le Pogam, S.1
Kang, H.2
Harris, S.F.3
Leveque, V.4
Giannetti, A.M.5
Ali, S.6
Jiang, W.R.7
Rajyaguru, S.8
Tavares, G.9
Oshiro, C.10
Hendricks, T.11
Klumpp, K.12
Symons, J.13
Browner, M.F.14
Cammack, N.15
Najera, I.16
-
25
-
-
57049158011
-
Lack of viral resistance after 14-day monotherapy treatment with R7128 in treatment-experienced patients infected with HCV genotype 1, abstr. 26. Abstr
-
February
-
Le Pogam, S., A. Seshaadri, A. Kosaka, S. Hu, A. Beard, J. Symons, N. Cammack, and I. Najera. 2008. Lack of viral resistance after 14-day monotherapy treatment with R7128 in treatment-experienced patients infected with HCV genotype 1, abstr. 26. Abstr. Conf. Hepatitis B & C Virus Resist. Antivir. Ther., Paris, France, 14 to 16 February, 2008.
-
(2008)
Conf. Hepatitis B & C Virus Resist. Antivir. Ther., Paris, France, 14 to 16
-
-
Le Pogam, S.1
Seshaadri, A.2
Kosaka, A.3
Hu, S.4
Beard, A.5
Symons, J.6
Cammack, N.7
Najera, I.8
-
26
-
-
0345188811
-
Replication of subgenomic hepatitis C virus RNAs in a hepatoma cell line
-
Lohmann, V., F. Korner, J. Koch, U. Herian, L. Theilmann, and R. Bartenschlager. 1999. Replication of subgenomic hepatitis C virus RNAs in a hepatoma cell line. Science 285:110-113.
-
(1999)
Science
, vol.285
, pp. 110-113
-
-
Lohmann, V.1
Korner, F.2
Koch, J.3
Herian, U.4
Theilmann, L.5
Bartenschlager, R.6
-
27
-
-
34250166157
-
Evolution of resistant M414T mutants among hepatitis C virus replicon cells treated with polymerase inhibitor A-782759
-
Lu, L., H. Mo, T. J. Pilot-Matias, and A. Molla. 2007. Evolution of resistant M414T mutants among hepatitis C virus replicon cells treated with polymerase inhibitor A-782759. Antimicrob. Agents Chemother. 51:1889-1896.
-
(2007)
Antimicrob. Agents Chemother
, vol.51
, pp. 1889-1896
-
-
Lu, L.1
Mo, H.2
Pilot-Matias, T.J.3
Molla, A.4
-
28
-
-
35648968189
-
Characterization of the metabolic activation of a HCV nucleoside inhibitor beta-D-2′-deoxy-2′-fluoro-2′-C-methylcytidine (PSI-6130) and identification of a novel active 5′-triphosphate species
-
Ma, H., W. R. Jiang, N. Robledo, V. Leveque, S. Ali, T. Lara-Jaime, M. Masjedizadeh, D. B. Smith, N. Cammack, K. Klumpp, and J. Symons. 2007. Characterization of the metabolic activation of a HCV nucleoside inhibitor beta-D-2′-deoxy-2′-fluoro-2′-C-methylcytidine (PSI-6130) and identification of a novel active 5′-triphosphate species. J. Biol. Chem. 282:29812-29820.
-
(2007)
J. Biol. Chem
, vol.282
, pp. 29812-29820
-
-
Ma, H.1
Jiang, W.R.2
Robledo, N.3
Leveque, V.4
Ali, S.5
Lara-Jaime, T.6
Masjedizadeh, M.7
Smith, D.B.8
Cammack, N.9
Klumpp, K.10
Symons, J.11
-
29
-
-
12344275294
-
Inhibition of native hepatitis C virus replicase by nucleotide and non-nucleoside inhibitors
-
Ma, H., V. Leveque, W. A. De, W. Li, T. Hendricks, S. M. Clausen, N. Cammack, and K. Klumpp. 2005. Inhibition of native hepatitis C virus replicase by nucleotide and non-nucleoside inhibitors. Virology 332:8-15.
