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Identification and analysis of fitness of resistance mutations against the HCV protease inhibitor SCH 503034.

Tong X, Chase R, Skelton A, Chen T, Wright-Minogue J, Malcolm BA.

Antiviral Res. 2006 Jun;70(2):28-38.


A novel HCV NS3 protease mutation selected by combination treatment of the protease inhibitor boceprevir and NS5B polymerase inhibitors.

Chase R, Skelton A, Xia E, Curry S, Liu S, McMonagle P, Huang HC, Tong X.

Antiviral Res. 2009 Nov;84(2):178-84. doi: 10.1016/j.antiviral.2009.09.003.


In vitro studies of cross-resistance mutations against two hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061.

Lin C, Gates CA, Rao BG, Brennan DL, Fulghum JR, Luong YP, Frantz JD, Lin K, Ma S, Wei YY, Perni RB, Kwong AD.

J Biol Chem. 2005 Nov 4;280(44):36784-91.


Mutations conferring resistance to SCH6, a novel hepatitis C virus NS3/4A protease inhibitor. Reduced RNA replication fitness and partial rescue by second-site mutations.

Yi M, Tong X, Skelton A, Chase R, Chen T, Prongay A, Bogen SL, Saksena AK, Njoroge FG, Veselenak RL, Pyles RB, Bourne N, Malcolm BA, Lemon SM.

J Biol Chem. 2006 Mar 24;281(12):8205-15.


Preclinical characterization of the antiviral activity of SCH 900518 (narlaprevir), a novel mechanism-based inhibitor of hepatitis C virus NS3 protease.

Tong X, Arasappan A, Bennett F, Chase R, Feld B, Guo Z, Hart A, Madison V, Malcolm B, Pichardo J, Prongay A, Ralston R, Skelton A, Xia E, Zhang R, Njoroge FG.

Antimicrob Agents Chemother. 2010 Jun;54(6):2365-70. doi: 10.1128/AAC.00135-10.


Resistance of hepatitis C virus to NS3-4A protease inhibitors: mechanisms of drug resistance induced by R155Q, A156T, D168A and D168V mutations.

Courcambeck J, Bouzidi M, Perbost R, Jouirou B, Amrani N, Cacoub P, Pèpe G, Sabatier JM, Halfon P.

Antivir Ther. 2006;11(7):847-55.


Characterization of resistance mutations against HCV ketoamide protease inhibitors.

Tong X, Bogen S, Chase R, Girijavallabhan V, Guo Z, Njoroge FG, Prongay A, Saksena A, Skelton A, Xia E, Ralston R.

Antiviral Res. 2008 Mar;77(3):177-85. doi: 10.1016/j.antiviral.2007.11.010.


Selection and characterization of hepatitis C virus replicons dually resistant to the polymerase and protease inhibitors HCV-796 and boceprevir (SCH 503034).

Flint M, Mullen S, Deatly AM, Chen W, Miller LZ, Ralston R, Broom C, Emini EA, Howe AY.

Antimicrob Agents Chemother. 2009 Feb;53(2):401-11. doi: 10.1128/AAC.01081-08.


Resistance profiling of hepatitis C virus protease inhibitors using full-length NS3.

Dahl G, Sandström A, Akerblom E, Danielson UH.

Antivir Ther. 2007;12(5):733-40.


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.

J Biol Chem. 2004 Apr 23;279(17):17508-14.


Characterization of resistance to the protease inhibitor boceprevir in hepatitis C virus-infected patients.

Susser S, Welsch C, Wang Y, Zettler M, Domingues FS, Karey U, Hughes E, Ralston R, Tong X, Herrmann E, Zeuzem S, Sarrazin C.

Hepatology. 2009 Dec;50(6):1709-18. doi: 10.1002/hep.23192.


A new stochastic model for subgenomic hepatitis C virus replication considers drug resistant mutants.

Ivanisenko NV, Mishchenko EL, Akberdin IR, Demenkov PS, Likhoshvai VA, Kozlov KN, Todorov DI, Gursky VV, Samsonova MG, Samsonov AM, Clausznitzer D, Kaderali L, Kolchanov NA, Ivanisenko VA.

PLoS One. 2014 Mar 18;9(3):e91502. doi: 10.1371/journal.pone.0091502.


Relative replication capacity and selective advantage profiles of protease inhibitor-resistant hepatitis C virus (HCV) NS3 protease mutants in the HCV genotype 1b replicon system.

He Y, King MS, Kempf DJ, Lu L, Lim HB, Krishnan P, Kati W, Middleton T, Molla A.

Antimicrob Agents Chemother. 2008 Mar;52(3):1101-10.


Mutations conferring resistance to a potent hepatitis C virus serine protease inhibitor in vitro.

Lu L, Pilot-Matias TJ, Stewart KD, Randolph JT, Pithawalla R, He W, Huang PP, Klein LL, Mo H, Molla A.

Antimicrob Agents Chemother. 2004 Jun;48(6):2260-6.


[Replication of the subgenomic hepatitis C virus replicon in the presence of the NS3 protease inhibitors: a stochastic model].

Ivanisenko NV, Mishchenko EL, Akberdin IR, Demenkov PS, Likhoshvai VA, Kozlov KN, Todorov DI, Samsonova MG, Samsonov AM, Kolchanov NA, Ivanisenko VA.

Biofizika. 2013 Sep-Oct;58(5):758-74. Russian.


Selection of replicon variants resistant to ACH-806, a novel hepatitis C virus inhibitor with no cross-resistance to NS3 protease and NS5B polymerase inhibitors.

Yang W, Zhao Y, Fabrycki J, Hou X, Nie X, Sanchez A, Phadke A, Deshpande M, Agarwal A, Huang M.

Antimicrob Agents Chemother. 2008 Jun;52(6):2043-52. doi: 10.1128/AAC.01548-07.


Dynamic hepatitis C virus genotypic and phenotypic changes in patients treated with the protease inhibitor telaprevir.

Sarrazin C, Kieffer TL, Bartels D, Hanzelka B, Müh U, Welker M, Wincheringer D, Zhou Y, Chu HM, Lin C, Weegink C, Reesink H, Zeuzem S, Kwong AD.

Gastroenterology. 2007 May;132(5):1767-77.


Mapping natural polymorphisms of hepatitis C virus NS3/4A protease and antiviral resistance to inhibitors in worldwide isolates.

López-Labrador FX, Moya A, Gonzàlez-Candelas F.

Antivir Ther. 2008;13(4):481-94.


HCV-NS3 inhibitors: determination of their kinetic parameters and mechanism.

Flores MV, Strawbridge J, Ciaramella G, Corbau R.

Biochim Biophys Acta. 2009 Oct;1794(10):1441-8. doi: 10.1016/j.bbapap.2009.06.004.


SCH 503034, a mechanism-based inhibitor of hepatitis C virus NS3 protease, suppresses polyprotein maturation and enhances the antiviral activity of alpha interferon in replicon cells.

Malcolm BA, Liu R, Lahser F, Agrawal S, Belanger B, Butkiewicz N, Chase R, Gheyas F, Hart A, Hesk D, Ingravallo P, Jiang C, Kong R, Lu J, Pichardo J, Prongay A, Skelton A, Tong X, Venkatraman S, Xia E, Girijavallabhan V, Njoroge FG.

Antimicrob Agents Chemother. 2006 Mar;50(3):1013-20.

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