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List of works by George Kukolj

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).

scientific article published on 4 December 2014

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

scientific article (publication date: 13 November 2003)

An NS3 serine protease inhibitor abrogates replication of subgenomic hepatitis C virus RNA.

scientific article published on 19 March 2003

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

scientific article

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

scientific article

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 ⬇️

scientific article published on July 15, 2013

Aza follow-ups to BI 207524, a thumb pocket 1 HCV NS5B polymerase inhibitor. Part 1: Mitigating the genotoxic liability of an aniline metabolite

scientific article published on 17 December 2014

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

scientific article published on 11 November 2013

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

scientific article published on 6 February 2010

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

scientific article published on August 2004

Binding site characterization and resistance to a class of non-nucleoside inhibitors of the hepatitis C virus NS5B polymerase

scientific article published on 27 September 2005

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

scientific article published on 2 September 2014

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

scientific article published on 11 November 2013

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

scientific article published on 21 September 2014

Development and validation of a high-throughput screening assay for the hepatitis C virus p7 viroporin

scientific article

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

scientific article published on 10 April 2014

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

scientific article published on 25 November 2014

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

scientific article

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) ⬇️

scientific article published on August 16, 2012

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

scientific article

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

scientific article published on August 15, 2012

Faldaprevir and deleobuvir for HCV genotype 1 infection.

scientific article published on August 2013

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

scientific article published on June 2013

Faldaprevir combined with pegylated interferon alfa-2a and ribavirin in treatment-naïve patients with chronic genotype 1 HCV: SILEN-C1 trial.

scientific article published on June 2013

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

scientific article

Hepatitis C virus subgenomic replicons in the human embryonic kidney 293 cell line

scientific article published on January 2004

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

scientific article

Importance of Ligand Bioactive Conformation in the Discovery of Potent Indole-Diamide Inhibitors of the Hepatitis C Virus NS5B ⬇️

scientific article published on November 3, 2010

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

scientific article published on October 2006

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

scientific article published on October 24, 2011

Interferon regulatory factor 3-independent double-stranded RNA-induced inhibition of hepatitis C virus replicons in human embryonic kidney 293 cells.

scientific article published on March 2005

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

scientific article published in July 2002

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

scientific article published on July 12, 2013

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

scientific article published on December 27, 2012

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

scientific article published on 3 January 2015

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

scientific article

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

scientific article published on December 2004

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

scientific article

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

scientific article published on February 2004

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

scientific article published on September 7, 2010

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

scientific article published on 10 March 2012

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

scientific article published on 5 August 2016

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

scientific article published on 4 June 2014

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

scientific article published on 2 January 2015

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

scientific article published on January 2009

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

scientific article published on 19 January 2011

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

scientific article published on 22 January 2004

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

scientific article published on May 23, 2013

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

scientific article published on August 6, 2012

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

scientific article

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

scientific article published on 22 July 2013

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