-
(2005)
Virology
, vol.332
, pp. 8-15
-
-
Ma, H.1
Leveque, V.2
De, W.A.3
Li, W.4
Hendricks, T.5
Clausen, S.M.6
Cammack, N.7
Klumpp, K.8
-
30
-
-
1542677267
-
-
Migliaccio, G., J. E. Tomassini, S. S. Carroll, L. Tomei, S. Altamura, B. Bhat, L. Bartholomew, M. R. Bosserman, A. Ceccacci, L. F. Colwell, R. Cortese, F. R. De, A. B. Eldrup, K. L. Getty, X. S. Hou, R. L. LaFemina, S. W. Ludmerer, M. MacCoss, D. R. McMasters, M. W. Stahlhut, D. B. Olsen, D. J. Hazuda, and O. A. Flores. 2003. Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitro. J. Biol. Chem. 278:49164-49170.
-
Migliaccio, G., J. E. Tomassini, S. S. Carroll, L. Tomei, S. Altamura, B. Bhat, L. Bartholomew, M. R. Bosserman, A. Ceccacci, L. F. Colwell, R. Cortese, F. R. De, A. B. Eldrup, K. L. Getty, X. S. Hou, R. L. LaFemina, S. W. Ludmerer, M. MacCoss, D. R. McMasters, M. W. Stahlhut, D. B. Olsen, D. J. Hazuda, and O. A. Flores. 2003. Characterization of resistance to non-obligate chain-terminating ribonucleoside analogs that inhibit hepatitis C virus replication in vitro. J. Biol. Chem. 278:49164-49170.
-
-
-
-
31
-
-
25844466713
-
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
-
Mo, H., L. Lu, T. Pilot-Matias, R. Pithawalla, R. Mondal, S. Masse, T. Dekhtyar, T. Ng, G. Koev, V. Stoll, K. D. Stewart, J. Pratt, P. Donner, T. Rockway, C. Maring, and A. Molla. 2005. 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. 49:4305-4314.
-
(2005)
Antimicrob. Agents Chemother
, vol.49
, pp. 4305-4314
-
-
Mo, H.1
Lu, L.2
Pilot-Matias, T.3
Pithawalla, R.4
Mondal, R.5
Masse, S.6
Dekhtyar, T.7
Ng, T.8
Koev, G.9
Stoll, V.10
Stewart, K.D.11
Pratt, J.12
Donner, P.13
Rockway, T.14
Maring, C.15
Molla, A.16
-
32
-
-
33846589710
-
Mechanism of activation of beta-D-2′- deoxy-2′-fluoro-2′-C-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase
-
Murakami, E., H. Bao, M. Ramesh, T. R. McBrayer, T. Whitaker, H. M. Micolochick Steuer, R. F. Schinazi, L. J. Stuyver, A. Obikhod, M. J. Otto, and P. A. Furman. 2007. Mechanism of activation of beta-D-2′- deoxy-2′-fluoro-2′-C-methylcytidine and inhibition of hepatitis C virus NS5B RNA polymerase. Antimicrob. Agents Chemother. 51:503-509.
-
(2007)
Antimicrob. Agents Chemother
, vol.51
, pp. 503-509
-
-
Murakami, E.1
Bao, H.2
Ramesh, M.3
McBrayer, T.R.4
Whitaker, T.5
Micolochick Steuer, H.M.6
Schinazi, R.F.7
Stuyver, L.J.8
Obikhod, A.9
Otto, M.J.10
Furman, P.A.11
-
33
-
-
38649112300
-
-
Murakami, E., C. Niu, H. Bao, H. M. Steuer, T. Whitaker, T. Nachman, M. Sofia, P. Wang, M. J. Otto, and P. A. Furman. 2008. The mechanism of action of β-D-2′-deoxy-2′-fluoro-2′-C- methylcytidine involves a second metabolic pathway leading to β-D-2′-deoxy-2′-fluoro-2′-C-methyluridine 5′-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. Antimicrob. Agents Chemother. 52:458-464.
