Peptide-based inhibitors of hepatitis C virus full-length NS3 (protease-helicase/NTPase): model compounds towards small molecule inhibitors

K Oscarsson, A Poliakov, S Oscarson… - Bioorganic & medicinal …, 2003 - Elsevier
From l-α-aminobutyric acid (Abu) a set of electrophilic and non-electrophilic replacements
for the P1 cysteine of substrate and product inhibitors of hepatitis C virus full-length NS3 …

Tetrapeptides as potent protease inhibitors of hepatitis C virus full-length NS3 (protease-helicase/NTPase)

A Johansson, A Poliakov, E Åkerblom… - Bioorganic & medicinal …, 2002 - Elsevier
A library of tetrapeptides was evaluated for Hepatitis C Virus NS3 protease inhibitor activity
in an in vitro assay system comprising the native bifunctional full-length NS3 (protease …

Acyl sulfonamides as potent protease inhibitors of the hepatitis C virus full-Length NS3 (protease-helicase/NTPase): a comparative study of different C-terminals

A Johansson, A Poliakov, E Åkerblom… - Bioorganic & medicinal …, 2003 - Elsevier
Synthesis and inhibitory potencies of three types of protease inhibitors of the hepatitis C
virus (HCV) full-length NS3 (protease-helicase/NTPase) are reported:(i) inhibitors …

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

J Rancourt, DR Cameron, V Gorys… - Journal of medicinal …, 2004 - ACS Publications
The structure− activity relationship at the C-terminal position of peptide-based inhibitors of
the hepatitis C virus NS3 protease is presented. The observation that the N-terminal …

Phenylglycine as a novel P2 scaffold in hepatitis C virus NS3 protease inhibitors

P Örtqvist, SD Peterson, E Åkerblom, T Gossas… - Bioorganic & medicinal …, 2007 - Elsevier
Molecular modeling and inhibitory potencies of tetrapeptide protease inhibitors of HCV NS3
proposed phenylglycine as a new promising P2 residue. The results suggest that …

Inhibition of hepatitis C virus NS3 protease activity by product-based peptides is dependent on helicase domain

A Johansson, I Hubatsch, E Åkerblom… - Bioorganic & medicinal …, 2001 - Elsevier
Structure–activity relationships (SARs) of product-based inhibitors of hepatitis C virus NS3
protease were evaluated using an in vitro assay system comprising the native bifunctional …

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

M Llinàs-Brunet, MD Bailey, N Goudreau… - Journal of medicinal …, 2010 - ACS Publications
C-Terminal carboxylic acid containing inhibitors of the NS3 protease are reported. A novel
series of linear tripeptide inhibitors that are very potent and selective against the NS3 …

Exploration of acyl sulfonamides as carboxylic acid replacements in protease inhibitors of the hepatitis C virus full-length NS3

R Rönn, YA Sabnis, T Gossas, E Åkerblom… - Bioorganic & medicinal …, 2006 - Elsevier
The hepatitis C virus (HCV) NS3 protease has emerged as a promising anti-HCV drug
target. Herein, we present an investigation of NS3 inhibitors comprising the acyl sulfonamide …

Discovery of novel potent and selective dipeptide hepatitis C virus NS3/4A serine protease inhibitors

P Raboisson, TI Lin, H de Kock, S Vendeville… - Bioorganic & medicinal …, 2008 - Elsevier
Starting from the previously reported HCV NS3/4A protease inhibitor BILN 2061 (1), we have
used a fast-follower approach to identify a novel series of HCV NS3/4A protease inhibitors in …

Solid-phase synthesis of peptidomimetic inhibitors for the hepatitis C virus NS3 protease

MA Poupart, DR Cameron, C Chabot… - The Journal of …, 2001 - ACS Publications
The NS3 serine protease enzyme of the hepatitis C virus (HCV) is essential for viral
replication. Short peptides mimicking the N-terminal substrate cleavage products of the NS3 …