Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease (Q27473126)

6 July 2017

title

Preclinical profile of VX-950, a potent, selective, and orally bioavailable inhibitor of hepatitis C virus NS3-4A serine protease (English)

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6 July 2017

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Robert B Perni

1

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6 July 2017

Susan J Almquist

2

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6 July 2017

Randal A Byrn

3

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6 July 2017

Gurudatt Chandorkar

4

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6 July 2017

Pravin R Chaturvedi

5

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Lawrence F Courtney

6

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Caroline J Decker

7

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Kirk Dinehart

8

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Cynthia A Gates

9

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Scott L Harbeson

10

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Angela Heiser

11

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6 July 2017

Gururaj Kalkeri

12

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6 July 2017

Elaine Kolaczkowski

13

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6 July 2017

Kai Lin

14

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6 July 2017

Yu-Ping Luong

15

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B Govinda Rao

16

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6 July 2017

William P Taylor

17

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6 July 2017

John A Thomson

18

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6 July 2017

Roger D Tung

19

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6 July 2017

Yunyi Wei

20

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Ann D Kwong

21

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6 July 2017

Chao Lin

22

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6 July 2017

language of work or name

English

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publication date

1 March 2006

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Antimicrobial Agents and Chemotherapy

6 July 2017

number of pages

11

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based on heuristic

inferred from page(s)

published in

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6 July 2017

volume

50

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6 July 2017

issue

3

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6 July 2017

page(s)

899-909

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In Vitro Selection and Characterization of Hepatitis C Virus Serine Protease Variants Resistant to an Active-Site Peptide Inhibitor

6 July 2017

cites work

1 reference

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21 March 2017

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Inhibition of the hepatitis C virus NS3/4A protease. The crystal structures of two protease-inhibitor complexes

21 March 2017

1 reference

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Hepatitis C virus-encoded enzymatic activities and conserved RNA elements in the 3' nontranslated region are essential for virus replication in vivo

21 March 2017

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Crystal structure of the hepatitis C virus NS3 protease domain complexed with a synthetic NS4A cofactor peptide

21 March 2017

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21 March 2017

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A central region in the hepatitis C virus NS4A protein allows formation of an active NS3-NS4A serine proteinase complex in vivo and in vitro

21 March 2017

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21 March 2017

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21 March 2017

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Replication of subgenomic hepatitis C virus RNAs in a hepatoma cell line

21 March 2017

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Hepatitis C viral dynamics in vivo and the antiviral efficacy of interferon-alpha therapy

21 March 2017

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Alpha-ketoacids are potent slow binding inhibitors of the hepatitis C virus NS3 protease

21 March 2017

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Peginterferon-alpha2a and ribavirin combination therapy in chronic hepatitis C: a randomized study of treatment duration and ribavirin dose

21 March 2017

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Diagnosis, management, and treatment of hepatitis C

7 April 2017

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

7 April 2017

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Epidemiology of hepatitis C: geographic differences and temporal trends

7 April 2017

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Kinetics of the reversible inhibition of enzyme-catalysed reactions by tight-binding inhibitors

7 April 2017

1 reference

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Combination of a hepatitis C virus NS3-NS4A protease inhibitor and alpha interferon synergistically inhibits viral RNA replication and facilitates viral RNA clearance in replicon cells

7 April 2017

1 reference

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Short-term antiviral efficacy of BILN 2061, a hepatitis C virus serine protease inhibitor, in hepatitis C genotype 1 patients.

29 September 2017

1 reference

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Sensitivity of NS3 serine proteases from hepatitis C virus genotypes 2 and 3 to the inhibitor BILN 2061.

29 September 2017

1 reference

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

29 September 2017

1 reference

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Inhibitors of hepatitis C virus NS3.4A protease 2. Warhead SAR and optimization

29 September 2017

1 reference

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P1 and P3 optimization of novel bicycloproline P2 bearing tetrapeptidyl alpha-ketoamide based HCV protease inhibitors

29 September 2017

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1426435

NS3.4A protease as a target for interfering with hepatitis C virus replication.

29 September 2017

1 reference

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Approaching a new era for hepatitis C virus therapy: inhibitors of the NS3-4A serine protease and the NS5B RNA-dependent RNA polymerase.

29 September 2017

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National Institutes of Health Consensus Development Conference Statement: Management of hepatitis C: 2002--June 10-12, 2002.

29 September 2017

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Hepatitis C: an epidemiological review

29 September 2017

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The hepatitis C virus NS3 serine proteinase and NS4A cofactor: establishment of a cell-free trans-processing assay

29 September 2017

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The behavior and significance of slow-binding enzyme inhibitors

29 September 2017

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Molecular characterization and dynamics of hepatitis C virus replication in human fetal hepatocytes infected in vitro

29 September 2017

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Mechanistic role of an NS4A peptide cofactor with the truncated NS3 protease of hepatitis C virus: elucidation of the NS4A stimulatory effect via kinetic analysis and inhibitor mapping

2 June 2018

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Purification and characterization of the NS3 serine protease domain of hepatitis C virus expressed in Saccharomyces cerevisiae.

2 June 2018

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

2 June 2018

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Antiviral efficacy of NS3-serine protease inhibitor BILN-2061 in patients with chronic genotype 2 and 3 hepatitis C.

27 November 2018

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https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1426435

P4 and P1' optimization of bicycloproline P2 bearing tetrapeptidyl alpha-ketoamides as HCV protease inhibitors

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1426435

P4 cap modified tetrapeptidyl alpha-ketoamides as potent HCV NS3 protease inhibitors

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1426435

Inhibitors of hepatitis C virus NS3.4A protease. Part 3: P2 proline variants

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1426435

In vitro resistance studies of hepatitis C virus serine protease inhibitors, VX-950 and BILN 2061: structural analysis indicates different resistance mechanisms

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1426435

Discovery of a novel bicycloproline P2 bearing peptidyl alpha-ketoamide LY514962 as HCV protease inhibitor

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1426435

Inhibitors of hepatitis C virus NS3·4A protease 1. Non-Charged tetrapeptide variants

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1426435

A continuous assay of hepatitis C virus protease based on resonance energy transfer depsipeptide substrates

27 November 2018

1 reference

https://eutils.ncbi.nlm.nih.gov/entrez/eutils/elink.fcgi?dbfrom=pmc&linkname=pmc_refs_pubmed&retmode=json&id=1426435

Characterization of the two-step pathway for inhibition of thrombin by alpha-ketoamide transition state analogs

27 November 2018

1 reference

PubMed

https://pubmed.ncbi.nlm.nih.gov/16495249

inferred from PubMed ID database lookup

12 December 2020

based on heuristic

Identifiers

DOI

10.1128/AAC.50.3.899-909.2006

1 reference

6 July 2017

1 reference

6 July 2017

1 reference