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Overview
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Background
Telaprevir (also known as VX-950), derived from the viral NS5A/5B substrate of the protease through structure-based techniques, is a novel and potent inhibitor of hepatitis C virus (HCV) NS3-4A protease, which covalently and reversibly inhibit the NS3-4A protease via a slow-binding and slow-dissociation mechanism. Results of multiple studies show that telaprevir potently inhibits a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide with the inhibitory constant (Ki) of 7 nM, exhibits strong anti-HCV in HCV replicon cells in vitro, and suppresses HCV replication as well as the emergence of resistance in HCV replicon cells with a synergistic effect with IFN-α.
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- Properties
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Overview