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...

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Autores principales: 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
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2014
Materias:
Article
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.
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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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