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Preclinical Characterization of BI 201335, a C-Terminal Carboxylic Acid Inhibitor of the Hepatitis C Virus NS3-NS4A Protease

Preclinical Characterization of BI 201335, a C-Terminal Carboxylic Acid Inhibitor of the Hepatitis C Virus NS3-NS4A Protease

by WHITE, Peter W, LLINAS-BRUNET, Montse, KUKOLJ, George, AMAD, Ma'an, BETHELL, Richard C, BOLGER, Gordon, CORDINGLEY, Michael G, JIANMIN DUAN, GARNEAU, Michel, LAGACE, Lisette, THIBEAULT, Diane
Published in Antimicrobial Agents and Chemotherapy (01.11.2010)

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Discovery of Hepatitis C Virus NS3-4A Protease Inhibitors with Improved Barrier to Resistance and Favorable Liver Distribution

Discovery of Hepatitis C Virus NS3-4A Protease Inhibitors with Improved Barrier to Resistance and Favorable Liver Distribution

by Moreau, Benoît, O’Meara, Jeff A., Bordeleau, Josée, Garneau, Michel, Godbout, Cedrickx, Gorys, Vida, Leblanc, Mélissa, Villemure, Elisia, White, Peter W., Llinàs-Brunet, Montse
Published in Journal of medicinal chemistry (13.03.2014)

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Discovery of a Potent and Selective Noncovalent Linear Inhibitor of the Hepatitis C Virus NS3 Protease (BI 201335)

Discovery of a Potent and Selective Noncovalent Linear Inhibitor of the Hepatitis C Virus NS3 Protease (BI 201335)

by Llinàs-Brunet, Montse, Bailey, Murray D, Goudreau, Nathalie, Bhardwaj, Punit K, Bordeleau, Josée, Bös, Michael, Bousquet, Yves, Cordingley, Michael G, Duan, Jiamin, Forgione, Pat, Garneau, Michel, Ghiro, Elise, Gorys, Vida, Goulet, Sylvie, Halmos, Ted, Kawai, Stephen H, Naud, Julie, Poupart, Marc-André, White, Peter W
Published in Journal of medicinal chemistry (09.09.2010)

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Molecular Dynamics Simulations and Structure-Based Rational Design Lead to Allosteric HCV NS5B Polymerase Thumb Pocket 2 Inhibitor with Picomolar Cellular Replicon Potency

Molecular Dynamics Simulations and Structure-Based Rational Design Lead to Allosteric HCV NS5B Polymerase Thumb Pocket 2 Inhibitor with Picomolar Cellular Replicon Potency

by Hucke, Oliver, Coulombe, René, Bonneau, Pierre, Bertrand-Laperle, Mégan, Brochu, Christian, Gillard, James, Joly, Marc-André, Landry, Serge, Lepage, Olivier, Llinàs-Brunet, Montse, Pesant, Marc, Poirier, Martin, Poirier, Maude, McKercher, Ginette, Marquis, Martin, Kukolj, George, Beaulieu, Pierre L., Stammers, Timothy A.
Published in Journal of medicinal chemistry (13.03.2014)

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Molecular Mechanism by Which a Potent Hepatitis C Virus NS3-NS4A Protease Inhibitor Overcomes Emergence of Resistance

Molecular Mechanism by Which a Potent Hepatitis C Virus NS3-NS4A Protease Inhibitor Overcomes Emergence of Resistance

by O'Meara, Jeff A., Lemke, Christopher T., Godbout, Cédrickx, Kukolj, George, Lagacé, Lisette, Moreau, Benoît, Thibeault, Diane, White, Peter W., Llinàs-Brunet, Montse
Published in The Journal of biological chemistry (22.02.2013)

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Use of the Fused NS4A Peptide−NS3 Protease Domain To Study the Importance of the Helicase Domain for Protease Inhibitor Binding to Hepatitis C Virus NS3-NS4A

Use of the Fused NS4A Peptide−NS3 Protease Domain To Study the Importance of the Helicase Domain for Protease Inhibitor Binding to Hepatitis C Virus NS3-NS4A

by Thibeault, Diane, Massariol, Marie-Josée, Zhao, Songping, Welchner, Ewald, Goudreau, Nathalie, Gingras, Rock, Llinàs-Brunet, Montse, White, Peter W
Published in Biochemistry (Easton) (03.02.2009)

