Information de reference pour ce titreAccession Number: | 01515467-201307000-00014.
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Author: | Vausselin, Thibaut 1; Calland, Noemie 1; Belouzard, Sandrine 1; Descamps, Veronique 2; Douam, Florian 3,4,5; Helle, Francois 2; Francois, Catherine 2; Lavillette, Dimitri 3,4,5; Duverlie, Gilles 2; Wahid, Ahmed 1,6; Feneant, Lucie 1; Cocquerel, Laurence 1; Guerardel, Yann 7; Wychowski, Czeslaw 1; Biot, Christophe 7; Dubuisson, Jean 1
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Institution: | (1) Institut Pasteur de Lille, Center for Infection and Immunity of Lille, Lille, France; CNRS UMR8204, Lille, France; INSERM U1019, Lille, France; and Universite Lille Nord de France, Lille, France (2) Laboratoire de Virologie EA4294, Centre Hospitalier Universitaire d'Amiens, Universite de Picardie Jules Verne, Amiens, France (3) INSERM, U758, Human Virology Laboratory, Lyon, France (4) Ecole Normale Superieure de Lyon, Lyon, France (5) Universite de Lyon, UCB-Lyon1, Lyon, France (6) Department of Biochemistry, Faculty of Pharmacy, Minia University, Minia, Egypt (7) Universite Lille Nord de France, Universite Lille1, CNRS UMR8576, Villeneuve d'Ascq, France
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Title: | |
Source: | Hepatology. 58(1):86-97, July 2013.
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Abstract: | : Hepatitis C virus (HCV) is a major cause of chronic liver disease. Despite recent success in improving anti-HCV therapy, additional progress is still needed to develop cheaper and interferon (IFN)-free treatments. Here, we report that ferroquine (FQ), an antimalarial ferrocenic analog of chloroquine, is a novel inhibitor of HCV. FQ potently inhibited HCV infection of hepatoma cell lines by affecting an early step of the viral life cycle. The antiviral activity of FQ on HCV entry was confirmed with pseudoparticles expressing HCV envelope glycoproteins E1 and E2 from six different genotypes. In addition to its effect on HCV entry, FQ also inhibited HCV RNA replication, albeit at a higher concentration. We also showed that FQ has no effect on viral assembly and virion secretion. Using a binding assay at 4[degrees]C, we showed that FQ does not prevent attachment of the virus to the cell surface. Furthermore, virus internalization was not affected by FQ, whereas the fusion process was impaired in the presence of FQ as shown in a cell-cell fusion assay. Finally, virus with resistance to FQ was selected by sequential passage in the presence of the drug, and resistance was shown to be conferred by a single mutation in E1 glycoprotein (S327A). By inhibiting cell-free virus transmission using a neutralizing antibody, we also showed that FQ inhibits HCV cell-to-cell spread between neighboring cells. Combinations of FQ with IFN, or an inhibitor of HCV NS3/4A protease, also resulted in additive to synergistic activity. Conclusion: FQ is a novel, interesting anti-HCV molecule that could be used in combination with other direct-acting antivirals. (HEPATOLOGY 2013)
Copyright (C) 2013 John Wiley & Sons, Inc.
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Language: | English.
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Document Type: | Viral Hepatitis.
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Journal Subset: | Clinical Medicine.
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ISSN: | 0270-9139
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DOI Number: | https://dx.doi.org/10.1002/hep.2...- ouverture dans une nouvelle fenêtre
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