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A new class of hepatitis B and D virus entry inhibitors, proanthocyanidin and its analogs, that directly act on the viral large surface proteins
Senko Tsukuda1,2, Koichi Watashi1,3,4, *, Taichi Hojima5, Masanori Isogawa6, Masashi Iwamoto1,3, Katsumi Omagari6, Ryosuke Suzuki1, Hideki Aizaki1, Soichi Kojima2, Masaya Sugiyama7, Akiko Saito5, Yasuhito Tanaka6, Masashi Mizokami7, Camille Sureau8 and Takaji Wakita1
Version of Record online: 17 JAN 2017
DOI: 10.1002 / hep.28952
© 2016 by the American Association for the Study of Liver Diseases.
Issue
Hepatology
Volume 65, Issue 4, pages 1104-1116, April 2017
Article has an altmetric score of 43
Author Information
1 Department of Virology II, National Institute of Infectious Diseases, Tokyo, Japan
2 Micro-Signaling Regulation Technology Unit, RIKEN CLST, Wako, Japan
3 Department of Applied Biological Science, Tokyo University of Science, Noda, Japan
4 CREST, Japan Science and Technology Agency (JST), Saitama, Japan
5 Department of Advanced Science and Engineering, Graduate School of Engineering, Osaka Electro-Communication University, Neyagawa, Japan
6 Department of Virology and Liver Unit, Nagoya City University Graduate School of Medicinal Sciences, Nagoya, Japan
7 Research Center for Hepatitis and Immunology, National Center for Global Health and Medicine, Ichikawa, Japan
8 Laboratoire de Virologie Moléculaire, Institut National de la Transfusion Sanguine, Paris, France
Email: Koichi Watashi ([email protected])
* ADDRESS CORRESPONDENCE AND REPRINT REQUESTS TO:
Koichi Watashi, Ph.D.
Department of Virology II, National Institute of Infectious Diseases
1-23-1 Toyama
Shinjuku-ku
Tokyo, 162-8640, Japan
E-mail: [email protected]
Tel: + 81-3-5285-1111
(HBV), especially viral-targeting compounds (HCV), have the necessary strategies for developing against antigiral compounds against hepatitis B virus (HBV), especially viral-targeting compounds (PAC) and its analogs, which inhibit HBV entry into host cells by targeting the HBV large surface protein (LHBs), which is an oligomeric flavonoid, . Through cell-based chemical screening, PAC was identified to inhibit HBV infection with little cytotoxic effect. PAC prevented the attachment of the preS1 region in the LHBs to its cellular receptor, sodium taurocholate cotransporting polypeptide (NTCP). PAC was shown to target HBV Particles and impair their infectivity, it did not affect the NTCP-mediated bile acid transport activity. Chemical biological techniques durability that PAC after interacted with the region essential for receptor binding in the preS1 region in the LHBs protein. Importantly, PAC had a pan -genotypic anti-HBV activity and was also effective against a clinically relevant nucleoside analog-resistant HBV isolate. We have derived that PAC augmented the ability of a nucleoside analog, tenofovir, to interrupt HBV spread over time in primary human hepatocytes by cotreatment. Quot; derivative analysis could identify small vio that blend more-potent anti-HBV activity over PAC. PAC and its analogs represent a new class of anti-HBV agents that directly target the preS1 region of the HBV large surface protein. These agents could Contribute to the development of a potent, well-tolerated, and broadly active inhibitor of HBV infection. (Hepatology 2017; 65: 1104-1116).
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