-
Murakami, E., C. Niu, H. Bao, H. M. Steuer, T. Whitaker, T. Nachman, M. Sofia, P. Wang, M. J. Otto, and P. A. Furman. 2008. The mechanism of action of β-D-2′-deoxy-2′-fluoro-2′-C- methylcytidine involves a second metabolic pathway leading to β-D-2′-deoxy-2′-fluoro-2′-C-methyluridine 5′-triphosphate, a potent inhibitor of the hepatitis C virus RNA-dependent RNA polymerase. Antimicrob. Agents Chemother. 52:458-464.
-
-
-
-
34
-
-
57049140853
-
The nucleoside inhibitor MK-0608 mediates suppression of HCV replication for greater than 30 days in chronically infected chimpanzees, abstr. 1159. Abstr
-
September
-
Olsen, D. B. 2006. The nucleoside inhibitor MK-0608 mediates suppression of HCV replication for greater than 30 days in chronically infected chimpanzees, abstr. 1159. Abstr. 46th Intersci. Conf. Antimicrob. Agents Chemother., San Francisco, CA, 27 to 30 September, 2006.
-
(2006)
46th Intersci. Conf. Antimicrob. Agents Chemother., San Francisco, CA, 27 to 30
-
-
Olsen, D.B.1
-
35
-
-
4644257970
-
A 7-deaza-adenosine analog is a potent and selective inhibitor of hepatitis C virus replication with excellent pharmacokinetic properties
-
Olsen, D. B., A. B. Eldrup, L. Bartholomew, B. Bhat, M. R. Bosserman, A. Ceccacci, L. F. Colwell, J. F. Fay, O. A. Flores, K. L. Getty, J. A. Grobler, R. L. LaFemina, E. J. Markel, G. Migliaccio, M. Prhavc, M. W. Stahlhut, J. E. Tomassini, M. MacCoss, D. J. Hazuda, and S. S. Carroll. 2004. A 7-deaza-adenosine analog is a potent and selective inhibitor of hepatitis C virus replication with excellent pharmacokinetic properties. Antimicrob. Agents Chemother. 48:3944-3953.
-
(2004)
Antimicrob. Agents Chemother
, vol.48
, pp. 3944-3953
-
-
Olsen, D.B.1
Eldrup, A.B.2
Bartholomew, L.3
Bhat, B.4
Bosserman, M.R.5
Ceccacci, A.6
Colwell, L.F.7
Fay, J.F.8
Flores, O.A.9
Getty, K.L.10
Grobler, J.A.11
LaFemina, R.L.12
Markel, E.J.13
Migliaccio, G.14
Prhavc, M.15
Stahlhut, M.W.16
Tomassini, J.E.17
MacCoss, M.18
Hazuda, D.J.19
Carroll, S.S.20
more..
-
36
-
-
33750465538
-
Synthesis and pharmacokinetics of valopicitabine (NM283), an efficient prodrug of the potent anti-HCV agent 2′-C-methylcytidine
-
Pierra, C., A. Amador, S. Benzaria, E. Cretton-Scott, M. D'Amours, J. Mao, S. Mathieu, A. Moussa, E. G. Bridges, D. N. Standring, J. P. Sommadossi, R. Storer, and G. Gosselin. 2006. Synthesis and pharmacokinetics of valopicitabine (NM283), an efficient prodrug of the potent anti-HCV agent 2′-C-methylcytidine. J. Med. Chem. 49:6614-6620.
