Literature DB >> 22024816

In vitro resistance profile of the hepatitis C virus NS3 protease inhibitor BI 201335.

Lisette Lagacé1, Peter W White, Christiane Bousquet, Nathalie Dansereau, Florence Dô, Montse Llinas-Brunet, Martin Marquis, Marie-Josée Massariol, Roger Maurice, Catherine Spickler, Diane Thibeault, Ibtissem Triki, Songping Zhao, George Kukolj.   

Abstract

The in vitro resistance profile of BI 201335 was evaluated through selection and characterization of variants in genotype 1a (GT 1a) and genotype 1b (GT 1b) replicons. NS3 R155K and D168V were the most frequently observed resistant variants. Phenotypic characterization of the mutants revealed shifts in sensitivity specific to BI 201335 that did not alter susceptibility to alpha interferon. In contrast to macrocyclic and covalent protease inhibitors, changes at V36, T54, F43, and Q80 did not confer resistance to BI 201335.

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Year:  2011        PMID： 22024816      PMCID： PMC3256085          DOI： 10.1128/AAC.05166-11

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN： 0066-4804            Impact factor:   5.191


  28 in total

1.  Discovery of a potent and selective noncovalent linear inhibitor of the hepatitis C virus NS3 protease (BI 201335).

Authors:  Montse Llinàs-Brunet; Murray D Bailey; Nathalie Goudreau; Punit K Bhardwaj; Josée Bordeleau; Michael Bös; Yves Bousquet; Michael G Cordingley; Jiamin Duan; Pat Forgione; Michel Garneau; Elise Ghiro; Vida Gorys; Sylvie Goulet; Ted Halmos; Stephen H Kawai; Julie Naud; Marc-André Poupart; Peter W White
Journal:  J Med Chem       Date:  2010-09-09       Impact factor: 7.446

2.  Induced-fit binding of the macrocyclic noncovalent inhibitor TMC435 to its HCV NS3/NS4A protease target.

Authors:  Maxwell D Cummings; Jimmy Lindberg; Tse-I Lin; Herman de Kock; Oliver Lenz; Elisabet Lilja; Sara Felländer; Vera Baraznenok; Susanne Nyström; Magnus Nilsson; Lotta Vrang; Michael Edlund; Asa Rosenquist; Bertil Samuelsson; Pierre Raboisson; Kenneth Simmen
Journal:  Angew Chem Int Ed Engl       Date:  2010-02-22       Impact factor: 15.336

3.  In vitro resistance profile of the hepatitis C virus NS3/4A protease inhibitor TMC435.

Authors:  Oliver Lenz; Thierry Verbinnen; Tse-I Lin; Leen Vijgen; Maxwell D Cummings; Jimmy Lindberg; Jan Martin Berke; Pascale Dehertogh; Els Fransen; Annick Scholliers; Katrien Vermeiren; Tania Ivens; Pierre Raboisson; Michael Edlund; Susan Storm; Lotta Vrang; Herman de Kock; Gregory C Fanning; Kenneth A Simmen
Journal:  Antimicrob Agents Chemother       Date:  2010-02-22       Impact factor: 5.191

Review 4.  Resistance to direct antiviral agents in patients with hepatitis C virus infection.

Authors:  Christoph Sarrazin; Stefan Zeuzem
Journal:  Gastroenterology       Date:  2009-12-16       Impact factor: 22.682

5.  Susceptibility of treatment-naive hepatitis C virus (HCV) clinical isolates to HCV protease inhibitors.

Authors:  Andrew Bae; Siu-Chi Sun; Xiaoping Qi; Xiaowu Chen; Karin Ku; Angela Worth; Kelly A Wong; Jeanette Harris; Michael D Miller; Hongmei Mo
Journal:  Antimicrob Agents Chemother       Date:  2010-09-20       Impact factor: 5.191

6.  Preclinical characterization of BI 201335, a C-terminal carboxylic acid inhibitor of the hepatitis C virus NS3-NS4A protease.

Authors:  Peter W White; Montse Llinàs-Brunet; Ma'an Amad; Richard C Bethell; Gordon Bolger; Michael G Cordingley; Jianmin Duan; Michel Garneau; Lisette Lagacé; Diane Thibeault; George Kukolj
Journal:  Antimicrob Agents Chemother       Date:  2010-09-07       Impact factor: 5.191

7.  Protease and helicase activities of hepatitis C virus genotype 4, 5, and 6 NS3-NS4A proteins.

Authors:  Marie-Josée Massariol; Songping Zhao; Martin Marquis; Diane Thibeault; Peter W White
Journal:  Biochem Biophys Res Commun       Date:  2009-11-26       Impact factor: 3.575

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

Authors:  Simone Susser; Christoph Welsch; Yalan Wang; Markus Zettler; Francisco S Domingues; Ursula Karey; Eric Hughes; Robert Ralston; Xiao Tong; Eva Herrmann; Stefan Zeuzem; Christoph Sarrazin
Journal:  Hepatology       Date:  2009-12       Impact factor: 17.425

9.  Rapid HCV-RNA decline with once daily TMC435: a phase I study in healthy volunteers and hepatitis C patients.

Authors:  Henk W Reesink; Gregory C Fanning; Khalid Abou Farha; Christine Weegink; André Van Vliet; Gerben Van 't Klooster; Oliver Lenz; Fatima Aharchi; Kris Mariën; Pieter Van Remoortere; Herman de Kock; Fabrice Broeckaert; Paul Meyvisch; Els Van Beirendonck; Kenneth Simmen; René Verloes
Journal:  Gastroenterology       Date:  2009-10-21       Impact factor: 22.682

10.  GT-1a or GT-1b subtype-specific resistance profiles for hepatitis C virus inhibitors telaprevir and HCV-796.

Authors:  Matthew F McCown; Sonal Rajyaguru; Simran Kular; Nick Cammack; Isabel Nájera
Journal:  Antimicrob Agents Chemother       Date:  2009-03-09       Impact factor: 5.191
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  17 in total

1.  Molecular mechanism by which a potent hepatitis C virus NS3-NS4A protease inhibitor overcomes emergence of resistance.

