Article ; Online: SARS-CoV-2 E protein is a potential ion channel that can be inhibited by Gliclazide and Memantine.
Biochemical and biophysical research communications
2020 Volume 530, Issue 1, Page(s) 10–14
Abstract: ... library of ion channel blockers yielded two compounds that inhibit the E protein: Gliclazide and Memantine ... the E protein, is a potential ion channel and, therefore, is an excellent drug target. Channel activity ... In conclusion, as a route to curb viral virulence and abate COVID-19, we point to the E protein of SARS-CoV-2 ...
| Abstract | COVID-19 is one of the most impactful pandemics in recorded history. As such, the identification of inhibitory drugs against its etiological agent, SARS-CoV-2, is of utmost importance, and in particular, repurposing may provide the fastest route to curb the disease. As the first step in this route, we sought to identify an attractive and viable target in the virus for pharmaceutical inhibition. Using three bacteria-based assays that were tested on known viroporins, we demonstrate that one of its essential components, the E protein, is a potential ion channel and, therefore, is an excellent drug target. Channel activity was demonstrated for E proteins in other coronaviruses, providing further emphasis on the importance of this functionally to the virus' pathogenicity. The results of a screening effort involving a repurposing drug library of ion channel blockers yielded two compounds that inhibit the E protein: Gliclazide and Memantine. In conclusion, as a route to curb viral virulence and abate COVID-19, we point to the E protein of SARS-CoV-2 as an attractive drug target and identify off-label compounds that inhibit it. |
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| MeSH term(s) | Antiviral Agents/pharmacology ; Betacoronavirus/drug effects ; Betacoronavirus/metabolism ; COVID-19 ; Coronavirus Envelope Proteins ; Coronavirus Infections/drug therapy ; Coronavirus Infections/virology ; Drug Discovery ; Drug Repositioning ; Gliclazide/pharmacology ; Humans ; Ion Channels/antagonists & inhibitors ; Ion Channels/metabolism ; Memantine/pharmacology ; Pandemics ; Pneumonia, Viral/drug therapy ; Pneumonia, Viral/virology ; SARS-CoV-2 ; Viral Envelope Proteins/antagonists & inhibitors ; Viral Envelope Proteins/metabolism |
| Chemical Substances | Antiviral Agents ; Coronavirus Envelope Proteins ; Ion Channels ; Viral Envelope Proteins ; envelope protein, SARS-CoV-2 ; Gliclazide (G4PX8C4HKV) ; Memantine (W8O17SJF3T) |
| Keywords | covid19 |
| Language | English |
| Publishing date | 2020-06-20 |
| Publishing country | United States |
| Document type | Journal Article |
| ZDB-ID | 205723-2 |
| ISSN | 1090-2104 ; 0006-291X ; 0006-291X |
| ISSN (online) | 1090-2104 ; 0006-291X |
| ISSN | 0006-291X |
| DOI | 10.1016/j.bbrc.2020.05.206 |
| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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