-
(2006)
J. Med. Chem
, vol.49
, pp. 6614-6620
-
-
Pierra, C.1
Amador, A.2
Benzaria, S.3
Cretton-Scott, E.4
D'Amours, M.5
Mao, J.6
Mathieu, S.7
Moussa, A.8
Bridges, E.G.9
Standring, D.N.10
Sommadossi, J.P.11
Storer, R.12
Gosselin, G.13
-
37
-
-
26644455085
-
Nm 283, an efficient prodrug of the potent anti-HCV agent 2′-C-methylcytidine
-
Pierra, C., S. Benzaria, A. Amador, A. Moussa, S. Mathieu, R. Storer, and G. Gosselin. 2005. Nm 283, an efficient prodrug of the potent anti-HCV agent 2′-C-methylcytidine. Nucleosides Nucleotides Nucleic Acids 24:767-770.
-
(2005)
Nucleosides Nucleotides Nucleic Acids
, vol.24
, pp. 767-770
-
-
Pierra, C.1
Benzaria, S.2
Amador, A.3
Moussa, A.4
Mathieu, S.5
Storer, R.6
Gosselin, G.7
-
38
-
-
0036196022
-
Persistent and transient replication of full-length hepatitis C virus genomes in cell culture
-
Pietschmann, T., V. Lohmann, A. Kaul, N. Krieger, G. Rinck, G. Rutter, D. Strand, and R. Bartenschlager. 2002. Persistent and transient replication of full-length hepatitis C virus genomes in cell culture. J. Virol. 76:4008-4021.
-
(2002)
J. Virol
, vol.76
, pp. 4008-4021
-
-
Pietschmann, T.1
Lohmann, V.2
Kaul, A.3
Krieger, N.4
Rinck, G.5
Rutter, G.6
Strand, D.7
Bartenschlager, R.8
-
39
-
-
0035148546
-
Characterization of cell lines carrying self-replicating hepatitis C virus RNAs
-
Pietschmann, T., V. Lohmann, G. Rutter, K. Kurpanek, and R. Bartenschlager. 2001. Characterization of cell lines carrying self-replicating hepatitis C virus RNAs. J. Virol. 75:1252-1264.
-
(2001)
J. Virol
, vol.75
, pp. 1252-1264
-
-
Pietschmann, T.1
Lohmann, V.2
Rutter, G.3
Kurpanek, K.4
Bartenschlager, R.5
-
40
-
-
57049178815
-
Robust synergistic antiviral effect of R1626 in combination with Peginterferon alfa-2a (40KD), with or without ribavirin - interim analysis results of phase 2a study, abstr. 167. Abstr
-
November
-
Pockros, P., D. Nelson, E. Godofsky, M. Rodriguez-Torres, G. T. Everson, M. W. Fried, R. H. Ghalib, S. Harrison, L. M. Nyberg, M. L. Shiffman, G. Hill, and A. Chan. 2007. Robust synergistic antiviral effect of R1626 in combination with Peginterferon alfa-2a (40KD), with or without ribavirin - interim analysis results of phase 2a study, abstr. 167. Abstr. 58th Annu. Meet. Am. Assoc. Study Liver Diseases, Boston, MA, 2 to 6 November, 2007.
-
(2007)
58th Annu. Meet. Am. Assoc. Study Liver Diseases, Boston, MA, 2 to 6
-
-
Pockros, P.1
Nelson, D.2
Godofsky, E.3
Rodriguez-Torres, M.4
Everson, G.T.5
Fried, M.W.6
Ghalib, R.H.7
Harrison, S.8
Nyberg, L.M.9
Shiffman, M.L.10
Hill, G.11
Chan, A.12
-
41
-
-
57049164695
-
-
Reddy, R., M. Rodriguez-Torres, E. Gane, R. Robson, J. Lalenzari, G. T. Everson, E. DeJesus, J. G. McHutchison, H. E. Vargas, A. Beard, C. A. Rodriguez, G. Z. Hill, W. T. Symonds, and M. M. Berry. 2007. Antiviral activity, pharmacokinetics, safety, and tolerability of R7128, a novel nucleoside HCV RNA polymerase inhibitor, following multiple, ascending, oral doses in patients with HCV genotype 1 infection who have failed prior interferon therapy, abstr. LB9. Abstr. 58th Annu. Meet. Am. Assoc. Study Liver Diseases, Boston, MA, 2 to 6 November, 2007.
