Cargando…

Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library

SARS-CoV-2, the etiological agent of the COVID-19 pandemic, is a member of the Coronaviridae family. It is an enveloped virus with ion channels in its membrane, the most characterized of which is the E protein. Therefore, in an attempt to identify blockers of the E channel, we screened a library of...

Descripción completa

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/PMC8308726/
https://www.ncbi.nlm.nih.gov/pubmed/34201587
http://dx.doi.org/10.3390/ph14070604
_version_ 1783728350011850752
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 SARS-CoV-2, the etiological agent of the COVID-19 pandemic, is a member of the Coronaviridae family. It is an enveloped virus with ion channels in its membrane, the most characterized of which is the E protein. Therefore, in an attempt to identify blockers of the E channel, we screened a library of 2839 approved-for-human-use drugs. Our approach yielded eight compounds that exhibited appreciable activity in three bacteria-based channel assays. Considering the fact that the E channel is the most conserved of all SARS-CoV-2 proteins, any inhibitor of its activity may provide an option to curb the viral spread. In addition, inhibitors can also enhance our ability to understand the exact role played by the E protein during the infectivity cycle. Finally, detailed electrophysiological analyses, alongside in vitro and in vivo studies will be needed to establish the exact potential of each of the blockers identified in our study.
format Online
Article
Text
id pubmed-8308726
institution National Center for Biotechnology Information
language English
publishDate 2021
publisher MDPI
record_format MEDLINE/PubMed
spelling pubmed-83087262021-07-25 Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library Tomar, Prabhat Pratap Singh Krugliak, Miriam Arkin, Isaiah T. Pharmaceuticals (Basel) Article SARS-CoV-2, the etiological agent of the COVID-19 pandemic, is a member of the Coronaviridae family. It is an enveloped virus with ion channels in its membrane, the most characterized of which is the E protein. Therefore, in an attempt to identify blockers of the E channel, we screened a library of 2839 approved-for-human-use drugs. Our approach yielded eight compounds that exhibited appreciable activity in three bacteria-based channel assays. Considering the fact that the E channel is the most conserved of all SARS-CoV-2 proteins, any inhibitor of its activity may provide an option to curb the viral spread. In addition, inhibitors can also enhance our ability to understand the exact role played by the E protein during the infectivity cycle. Finally, detailed electrophysiological analyses, alongside in vitro and in vivo studies will be needed to establish the exact potential of each of the blockers identified in our study. MDPI 2021-06-23 /pmc/articles/PMC8308726/ /pubmed/34201587 http://dx.doi.org/10.3390/ph14070604 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 (https://creativecommons.org/licenses/by/4.0/).
spellingShingle Article
Tomar, Prabhat Pratap Singh
Krugliak, Miriam
Arkin, Isaiah T.
Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library
title Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library
title_full Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library
title_fullStr Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library
title_full_unstemmed Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library
title_short Identification of SARS-CoV-2 E Channel Blockers from a Repurposed Drug Library
title_sort identification of sars-cov-2 e channel blockers from a repurposed drug library
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8308726/
https://www.ncbi.nlm.nih.gov/pubmed/34201587
http://dx.doi.org/10.3390/ph14070604
work_keys_str_mv AT tomarprabhatpratapsingh identificationofsarscov2echannelblockersfromarepurposeddruglibrary
AT krugliakmiriam identificationofsarscov2echannelblockersfromarepurposeddruglibrary
AT arkinisaiaht identificationofsarscov2echannelblockersfromarepurposeddruglibrary