G. Kukolj

发表

Conformation-based restrictions and scaffold replacements in the design of hepatitis C virus polymerase inhibitors: discovery of deleobuvir (BI 207127).

C. Brochu, S. LaPlante, M. Bös, 2014, Journal of medicinal chemistry.

Importance of ligand bioactive conformation in the discovery of potent indole-diamide inhibitors of the hepatitis C virus NS5B.

Araz Jakalian, Martin Poirier, C. Brochu, 2010, Journal of the American Chemical Society.

Non-nucleoside benzimidazole-based allosteric inhibitors of the hepatitis C virus NS5B polymerase: inhibition of subgenomic hepatitis C virus RNA replicons in Huh-7 cells.

Yves Bousquet, J. Gillard, P. Beaulieu, 2004, Journal of medicinal chemistry.

Subcellular localization of avian sarcoma virus and human immunodeficiency virus type 1 integrases

G. Kukolj, A. Skalka, K. Jones, 1997, Journal of virology.

Characterization of the nuclear localization signal in the avian sarcoma virus integrase.

G. Kukolj, A. Skalka, R. Katz, 1998, Gene.

Interferon Regulatory Factor 3-Independent Double-Stranded RNA-Induced Inhibition of Hepatitis C Virus Replicons in Human Embryonic Kidney 293 Cells

G. Kukolj, S. Ali, 2005, Journal of Virology.

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

Steven R. LaPlante, P. Bonneau, D. Lamarre, 2003, Nature.

The bacteriophage D108 Ner repressor binds a conformationally distinct operator

G. Kukolj, M. Dubow, 2000, Molecular and General Genetics MGG.

A prodrug strategy for the oral delivery of a poorly soluble HCV NS5B thumb pocket 1 polymerase inhibitor using self-emulsifying drug delivery systems (SEDDS).

J. Duan, M. Garneau, Timothy A. Stammers, 2015, Bioorganic & medicinal chemistry letters.

Discovery and Synthesis of C-Nucleosides as Potential New Anti-HCV Agents.

Edward M. Tyndall, J. Duan, C. Morton, 2014, ACS medicinal chemistry letters.

Derivatives of imidazotriazine and pyrrolotriazine C-nucleosides as potential new anti-HCV agents.

Edward M. Tyndall, J. Duan, C. Morton, 2014, Bioorganic & medicinal chemistry letters.

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

G. Kukolj, P. White, Jeff O'meara, 2012, The Journal of Biological Chemistry.

Benzimidazole Thumb Pocket I finger-loop inhibitors of HCV NS5B polymerase: improved drug-like properties through C-2 SAR in three sub-series.

J. Duan, M. Garneau, S. LaPlante, 2010, Bioorganic & medicinal chemistry letters.

Carboxylic Acid Inhibitor of the Hepatitis C Virus NS3-NS4A

J. Duan, M. Garneau, G. Kukolj, 2010 .

Molecular dynamics simulations and structure-based rational design lead to allosteric HCV NS5B polymerase thumb pocket 2 inhibitor with picomolar cellular replicon potency.

O. Hucke, P. Bonneau, C. Brochu, 2014, Journal of medicinal chemistry.

Discovery of the first thumb pocket 1 NS5B polymerase inhibitor (BILB 1941) with demonstrated antiviral activity in patients chronically infected with genotype 1 hepatitis C virus (HCV).

J. Duan, M. Garneau, S. LaPlante, 2012, Journal of medicinal chemistry.

Specific inhibitors of HCV polymerase identified using an NS5B with lower affinity for template/primer substrate.

D. Lamarre, S. LaPlante, P. Beaulieu, 2004, Nucleic acids research.

Indole 5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase with nanomolar potency in cell-based subgenomic replicons (part 2): central amino acid linker and right-hand-side SAR studies.

Martin Poirier, J. Duan, M. Garneau, 2011, Bioorganic & medicinal chemistry letters.

Multi-parameter optimization of aza-follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 2: Impact of lipophilicity on promiscuity and in vivo toxicity.

J. Duan, M. Garneau, S. LaPlante, 2015, Bioorganic & medicinal chemistry letters.

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

G. Kukolj, M. Massariol, P. White, 2011, Antimicrobial Agents and Chemotherapy.

DNA ends by retroviral integrases in vitro

G. Kukolj, A. Skalka, 2007 .

Studyin a Phase 1b Multiple-Rising-Dose NS3 Protease Inhibitor Faldaprevir (BI Genotype 1-Infected Patients Receiving the Viral Resistance in Hepatitis C Virus

G. Kukolj, R. Bethell, M. Marquis, 2014 .

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

G. Kukolj, R. Bethell, M. Marquis, 2013, Antimicrobial Agents and Chemotherapy.

STARTVerso1: A randomized trial of faldaprevir plus pegylated interferon/ribavirin for chronic HCV genotype-1 infection.