-
Reddy, R., M. Rodriguez-Torres, E. Gane, R. Robson, J. Lalenzari, G. T. Everson, E. DeJesus, J. G. McHutchison, H. E. Vargas, A. Beard, C. A. Rodriguez, G. Z. Hill, W. T. Symonds, and M. M. Berry. 2007. Antiviral activity, pharmacokinetics, safety, and tolerability of R7128, a novel nucleoside HCV RNA polymerase inhibitor, following multiple, ascending, oral doses in patients with HCV genotype 1 infection who have failed prior interferon therapy, abstr. LB9. Abstr. 58th Annu. Meet. Am. Assoc. Study Liver Diseases, Boston, MA, 2 to 6 November, 2007.
-
-
-
-
42
-
-
57049122694
-
-
Roberts, S., G. Cooksley, D. Shaw, H. K. Berns, M. T. Brandt, S. H. Fettner, G. Hill, D. Ipe, K. Klumpp, M. Mannino, E. O'Mara, Y. Tu, and C. B. Washington. 2006. Interim results of a multiple ascending dose study of R1626, a novel nucleoside analog targeting HCV polymerase in chronic HCV patients, abstr. 731. Abstr. 41th Annu. Meet. Eur. Assoc. Study Liver, Vienna, Austria, 26 to 30 April, 2006.
-
Roberts, S., G. Cooksley, D. Shaw, H. K. Berns, M. T. Brandt, S. H. Fettner, G. Hill, D. Ipe, K. Klumpp, M. Mannino, E. O'Mara, Y. Tu, and C. B. Washington. 2006. Interim results of a multiple ascending dose study of R1626, a novel nucleoside analog targeting HCV polymerase in chronic HCV patients, abstr. 731. Abstr. 41th Annu. Meet. Eur. Assoc. Study Liver, Vienna, Austria, 26 to 30 April, 2006.
-
-
-
-
43
-
-
34247205808
-
SCH 503034, a novel hepatitis C virus protease inhibitor, plus pegylated interferon alpha-2b for genotype 1 nonresponders
-
Sarrazin, C., R. Rouzier, F. Wagner, N. Forestier, D. Larrey, S. K. Gupta, M. Hussain, A. Shah, D. Cutler, J. Zhang, and S. Zeuzem. 2007. SCH 503034, a novel hepatitis C virus protease inhibitor, plus pegylated interferon alpha-2b for genotype 1 nonresponders. Gastroenterology 132:1270-1278.
-
(2007)
Gastroenterology
, vol.132
, pp. 1270-1278
-
-
Sarrazin, C.1
Rouzier, R.2
Wagner, F.3
Forestier, N.4
Larrey, D.5
Gupta, S.K.6
Hussain, M.7
Shah, A.8
Cutler, D.9
Zhang, J.10
Zeuzem, S.11
-
44
-
-
33646457538
-
Inhibition of hepatitis C replicon RNA synthesis by beta-D-2′-deoxy- 2′-fluoro-2′-C-methylcytidine: A specific inhibitor of hepatitis C virus replication
-
Stuyver, L. J., T. R. McBrayer, P. M. Tharnish, J. Clark, L. Hollecker, S. Lostia, T. Nachman, J. Grier, M. A. Bennett, M. Y. Xie, R. F. Schinazi, J. D. Morrey, J. L. Julander, P. A. Furman, and M. J. Otto. 2006. Inhibition of hepatitis C replicon RNA synthesis by beta-D-2′-deoxy- 2′-fluoro-2′-C-methylcytidine: a specific inhibitor of hepatitis C virus replication. Antivir. Chem. Chemother. 17:79-87.
