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Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing

The etiological agent of the COVID-19 pandemic is SARS-CoV-2. As a member of the Coronaviridae, the enveloped pathogen has several membrane proteins, of which two, E and 3a, were suggested to function as ion channels. In an effort to increase our treatment options, alongside providing new research t...

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Detalles Bibliográficos
Autores principales: Tomar, Prabhat Pratap Singh, Krugliak, Miriam, Arkin, Isaiah T.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2021
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8004704/
https://www.ncbi.nlm.nih.gov/pubmed/33807095
http://dx.doi.org/10.3390/v13030532
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author Tomar, Prabhat Pratap Singh
Krugliak, Miriam
Arkin, Isaiah T.
author_facet Tomar, Prabhat Pratap Singh
Krugliak, Miriam
Arkin, Isaiah T.
author_sort Tomar, Prabhat Pratap Singh
collection PubMed
description The etiological agent of the COVID-19 pandemic is SARS-CoV-2. As a member of the Coronaviridae, the enveloped pathogen has several membrane proteins, of which two, E and 3a, were suggested to function as ion channels. In an effort to increase our treatment options, alongside providing new research tools, we have sought to inhibit the 3a channel by targeted drug repurposing. To that end, using three bacteria-based assays, we screened a library of 2839 approved-for-human-use drugs and identified the following potential channel-blockers: Capreomycin, Pentamidine, Spectinomycin, Kasugamycin, Plerixafor, Flumatinib, Litronesib, Darapladib, Floxuridine and Fludarabine. The stage is now set for examining the activity of these compounds in detailed electrophysiological studies and their impact on the whole virus with appropriate biosafety measures.
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spelling pubmed-80047042021-03-29 Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing Tomar, Prabhat Pratap Singh Krugliak, Miriam Arkin, Isaiah T. Viruses Article The etiological agent of the COVID-19 pandemic is SARS-CoV-2. As a member of the Coronaviridae, the enveloped pathogen has several membrane proteins, of which two, E and 3a, were suggested to function as ion channels. In an effort to increase our treatment options, alongside providing new research tools, we have sought to inhibit the 3a channel by targeted drug repurposing. To that end, using three bacteria-based assays, we screened a library of 2839 approved-for-human-use drugs and identified the following potential channel-blockers: Capreomycin, Pentamidine, Spectinomycin, Kasugamycin, Plerixafor, Flumatinib, Litronesib, Darapladib, Floxuridine and Fludarabine. The stage is now set for examining the activity of these compounds in detailed electrophysiological studies and their impact on the whole virus with appropriate biosafety measures. MDPI 2021-03-23 /pmc/articles/PMC8004704/ /pubmed/33807095 http://dx.doi.org/10.3390/v13030532 Text en © 2021 by the authors. https://creativecommons.org/licenses/by/4.0/Licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution (CC BY) license (http://creativecommons.org/licenses/by/4.0/ (https://creativecommons.org/licenses/by/4.0/) ).
spellingShingle Article
Tomar, Prabhat Pratap Singh
Krugliak, Miriam
Arkin, Isaiah T.
Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing
title Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing
title_full Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing
title_fullStr Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing
title_full_unstemmed Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing
title_short Blockers of the SARS-CoV-2 3a Channel Identified by Targeted Drug Repurposing
title_sort blockers of the sars-cov-2 3a channel identified by targeted drug repurposing
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8004704/
https://www.ncbi.nlm.nih.gov/pubmed/33807095
http://dx.doi.org/10.3390/v13030532
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