TY - JOUR
T1 - Blockers of the sars-cov-2 3a channel identified by targeted drug repurposing
AU - Tomar, Prabhat Pratap Singh
AU - Krugliak, Miriam
AU - Arkin, Isaiah T.
N1 - Publisher Copyright:
© 2021 by the authors. Licensee MDPI, Basel, Switzerland.
PY - 2021/3/23
Y1 - 2021/3/23
N2 - 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.
AB - 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.
KW - Antiviral drugs
KW - Bacterial assays
KW - Channel blockers
KW - Viral channels
UR - http://www.scopus.com/inward/record.url?scp=85103919743&partnerID=8YFLogxK
U2 - 10.3390/v13030532
DO - 10.3390/v13030532
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C2 - 33807095
AN - SCOPUS:85103919743
SN - 1999-4915
VL - 13
JO - Viruses
JF - Viruses
IS - 3
M1 - 532
ER -