T. Asselah, D. Ouzan, J. Dufour, 2015, Journal of hepatology.

STARTVerso 1 : A randomized trial of faldaprevir plus pegylated interferon / ribavirin for chronic HCV genotype-1 infection q

T. Asselah, D. Ouzan, J. Dufour, 2015 .

Faldaprevir combined with pegylated interferon alfa‐2a and ribavirin in treatment‐naïve patients with chronic genotype1 HCV: SILEN‐C1 trial

T. Asselah, B. Leggett, G. Kukolj, 2013, Hepatology.

Faldaprevir and deleobuvir for HCV genotype 1 infection.

M. Buti, T. Asselah, V. Soriano, 2013, The New England journal of medicine.

Faldaprevir (Bi 201335), Deleobuvir (Bi 207127) and Ribavirin Oral Therapy for Treatment-Naive HCV Genotype 1: Sound-C1 Final Results

T. Asselah, F. Zoulim, P. Angus, 2013, Antiviral therapy.

HCVerso1 and 2: faldaprevir with deleobuvir (BI 207127) and ribavirin for treatment-naïve patients with chronic hepatitis C virus genotype-1b infection

M. Buti, G. Kukolj, C. Sarrazin, 2016, Clinical and experimental gastroenterology.

CD160 isoforms and regulation of CD4 and CD8 T-cell responses

G. Kukolj, M. Cordingley, R. Bethell, 2014, Journal of Translational Medicine.

An advanced BLT-humanized mouse model for extended HIV-1 cure studies

G. Kukolj, B. Race, K. Phillips, 2018, AIDS.

Faldaprevir combined with peginterferon alfa‐2a and ribavirin in chronic hepatitis C virus genotype‐1 patients with prior nonresponse: SILEN‐C2 trial

T. Asselah, J. Pawlotsky, G. Kukolj, 2013, Hepatology.

Restoration of HCV-specific CD8+ T cell function by interferon-free therapy.

G. Kukolj, V. Lohmann, R. Thimme, 2014, Journal of hepatology.

Improved replicon cellular activity of non-nucleoside allosteric inhibitors of HCV NS5B polymerase: from benzimidazole to indole scaffolds.

C. Brochu, S. LaPlante, J. Gillard, 2006, Bioorganic & medicinal chemistry letters.

Expression of hTERT and hTR in cis reconstitutes and active human telomerase ribonucleoprotein.

G. Kukolj, F. Bachand, C. Autexier, 2000, RNA.

Integration host factor activates the Ner-repressed early promoter of transposable Mu-like phage D108.

G. Kukolj, M. Dubow, 1992, The Journal of biological chemistry.

Discovery of BI 207524, an indole diamide NS5B thumb pocket 1 inhibitor with improved potency for the potential treatment of chronic hepatitis C virus infection.

J. Duan, M. Garneau, P. Anderson, 2014, Journal of medicinal chemistry.

Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery of benzimidazole 5-carboxylic amide derivatives with low-nanomolar potency.

M. Bös, J. Gillard, P. Beaulieu, 2004, Bioorganic & medicinal chemistry letters.

Non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase: discovery and preliminary SAR of benzimidazole derivatives.

S. LaPlante, M. Bös, J. Gillard, 2004, Bioorganic & medicinal chemistry letters.

An NS3 Serine Protease Inhibitor Abrogates Replication of Subgenomic Hepatitis C Virus RNA*

D. Lamarre, A. Pause, G. Kukolj, 2003, Journal of Biological Chemistry.

Internal initiation sites of de novo RNA synthesis within the hepatitis C virus polypyrimidine tract.

D. Lamarre, G. Kukolj, G. McKercher, 2002, Biochemical and biophysical research communications.

An NS 3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

P. Bonneau, D. Lamarre, P. Anderson, 2003 .

101 SVR4 AND SVR12 WITH AN INTERFERON-FREE REGIMEN OF BI201335 AND BI207127, +/- RIBAVIRIN, IN TREATMENT-NAIVE PATIENTS WITH CHRONIC GENOTYPE-1 HCV INFECTION: INTERIM RESULTS OF SOUND-C2

M. Buti, T. Asselah, G. Kukolj, 2012 .

Efficacy of the protease inhibitor BI 201335, polymerase inhibitor BI 207127, and ribavirin in patients with chronic HCV infection.

T. Asselah, F. Zoulim, P. Angus, 2011, Gastroenterology.

Solution Structure of Substrate-based Ligands When Bound to Hepatitis C Virus NS3 Protease Domain*

D. Lamarre, S. LaPlante, G. Kukolj, 1999, The Journal of Biological Chemistry.

Potency, safety, and pharmacokinetics of the NS3/4A protease inhibitor BI201335 in patients with chronic HCV genotype-1 infection.

