Stefano Elli, Denisa Bojkova, Marco Bechtel, Thomas Vial, David Boltz, Miguel Muzzio, Xinjian Peng, Federico Sala, Cesare Cosentino, Andrew Goy, Marco Guerrini, Lutz Müller, Jindrich Cinatl, Victor Margitich, Aartjan J. W. te Velthuis
- Pandemic SARS-CoV-2 causes a mild to severe respiratory disease called coronavirus disease 2019 (COVID-19). While control of the SARS-CoV-2 spread partly depends on vaccine-induced or naturally acquired protective herd immunity, antiviral strategies are still needed to manage COVID-19. Enisamium is an inhibitor of influenza A and B viruses in cell culture and clinically approved in countries of the Commonwealth of Independent States. In vitro, enisamium acts through metabolite VR17-04 and inhibits the activity of the influenza A virus RNA polymerase. Here we show that enisamium can inhibit coronavirus infections in NHBE and Caco-2 cells, and the activity of the SARS-CoV-2 RNA polymerase in vitro. Docking and molecular dynamics simulations provide insight into the mechanism of action and indicate that enisamium metabolite VR17-04 prevents GTP and UTP incorporation. Overall, these results suggest that enisamium is an inhibitor of SARS-CoV-2 RNA synthesis in vitro.
MetadatenAuthor: | Stefano ElliORCiD, Denisa BojkovaORCiDGND, Marco Bechtel, Thomas Vial, David Boltz, Miguel Muzzio, Xinjian Peng, Federico Sala, Cesare Cosentino, Andrew Goy, Marco GuerriniORCiD, Lutz MüllerORCiD, Jindrich CinatlORCiDGND, Victor Margitich, Aartjan J. W. te VelthuisORCiD |
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URN: | urn:nbn:de:hebis:30:3-692539 |
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DOI: | https://doi.org/10.3390/biomedicines9091254 |
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ISSN: | 2227-9059 |
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Parent Title (English): | Biomedicines |
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Publisher: | MDPI |
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Place of publication: | Basel |
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Document Type: | Article |
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Language: | English |
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Date of Publication (online): | 2021/09/17 |
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Date of first Publication: | 2021/09/17 |
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Publishing Institution: | Universitätsbibliothek Johann Christian Senckenberg |
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Release Date: | 2023/07/05 |
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Tag: | Amizon; COVID-19; FAV00A; RNA polymerase; SARS-CoV-2; molecular dynamics simulation |
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Volume: | 9 |
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Issue: | 9, art. 1254 |
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Article Number: | 1254 |
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Page Number: | 13 |
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First Page: | 1 |
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Last Page: | 13 |
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Note: | Part of this research was funded by Farmak Public Joint Stock Company, Kiev, Ukraine. |
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Note: | Data Availability Statement
Protein expression constructs are available upon request. |
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HeBIS-PPN: | 511285930 |
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Institutes: | Medizin / Medizin |
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Dewey Decimal Classification: | 6 Technik, Medizin, angewandte Wissenschaften / 61 Medizin und Gesundheit / 610 Medizin und Gesundheit |
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Sammlungen: | Universitätspublikationen |
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Licence (German): | Creative Commons - CC BY - Namensnennung 4.0 International |
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