Authors:  Jeff A O'Meara; Christopher T Lemke; Cédrickx Godbout; George Kukolj; Lisette Lagacé; Benoît Moreau; Diane Thibeault; Peter W White; Montse Llinàs-Brunet
Journal:  J Biol Chem       Date:  2012-12-27       Impact factor: 5.157

2.  Resistance analysis of the hepatitis C virus NS3 protease inhibitor asunaprevir.

Authors:  Fiona McPhee; Jacques Friborg; Steven Levine; Chaoqun Chen; Paul Falk; Fei Yu; Dennis Hernandez; Min S Lee; Susan Chaniewski; Amy K Sheaffer; Claudio Pasquinelli
Journal:  Antimicrob Agents Chemother       Date:  2012-04-16       Impact factor: 5.191

3.  Antiviral effect, safety, and pharmacokinetics of five-day oral administration of Deleobuvir (BI 207127), an investigational hepatitis C virus RNA polymerase inhibitor, in patients with chronic hepatitis C.

Authors:  Dominique Larrey; Ansgar W Lohse; Christian Trepo; Jean-Pierre Bronowicki; Keikawus Arastéh; Marc Bourlière; Jose Luis Calleja; Jerry O Stern; Gerhard Nehmiz; Nasri Abdallah; Kristi L Berger; Martin Marquis; Jürgen Steffgen; George Kukolj
Journal:  Antimicrob Agents Chemother       Date:  2013-07-15       Impact factor: 5.191

4.  Baseline Polymorphisms and Emergence of Drug Resistance in the NS3/4A Protease of Hepatitis C Virus Genotype 1 following Treatment with Faldaprevir and Pegylated Interferon Alpha 2a/Ribavirin in Phase 2 and Phase 3 Studies.

Authors:  K L Berger; J Scherer; M Ranga; N Sha; J O Stern; A-M Quinson; G Kukolj
Journal:  Antimicrob Agents Chemother       Date:  2015-07-20       Impact factor: 5.191

Review 5.  Hepatitis C virus molecular evolution: transmission, disease progression and antiviral therapy.

Authors:  Maria Victoria Preciado; Pamela Valva; Alejandro Escobar-Gutierrez; Paula Rahal; Karina Ruiz-Tovar; Lilian Yamasaki; Carlos Vazquez-Chacon; Armando Martinez-Guarneros; Juan Carlos Carpio-Pedroza; Salvador Fonseca-Coronado; Mayra Cruz-Rivera
Journal:  World J Gastroenterol       Date:  2014-11-21       Impact factor: 5.742

6.  Baseline hepatitis C virus (HCV) NS3 polymorphisms and their impact on treatment response in clinical studies of the HCV NS3 protease inhibitor faldaprevir.

Authors:  Kristi L Berger; Ibtissem Triki; Mireille Cartier; Martin Marquis; Marie-Josée Massariol; Wulf O Böcher; Yakov Datsenko; Gerhard Steinmann; Joseph Scherer; Jerry O Stern; George Kukolj
Journal:  Antimicrob Agents Chemother       Date:  2013-11-11       Impact factor: 5.191

7.  Viral resistance in hepatitis C virus genotype 1-infected patients receiving the NS3 protease inhibitor Faldaprevir (BI 201335) in a phase 1b multiple-rising-dose study.

Authors:  Kristi L Berger; Lisette Lagacé; Ibtissem Triki; Mireille Cartier; Martin Marquis; Carol Lawetz; Richard Bethell; Joseph Scherer; George Kukolj
Journal:  Antimicrob Agents Chemother       Date:  2013-07-22       Impact factor: 5.191

Review 8.  Resistance detection and re-treatment options in hepatitis C virus-related chronic liver diseases after DAA-treatment failure.

Authors:  Evangelista Sagnelli; Mario Starace; Carmine Minichini; Mariantonietta Pisaturo; Margherita Macera; Caterina Sagnelli; Nicola Coppola
Journal:  Infection       Date:  2018-08-06       Impact factor: 3.553

9.  Evaluating the Role of Cellular Immune Responses in the Emergence of HCV NS3 Resistance Mutations During Protease Inhibitor Therapy.

Authors:  Enass A Abdel-Hameed; Susan D Rouster; Hong Ji; Ashley Ulm; Helal F Hetta; Nadeem Anwar; Kenneth E Sherman; Mohamed Tarek M Shata
Journal:  Viral Immunol       Date:  2016-02-17       Impact factor: 2.257

10.  Evaluation of phosphatidylinositol-4-kinase IIIα as a hepatitis C virus drug target.

Authors:  Frédéric H Vaillancourt; Martine Brault; Louise Pilote; Nathalie Uyttersprot; Elias T Gaillard; James H Stoltz; Brian L Knight; Lynn Pantages; Mary McFarland; Steffen Breitfelder; Tim T Chiu; Louiza Mahrouche; Anne-Marie Faucher; Mireille Cartier; Michael G Cordingley; Richard C Bethell; Huiping Jiang; Peter W White; George Kukolj
Journal:  J Virol       Date:  2012-08-15       Impact factor: 5.103
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