M. Manns, T. Berg, G. Kukolj, 2011, Journal of hepatology.

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

Peter W. White, J. Duan, M. Garneau, 2010, Antimicrobial Agents and Chemotherapy.

An NS 3 protease inhibitor with antiviral effects in humans infected with hepatitis C virus

P. Bonneau, D. Lamarre, P. Anderson, 2003 .

Binding mode determination of benzimidazole inhibitors of the hepatitis C virus RNA polymerase by a structure and dynamics strategy.

S. LaPlante, J. Gillard, A. Jakalian, 2004, Angewandte Chemie.

N-Acetamideindolecarboxylic acid allosteric 'finger-loop' inhibitors of the hepatitis C virus NS5B polymerase: discovery and initial optimization studies.

J. Duan, M. Garneau, C. Brochu, 2010, Bioorganic & medicinal chemistry letters.

Antiviral Activity of Bictegravir (GS-9883), a Novel Potent HIV-1 Integrase Strand Transfer Inhibitor with an Improved Resistance Profile

K. White, Helen Yu, G. Kukolj, 2016, Antimicrobial Agents and Chemotherapy.

Rapid and strong antiviral activity of the non-nucleosidic NS5B polymerase inhibitor BI 207127 in combination with peginterferon alfa 2a and ribavirin.

C. Trautwein, V. de Lédinghen, G. Gerken, 2012, Journal of hepatology.

Safety, pharmacokinetics and antiviral effect of BILB 1941, a novel hepatitis C virus RNA polymerase inhibitor, after 5 days oral treatment

X. Forns, P. Beaulieu, G. Kukolj, 2009, Antiviral therapy.

954 BI 201335, A POTENT HCV NS3 PROTEASE INHIBITOR, IN TREATMENT-NAIVE AND -EXPERIENCED CHRONIC HCV GENOTYPE-1 INFECTION: GENOTYPIC AND PHENOTYPIC ANALYSIS OF THE NS3 PROTEASE DOMAIN

M. Manns, G. Kukolj, S. Pol, 2009 .

758 CHARACTERIZATION OF RESISTANT MUTANTS SELECTED IN VITRO BY THE HCV NS3/4A PROTEASE INHIBITOR BI 201335

G. Kukolj, M. Massariol, P. White, 2010 .

777 PRECLINICAL CHARACTERIZATION OF NON-COVALENT HCV NS3/4A PROTEASE INHIBITOR BI 201335

J. Duan, M. Garneau, G. Kukolj, 2010 .

Resistance Analyses of HCV NS3/4A Protease and NS5B Polymerase from Clinical Studies of Deleobuvir and Faldaprevir

G. Kukolj, C. Sarrazin, D. Nelson, 2016, PloS one.

Anthranilic acid-based Thumb Pocket 2 HCV NS5B polymerase inhibitors with sub-micromolar potency in the cell-based replicon assay.

M. Garneau, S. LaPlante, R. Coulombe, 2013, Bioorganic & medicinal chemistry letters.

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

Araz Jakalian, Martin Poirier, Cédrickx Godbout, 2013, Bioorganic & medicinal chemistry letters.

Discovery of a novel series of non-nucleoside thumb pocket 2 HCV NS5B polymerase inhibitors.

Louise Thauvette, Araz Jakalian, M. Bös, 2013, Bioorganic & medicinal chemistry letters.

Binding Site Characterization and Resistance to a Class of Non-nucleoside Inhibitors of the Hepatitis C Virus NS5B Polymerase*

Louise Thauvette, Graham A. McGibbon, P. Beaulieu, 2005, Journal of Biological Chemistry.

Secondary structure and interaction of phage D108 Ner repressor with a 61-base-pair operator: evidence for altered protein and DNA structures in the complex.

G. Kukolj, M. Dubow, G. Thomas, 1994, Biochemistry.

Chronic Hepatitis C Polymerase Inhibitor, in Patients with an Investigational Hepatitis C Virus RNA Administration of Deleobuvir (BI 207127), Pharmacokinetics of Five-Day Oral Antiviral Effect, Safety, and

G. Kukolj, A. Lohse, M. Marquis, 2014 .

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

G. Kukolj, A. Lohse, M. Marquis, 2013, Antimicrobial Agents and Chemotherapy.

The Liver Partition Coefficient-Corrected Inhibitory Quotient and the Pharmacokinetic-Pharmacodynamic Relationship of Directly Acting Anti-Hepatitis C Virus Agents in Humans

J. Duan, M. Garneau, G. Kukolj, 2012, Antimicrobial Agents and Chemotherapy.

Identification of a lipid kinase as a host factor involved in hepatitis C virus RNA replication.

