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PBDE: Structure-Activity Studies for the Inhibition of Hepatitis C Virus NS3 Helicase
The helicase portion of the hepatitis C virus nonstructural protein 3 (NS3) is considered one of the most validated targets for developing direct acting antiviral agents. We isolated polybrominated diphenyl ether (PBDE) 1 from a marine sponge as an NS3 helicase inhibitor. In this study, we evaluated...
Autores principales: | , , , , , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2014
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271602/ https://www.ncbi.nlm.nih.gov/pubmed/24699145 http://dx.doi.org/10.3390/molecules19044006 |
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author | Salam, Kazi Abdus Furuta, Atsushi Noda, Naohiro Tsuneda, Satoshi Sekiguchi, Yuji Yamashita, Atsuya Moriishi, Kohji Nakakoshi, Masamichi Tani, Hidenori Roy, Sona Rani Tanaka, Junichi Tsubuki, Masayoshi Akimitsu, Nobuyoshi |
author_facet | Salam, Kazi Abdus Furuta, Atsushi Noda, Naohiro Tsuneda, Satoshi Sekiguchi, Yuji Yamashita, Atsuya Moriishi, Kohji Nakakoshi, Masamichi Tani, Hidenori Roy, Sona Rani Tanaka, Junichi Tsubuki, Masayoshi Akimitsu, Nobuyoshi |
author_sort | Salam, Kazi Abdus |
collection | PubMed |
description | The helicase portion of the hepatitis C virus nonstructural protein 3 (NS3) is considered one of the most validated targets for developing direct acting antiviral agents. We isolated polybrominated diphenyl ether (PBDE) 1 from a marine sponge as an NS3 helicase inhibitor. In this study, we evaluated the inhibitory effects of PBDE (1) on the essential activities of NS3 protein such as RNA helicase, ATPase, and RNA binding activities. The structure-activity relationship analysis of PBDE (1) against the HCV ATPase revealed that the biphenyl ring, bromine, and phenolic hydroxyl group on the benzene backbone might be a basic scaffold for the inhibitory potency. |
format | Online Article Text |
id | pubmed-6271602 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2014 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62716022019-01-02 PBDE: Structure-Activity Studies for the Inhibition of Hepatitis C Virus NS3 Helicase Salam, Kazi Abdus Furuta, Atsushi Noda, Naohiro Tsuneda, Satoshi Sekiguchi, Yuji Yamashita, Atsuya Moriishi, Kohji Nakakoshi, Masamichi Tani, Hidenori Roy, Sona Rani Tanaka, Junichi Tsubuki, Masayoshi Akimitsu, Nobuyoshi Molecules Article The helicase portion of the hepatitis C virus nonstructural protein 3 (NS3) is considered one of the most validated targets for developing direct acting antiviral agents. We isolated polybrominated diphenyl ether (PBDE) 1 from a marine sponge as an NS3 helicase inhibitor. In this study, we evaluated the inhibitory effects of PBDE (1) on the essential activities of NS3 protein such as RNA helicase, ATPase, and RNA binding activities. The structure-activity relationship analysis of PBDE (1) against the HCV ATPase revealed that the biphenyl ring, bromine, and phenolic hydroxyl group on the benzene backbone might be a basic scaffold for the inhibitory potency. MDPI 2014-04-02 /pmc/articles/PMC6271602/ /pubmed/24699145 http://dx.doi.org/10.3390/molecules19044006 Text en © 2014 by the authors. Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article Salam, Kazi Abdus Furuta, Atsushi Noda, Naohiro Tsuneda, Satoshi Sekiguchi, Yuji Yamashita, Atsuya Moriishi, Kohji Nakakoshi, Masamichi Tani, Hidenori Roy, Sona Rani Tanaka, Junichi Tsubuki, Masayoshi Akimitsu, Nobuyoshi PBDE: Structure-Activity Studies for the Inhibition of Hepatitis C Virus NS3 Helicase |
title | PBDE: Structure-Activity Studies for the Inhibition of Hepatitis C Virus NS3 Helicase |
title_full | PBDE: Structure-Activity Studies for the Inhibition of Hepatitis C Virus NS3 Helicase |
title_fullStr | PBDE: Structure-Activity Studies for the Inhibition of Hepatitis C Virus NS3 Helicase |
title_full_unstemmed | PBDE: Structure-Activity Studies for the Inhibition of Hepatitis C Virus NS3 Helicase |
title_short | PBDE: Structure-Activity Studies for the Inhibition of Hepatitis C Virus NS3 Helicase |
title_sort | pbde: structure-activity studies for the inhibition of hepatitis c virus ns3 helicase |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6271602/ https://www.ncbi.nlm.nih.gov/pubmed/24699145 http://dx.doi.org/10.3390/molecules19044006 |
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