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Hepatitis C virus serine protease: synthesis of radioactive and stable isotope-labeled potent inhibitors

Hepatitis C virus serine protease: synthesis of radioactive and stable isotope-labeled potent inhibitors

by Latli, Bachir, Hrapchak, Matt, Gorys, Vida, Llinàs-Brunet, Montse, Campbell, Scot S., Song, Jinhua, Senanayake, Chris H.
Published in Journal of labelled compounds & radiopharmaceuticals (15.05.2014)

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Dimethylthiazolidine Carboxylic Acid as a Rigid P3 Unit in Inhibitors of Serine Proteases: Application to Two Targets

Dimethylthiazolidine Carboxylic Acid as a Rigid P3 Unit in Inhibitors of Serine Proteases: Application to Two Targets

by Kawai, Stephen H., Aubry, Norman, Duceppe, Jean-Simon, Llinàs-Brunet, Montse, LaPlante, Steven R.
Published in Chemical biology & drug design (01.11.2009)

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The Use of Chemical Double-Mutant Cycles in Biomolecular Recognition Studies: Application to HCV NS3 Protease Inhibitors

The Use of Chemical Double-Mutant Cycles in Biomolecular Recognition Studies: Application to HCV NS3 Protease Inhibitors

by Kawai, Stephen H., Bailey, Murray D., Halmos, Ted, Forgione, Pat, LaPlante, Steven R., Llinàs-Brunet, Montse, Naud, Julie, Goudreau, Natalie
Published in ChemMedChem (17.11.2008)

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Combined X-ray, NMR, and Kinetic Analyses Reveal Uncommon Binding Characteristics of the Hepatitis C Virus NS3-NS4A Protease Inhibitor BI 201335

Combined X-ray, NMR, and Kinetic Analyses Reveal Uncommon Binding Characteristics of the Hepatitis C Virus NS3-NS4A Protease Inhibitor BI 201335

by Lemke, Christopher T., Goudreau, Nathalie, Zhao, Songping, Hucke, Oliver, Thibeault, Diane, Llinàs-Brunet, Montse, White, Peter W.
Published in The Journal of biological chemistry (01.04.2011)

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An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

An NS3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

by Lamarre, Daniel, Anderson, Paul C, Bailey, Murray, Beaulieu, Pierre, Bolger, Gordon, Bonneau, Pierre, Bös, Michael, Cameron, Dale R, Cartier, Mireille, Cordingley, Michael G, Faucher, Anne-Marie, Goudreau, Nathalie, Kawai, Stephen H, Kukolj, George, Lagacé, Lisette, LaPlante, Steven R, Narjes, Hans, Poupart, Marc-André, Rancourt, Jean, Sentjens, Roel E, St George, Roger, Simoneau, Bruno, Steinmann, Gerhard, Thibeault, Diane, Tsantrizos, Youla S, Weldon, Steven M, Yong, Chan-Loi, Llinàs-Brunet, Montse
Published in Nature (13.11.2003)

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In Vitro Resistance Profile of the Hepatitis C Virus NS3 Protease Inhibitor BI 201335

by LAGACE, Lisette, WHITE, Peter W, THIBEAULT, Diane, TRIKI, Ibtissem, SONGPING ZHAO, KUKOLJ, George, BOUSQUET, Christiane, DANSEREAU, Nathalie, DO, Florence, LLINAS-BRUNET, Montse, MARQUIS, Martin, MASSARIOL, Marie-Josée, MAURICE, Roger, SPICKLER, Catherine
Published in Antimicrobial Agents and Chemotherapy (01.01.2012)

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Structure-based design of novel HCV NS5B thumb pocket 2 allosteric inhibitors with submicromolar gt1 replicon potency: Discovery of a quinazolinone chemotype

Structure-based design of novel HCV NS5B thumb pocket 2 allosteric inhibitors with submicromolar gt1 replicon potency: Discovery of a quinazolinone chemotype

by Beaulieu, Pierre L., Coulombe, René, Duan, Jianmin, Fazal, Gulrez, Godbout, Cédrickx, Hucke, Oliver, Jakalian, Araz, Joly, Marc-André, Lepage, Olivier, Llinàs-Brunet, Montse, Naud, Julie, Poirier, Martin, Rioux, Nathalie, Thavonekham, Bounkham, Kukolj, George, Stammers, Timothy A.
Published in Bioorganic & medicinal chemistry letters (15.07.2013)