G. Kukolj, M. Cordingley, R. Bethell, 2009, Virology.

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

G. Kukolj, A. Quinson, J. Stern, 2015, Antimicrobial Agents and Chemotherapy.

HCVerso2: a phase III study of faldaprevir plus deleobuvir and ribavirin for chronic HCV genotype 1b infection in treatment naïve patients including those ineligible for pegylated interferon

T. Asselah, D. Ouzan, G. Kukolj, 2014 .

Baseline Hepatitis C Virus (HCV) NS3 Polymorphisms and Their Impact on Treatment Response in Clinical Studies of the HCV NS3 Protease Inhibitor Faldaprevir

G. Kukolj, M. Massariol, M. Marquis, 2013, Antimicrobial Agents and Chemotherapy.

Timing of DNA integration, transgenic mosaicism, and pronuclear microinjection

G. Kukolj, A. Skalka, A. Chan, 1999, Molecular reproduction and development.

Enhanced and coordinated processing of synapsed viral DNA ends by retroviral integrases in vitro.

G. Kukolj, A. Skalka, A M Skalka, 1995, Genes & development.

Role of DNA End Distortion in Catalysis by Avian Sarcoma Virus Integrase*

G. Kukolj, A. Skalka, R. Katz, 2001, The Journal of Biological Chemistry.

Development and Validation of a High-Throughput Screening Assay for the Hepatitis C Virus p7 Viroporin

G. Kukolj, P. White, C. Gervais, 2011, Journal of biomolecular screening.

Identification of NK Cell Subpopulations That Differentiate HIV-Infected Subject Cohorts with Diverse Levels of Virus Control

G. Nolan, A. Arvey, G. Kukolj, 2019, Journal of Virology.

Allosteric N-acetamide-indole-6-carboxylic acid thumb pocket 1 inhibitors of hepatitis C virus NS5B polymerase - Acylsulfonamides and acylsulfamides as carboxylic acid replacements

P. Kuhn, J. Duan, M. Garneau, 2013 .

Toll-Like Receptor 7 Agonist GS-9620 Induces HIV Expression and HIV-Specific Immunity in Cells from HIV-Infected Individuals on Suppressive Antiretroviral Therapy

G. Kukolj, T. Cihlar, D. Sloan, 2017, Journal of Virology.

Hepatitis C Virus Subgenomic Replicons in the Human Embryonic Kidney 293 Cell Line

D. Lamarre, G. Kukolj, Charles Pellerin, 2004, Journal of Virology.

Evaluation of Phosphatidylinositol-4-Kinase IIIα as a Hepatitis C Virus Drug Target

G. Kukolj, P. White, M. Cordingley, 2012, Journal of Virology.

Mechanisms of Hepatitis C Virus Drug Resistance

G. Kukolj, S. Ali, George Kukolj, 2009 .

Macrocyclic inhibitors of the NS3 protease as potential therapeutic agents of hepatitis C virus infection.

P. Bonneau, D. Lamarre, H. Nar, 2003, Angewandte Chemie.

From benzimidazole to indole-5-carboxamide Thumb Pocket I inhibitors of HCV NS5B polymerase. Part 1: indole C-2 SAR and discovery of diamide derivatives with nanomolar potency in cell-based subgenomic replicons.

J. Duan, M. Garneau, J. Gillard, 2011, Bioorganic & medicinal chemistry letters.

Sequence and phenotypic analysis for resistance monitoring in hepatitis C virus drug development: recommendations from the HCV DRAG.

Tara L. Kieffer, R. Schooley, C. Petropoulos, 2011, Gastroenterology.

Expression of green fluorescence protein in mammalian embryos: A novel reporter gene for the study of transgenesis and embryo development

G. Kukolj, A. Skalka, A. Chan, 1997 .

Discovery of benzimidazole-diamide finger loop (Thumb Pocket I) allosteric inhibitors of HCV NS5B polymerase: Implementing parallel synthesis for rapid linker optimization.

J. Gillard, M. Poirier, P. Beaulieu, 2010, Bioorganic & medicinal chemistry letters.

Enantiomeric atropisomers inhibit HCV polymerase and/or HIV matrix: characterizing hindered bond rotations and target selectivity.

O. Hucke, S. LaPlante, R. Coulombe, 2014, Journal of medicinal chemistry.

Structure-based design of novel HCV NS 5 B thumb pocket 2 allosteric inhibitors with submicromolar gt 1 replicon potency : Discovery of a

J. Duan, O. Hucke, R. Coulombe, 2013 .

AAV-HBV mouse model replicates immune exhaustion patterns of chronic HBV patients at single-cell level

O. Podlaha, G. Kukolj, E. van Gulck, 2023, bioRxiv.

Faldaprevir and deleobuvir for HCV genotype 1 infection.

M. Buti, T. Asselah, V. Soriano, 2013, The New England journal of medicine.