Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations

Targeted protein degradation (TPD) is a promising strategy for drug development. In this proof-of-concept study, the authors use telaprevir, which binds hepatitis C virus (HCV) NS3/4A protease, to target the protease for protein degradation, and show inhibition of wildtype as well as drug resistant...

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Autores principales: Mélissanne de Wispelaere, Guangyan Du, Katherine A. Donovan, Tinghu Zhang, Nicholas A. Eleuteri, Jingting C. Yuan, Joann Kalabathula, Radosław P. Nowak, Eric S. Fischer, Nathanael S. Gray, Priscilla L. Yang
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Lenguaje:EN
Publicado: Nature Portfolio 2019
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Acceso en línea:https://doaj.org/article/5d5842f94e6549918072db60b50a3ebb
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spelling oai:doaj.org-article:5d5842f94e6549918072db60b50a3ebb2021-12-02T16:58:03ZSmall molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations10.1038/s41467-019-11429-w2041-1723https://doaj.org/article/5d5842f94e6549918072db60b50a3ebb2019-08-01T00:00:00Zhttps://doi.org/10.1038/s41467-019-11429-whttps://doaj.org/toc/2041-1723Targeted protein degradation (TPD) is a promising strategy for drug development. In this proof-of-concept study, the authors use telaprevir, which binds hepatitis C virus (HCV) NS3/4A protease, to target the protease for protein degradation, and show inhibition of wildtype as well as drug resistant HCV.Mélissanne de WispelaereGuangyan DuKatherine A. DonovanTinghu ZhangNicholas A. EleuteriJingting C. YuanJoann KalabathulaRadosław P. NowakEric S. FischerNathanael S. GrayPriscilla L. YangNature PortfolioarticleScienceQENNature Communications, Vol 10, Iss 1, Pp 1-11 (2019)
institution DOAJ
collection DOAJ
language EN
topic Science
Q
spellingShingle Science
Q
Mélissanne de Wispelaere
Guangyan Du
Katherine A. Donovan
Tinghu Zhang
Nicholas A. Eleuteri
Jingting C. Yuan
Joann Kalabathula
Radosław P. Nowak
Eric S. Fischer
Nathanael S. Gray
Priscilla L. Yang
Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations
description Targeted protein degradation (TPD) is a promising strategy for drug development. In this proof-of-concept study, the authors use telaprevir, which binds hepatitis C virus (HCV) NS3/4A protease, to target the protease for protein degradation, and show inhibition of wildtype as well as drug resistant HCV.
format article
author Mélissanne de Wispelaere
Guangyan Du
Katherine A. Donovan
Tinghu Zhang
Nicholas A. Eleuteri
Jingting C. Yuan
Joann Kalabathula
Radosław P. Nowak
Eric S. Fischer
Nathanael S. Gray
Priscilla L. Yang
author_facet Mélissanne de Wispelaere
Guangyan Du
Katherine A. Donovan
Tinghu Zhang
Nicholas A. Eleuteri
Jingting C. Yuan
Joann Kalabathula
Radosław P. Nowak
Eric S. Fischer
Nathanael S. Gray
Priscilla L. Yang
author_sort Mélissanne de Wispelaere
title Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations
title_short Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations
title_full Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations
title_fullStr Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations
title_full_unstemmed Small molecule degraders of the hepatitis C virus protease reduce susceptibility to resistance mutations
title_sort small molecule degraders of the hepatitis c virus protease reduce susceptibility to resistance mutations
publisher Nature Portfolio
publishDate 2019
url https://doaj.org/article/5d5842f94e6549918072db60b50a3ebb
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