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      Benzimidazole derivative, BM601, a novel inhibitor of hepatitis B virus and HBsAg secretion.

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          Abstract

          Hepatitis B virus (HBV) belongs to the Hepadnaviridae family. HBsAg, greatly outnumbered mature virion, has been mysterious since the discovery of HBV. A novel benzimidazole derivative, BM601, is identified inhibiting the secretion of HBV virions and HBsAg, with 50% effective concentration of 0.6μM and 1.5μM, as well as 50% cytotoxicity concentration of 24.5μM. It has no effect on transcription, protein production, nucleocapsid formation or intracellular HBV DNA synthesis. Immunofluorescence analysis suggests that BM601 might inhibit virion and HBsAg secretion by interfering surface protein aggregation in trans Golgi apparatus. Furthermore, BM601 does not trigger cellular stress response or affect HBeAg or host protein secretion. We hypothesize that BM601 is a secretion inhibitor functioning at the level of virion and HBsAg secretion pathway.

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          Author and article information

          Journal
          Antiviral Res.
          Antiviral research
          Elsevier BV
          1872-9096
          0166-3542
          Jul 2014
          : 107
          Affiliations
          [1 ] Laboratory of Immunopharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China.
          [2 ] Institute of Drug Discovery and Development, Shanghai Engineering Research Center of Molecular Therapeutics and New Drug Development, East China Normal University, China. Electronic address: wlu@chem.ecnu.edu.cn.
          [3 ] Laboratory of Immunopharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China. Electronic address: tangwei@mail.shcnc.ac.cn.
          [4 ] Laboratory of Immunopharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, China; Shanghai University of Traditional Chinese Medicine, China. Electronic address: jpzuo@mail.shcnc.ac.cn.
          Article
          S0166-3542(14)00108-9
          10.1016/j.antiviral.2014.04.002
          24746457
          6cb70f79-04c8-42be-9e28-da4162a9cdb0
          History

          Anti-hepatitis B virus compound,Benzimidazole derivative,Secretion inhibitor

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