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A Systematic Approach to the Optimization of Substrate-Based Inhibitors of the Hepatitis C Virus NS3 Protease: Discovery of Potent and Specific Tripeptide Inhibitors

A Systematic Approach to the Optimization of Substrate-Based Inhibitors of the Hepatitis C Virus NS3 Protease: Discovery of Potent and Specific Tripeptide Inhibitors

by Llinàs-Brunet, Montse, Bailey, Murray D, Ghiro, Elise, Gorys, Vida, Halmos, Ted, Poirier, Martin, Rancourt, Jean, Goudreau, Nathalie
Published in Journal of medicinal chemistry (16.12.2004)

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Structure−Activity Study on a Novel Series of Macrocyclic Inhibitors of the Hepatitis C Virus NS3 Protease Leading to the Discovery of BILN 2061

Structure−Activity Study on a Novel Series of Macrocyclic Inhibitors of the Hepatitis C Virus NS3 Protease Leading to the Discovery of BILN 2061

by Llinàs-Brunet, Montse, Bailey, Murray D, Bolger, Gordon, Brochu, Christian, Faucher, Anne-Marie, Ferland, Jean Marie, Garneau, Michel, Ghiro, Elise, Gorys, Vida, Grand-Maître, Chantal, Halmos, Ted, Lapeyre-Paquette, Nicole, Liard, Francine, Poirier, Martin, Rhéaume, Manon, Tsantrizos, Youla S, Lamarre, Daniel
Published in Journal of medicinal chemistry (25.03.2004)

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The therapeutic potential of NS3 protease inhibitors in HCV infection

The therapeutic potential of NS3 protease inhibitors in HCV infection

by Goudreau, Nathalie, Llinàs-Brunet, Montse
Published in Expert opinion on investigational drugs (01.09.2005)

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Potent triazolyl-proline-based inhibitors of HCV NS3 protease

Potent triazolyl-proline-based inhibitors of HCV NS3 protease

by Naud, Julie, Lemke, Christopher, Goudreau, Nathalie, Beaulieu, Eric, White, Peter D., Llinàs-Brunet, Montse, Forgione, Pat
Published in Bioorganic & medicinal chemistry (01.06.2008)

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Synthesis and optimization of a novel series of HCV NS3 protease inhibitors: 4-Arylproline analogs

Synthesis and optimization of a novel series of HCV NS3 protease inhibitors: 4-Arylproline analogs

by Bilodeau, François, Bailey, Murray D., Bhardwaj, Punit K., Bordeleau, Josée, Forgione, Pat, Garneau, Michel, Ghiro, Elise, Gorys, Vida, Halmos, Ted, Jolicoeur, Eric S., Leblanc, Mélissa, Lemke, Christopher T., Naud, Julie, O’Meara, Jeff, White, Peter W., Llinàs-Brunet, Montse
Published in Bioorganic & medicinal chemistry letters (15.07.2013)

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Peptide-Based Inhibitors of the Hepatitis C Virus NS3 Protease: Structure−Activity Relationship at the C-Terminal Position

Peptide-Based Inhibitors of the Hepatitis C Virus NS3 Protease: Structure−Activity Relationship at the C-Terminal Position

by Rancourt, Jean, Cameron, Dale R, Gorys, Vida, Lamarre, Daniel, Poirier, Martin, Thibeault, Diane, Llinàs-Brunet, Montse
Published in Journal of medicinal chemistry (06.05.2004)

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Peptide backbone replacement of hepatitis C virus NS3 serine protease C-terminal cleavage product analogs: Discovery of potent succinamide inhibitors

Peptide backbone replacement of hepatitis C virus NS3 serine protease C-terminal cleavage product analogs: Discovery of potent succinamide inhibitors

by Bailey, Murray D., Bordeleau, Josée, Garneau, Michel, Leblanc, Mélissa, Lemke, Christopher T., O’Meara, Jeff, White, Peter W., Llinàs-Brunet, Montse
Published in Bioorganic & medicinal chemistry letters (01.08.2013)

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