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Favipiravir strikes the SARS-CoV-2 at its Achilles heel, the RNA polymerase

The ongoing Corona Virus Disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), has emphasized the urgent need for antiviral therapeutics. The viral RNA-dependent-RNA-polymerase (RdRp) is a promising target with polymerase inhibitors successfully us...

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Autores principales: Shannon, A., Selisko, B., Le, NTT, Huchting, J., Touret, F., Piorkowski, G., Fattorini, V., Ferron, F., Decroly, E., Meier, C, Coutard, B., Peersen, O., Canard, B.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Cold Spring Harbor Laboratory 2020
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7263509/
https://www.ncbi.nlm.nih.gov/pubmed/32511380
http://dx.doi.org/10.1101/2020.05.15.098731
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author Shannon, A.
Selisko, B.
Le, NTT
Huchting, J.
Touret, F.
Piorkowski, G.
Fattorini, V.
Ferron, F.
Decroly, E.
Meier, C
Coutard, B.
Peersen, O.
Canard, B.
author_facet Shannon, A.
Selisko, B.
Le, NTT
Huchting, J.
Touret, F.
Piorkowski, G.
Fattorini, V.
Ferron, F.
Decroly, E.
Meier, C
Coutard, B.
Peersen, O.
Canard, B.
author_sort Shannon, A.
collection PubMed
description The ongoing Corona Virus Disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), has emphasized the urgent need for antiviral therapeutics. The viral RNA-dependent-RNA-polymerase (RdRp) is a promising target with polymerase inhibitors successfully used for the treatment of several viral diseases. Here we show that Favipiravir exerts an antiviral effect as a nucleotide analogue through a combination of chain termination, slowed RNA synthesis and lethal mutagenesis. The SARS-CoV RdRp complex is at least 10-fold more active than any other viral RdRp known. It possesses both unusually high nucleotide incorporation rates and high-error rates allowing facile insertion of Favipiravir into viral RNA, provoking C-to-U and G-to-A transitions in the already low cytosine content SARS-CoV-2 genome. The coronavirus RdRp complex represents an Achilles heel for SARS-CoV, supporting nucleoside analogues as promising candidates for the treatment of COVID-19.
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spelling pubmed-72635092020-06-07 Favipiravir strikes the SARS-CoV-2 at its Achilles heel, the RNA polymerase Shannon, A. Selisko, B. Le, NTT Huchting, J. Touret, F. Piorkowski, G. Fattorini, V. Ferron, F. Decroly, E. Meier, C Coutard, B. Peersen, O. Canard, B. bioRxiv Article The ongoing Corona Virus Disease 2019 (COVID-19) pandemic, caused by severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2), has emphasized the urgent need for antiviral therapeutics. The viral RNA-dependent-RNA-polymerase (RdRp) is a promising target with polymerase inhibitors successfully used for the treatment of several viral diseases. Here we show that Favipiravir exerts an antiviral effect as a nucleotide analogue through a combination of chain termination, slowed RNA synthesis and lethal mutagenesis. The SARS-CoV RdRp complex is at least 10-fold more active than any other viral RdRp known. It possesses both unusually high nucleotide incorporation rates and high-error rates allowing facile insertion of Favipiravir into viral RNA, provoking C-to-U and G-to-A transitions in the already low cytosine content SARS-CoV-2 genome. The coronavirus RdRp complex represents an Achilles heel for SARS-CoV, supporting nucleoside analogues as promising candidates for the treatment of COVID-19. Cold Spring Harbor Laboratory 2020-05-15 /pmc/articles/PMC7263509/ /pubmed/32511380 http://dx.doi.org/10.1101/2020.05.15.098731 Text en http://creativecommons.org/licenses/by-nd/4.0/It is made available under a CC-BY-ND 4.0 International license (http://creativecommons.org/licenses/by-nd/4.0/) .
spellingShingle Article
Shannon, A.
Selisko, B.
Le, NTT
Huchting, J.
Touret, F.
Piorkowski, G.
Fattorini, V.
Ferron, F.
Decroly, E.
Meier, C
Coutard, B.
Peersen, O.
Canard, B.
Favipiravir strikes the SARS-CoV-2 at its Achilles heel, the RNA polymerase
title Favipiravir strikes the SARS-CoV-2 at its Achilles heel, the RNA polymerase
title_full Favipiravir strikes the SARS-CoV-2 at its Achilles heel, the RNA polymerase
title_fullStr Favipiravir strikes the SARS-CoV-2 at its Achilles heel, the RNA polymerase
title_full_unstemmed Favipiravir strikes the SARS-CoV-2 at its Achilles heel, the RNA polymerase
title_short Favipiravir strikes the SARS-CoV-2 at its Achilles heel, the RNA polymerase
title_sort favipiravir strikes the sars-cov-2 at its achilles heel, the rna polymerase
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7263509/
https://www.ncbi.nlm.nih.gov/pubmed/32511380
http://dx.doi.org/10.1101/2020.05.15.098731
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