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Hepatitis C Virus NS3/4A Protease Inhibitors: A Light at the End of the Tunnel.


ABSTRACT: Hepatitis C virus (HCV) infection is a serious and growing threat to human health. The current treatment provides limited efficacy and is poorly tolerated, highlighting the urgent medical need for novel therapeutics. The membrane-targeted NS3 protein in complex with the NS4A comprises a serine protease domain (NS3/4A protease) that is essential for viral polyprotein maturation and contributes to the evasion of the host innate antiviral immunity by HCV. Therefore, the NS3/4A protease represents an attractive target for drug discovery, which is tied in with the challenge to develop selective small-molecule inhibitors. A rational drug design approach, based on the discovery of N-terminus product inhibition, led to the identification of potent and orally bioavailable NS3 inhibitors that target

SUBMITTER: Chatel-Chaix L 

PROVIDER: S-EPMC3185733 | biostudies-literature | 2010 Aug

REPOSITORIES: biostudies-literature