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Stapled peptide-based membrane fusion inhibitors of hepatitis C virus |
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| Authors: | Hong-Kui Cui Jie Qing Ye Guo Yu-Jia Wang Li-Jia Cui Tian-Hua He Linqi Zhang Lei Liu |
| Institution: | 1. Tsinghua-Peking Center for Life Sciences, Key Laboratory of Bioorganic Phosphorus Chemistry & Chemical Biology (Ministry of Education), Department of Chemistry, Tsinghua University, Beijing 100084, China;2. Comprehensive AIDS Research Center and Research Center for Public Health, School of Medicine, Tsinghua University, Beijing 100084, China;1. Max Planck Institut (MPI) für Molekulare Physiologie, Dept. of Chemical Biology, Otto-Hahn-Strasse 11, Dortmund, 44026, Germany |
| Abstract: | The strategy of peptide stapling was used to develop new molecules to inhibit the hepatitis C virus infection via disrupting the binding of HCV envelope glycoprotein E2 with human cell surface protein CD81. The peptide sequence was designed based on the large extra-cellular loop of CD81 with known importance in the HCV E2 binding interaction. Our results showed that the stapled peptides exhibited significantly higher α-helicity and proteolytic stability as compared to their linear peptide counterpart. The optimal compound was found to have an EC50 value of ca. 17–39 μM against different HCV subtypes and represented a new HCV membrane fusion inhibitor. |
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