-
(2006)
Antivir. Chem. Chemother
, vol.17
, pp. 79-87
-
-
Stuyver, L.J.1
McBrayer, T.R.2
Tharnish, P.M.3
Clark, J.4
Hollecker, L.5
Lostia, S.6
Nachman, T.7
Grier, J.8
Bennett, M.A.9
Xie, M.Y.10
Schinazi, R.F.11
Morrey, J.D.12
Julander, J.L.13
Furman, P.A.14
Otto, M.J.15
-
45
-
-
10744221995
-
Mechanism of action and antiviral activity of benzimidazole-based allosteric inhibitors of the hepatitis C virus RNA-dependent RNA polymerase
-
Tomei, L., S. Altamura, L. Bartholomew, A. Biroccio, A. Ceccacci, L. Pacini, F. Narjes, N. Gennari, M. Bisbocci, I. Incitti, L. Orsatti, S. Harper, I. Stansfield, M. Rowley, F. R. De, and G. Migliaccio. 2003. Mechanism of action and antiviral activity of benzimidazole-based allosteric inhibitors of the hepatitis C virus RNA-dependent RNA polymerase. J. Virol. 77:13225-13231.
-
(2003)
J. Virol
, vol.77
, pp. 13225-13231
-
-
Tomei, L.1
Altamura, S.2
Bartholomew, L.3
Biroccio, A.4
Ceccacci, A.5
Pacini, L.6
Narjes, F.7
Gennari, N.8
Bisbocci, M.9
Incitti, I.10
Orsatti, L.11
Harper, S.12
Stansfield, I.13
Rowley, M.14
De, F.R.15
Migliaccio, G.16
-
46
-
-
57049189519
-
-
Villano, S., A. Y. Howe, D. Raible, D. Harper, J. Speth, and G. Bichier. 2007. Analysis of HCV NS5B genetic variants following monotherapy with HCV-796, a non-nucleoside polymerase inhibitor, in treatment-naïve HCV-infected patients, abstr. 1302. Abstr. 58th Annu. Meet. Am. Assoc. Study Liver Diseases, Boston, MA, 2 to 6 November, 2007.
-
Villano, S., A. Y. Howe, D. Raible, D. Harper, J. Speth, and G. Bichier. 2007. Analysis of HCV NS5B genetic variants following monotherapy with HCV-796, a non-nucleoside polymerase inhibitor, in treatment-naïve HCV-infected patients, abstr. 1302. Abstr. 58th Annu. Meet. Am. Assoc. Study Liver Diseases, Boston, MA, 2 to 6 November, 2007.
-
-
-
-
47
-
-
0038322074
-
Non-nucleoside analogue inhibitors bind to an allosteric site on HCV NS5B polymerase. Crystal structures and mechanism of inhibition
-
Wang, M., K. K. Ng, M. M. Cherney, L. Chan, C. G. Yannopoulos, J. Bedard, N. Morin, N. Nguyen-Ba, M. H. Alaoui-Ismaili, R. C. Bethell, and M. N. James. 2003. Non-nucleoside analogue inhibitors bind to an allosteric site on HCV NS5B polymerase. Crystal structures and mechanism of inhibition. J. Biol. Chem. 278:9489-9495.
-
(2003)
J. Biol. Chem
, vol.278
, pp. 9489-9495
-
-
Wang, M.1
Ng, K.K.2
Cherney, M.M.3
Chan, L.4
Yannopoulos, C.G.5
Bedard, J.6
Morin, N.7
Nguyen-Ba, N.8
Alaoui-Ismaili, M.H.9
Bethell, R.C.10
James, M.N.11
-
48
-
-
3242700469
-
Adaptive mutations producing efficient replication of genotype 1a hepatitis C virus RNA in normal Huh7 cells
-
Yi, M., and S. M. Lemon. 2004. Adaptive mutations producing efficient replication of genotype 1a hepatitis C virus RNA in normal Huh7 cells. J. Virol. 78:7904-7915.
-
(2004)
J. Virol
, vol.78
, pp. 7904-7915
-
-
Yi, M.1
Lemon, S.M.2
|