TY  - JOUR
A1  - Elli, Stefano
A1  - Bojkova, Denisa
A1  - Bechtel, Marco
A1  - Vial, Thomas
A1  - Boltz, David
A1  - Muzzio, Miguel
A1  - Peng, Xinjian
A1  - Sala, Federico
A1  - Cosentino, Cesare
A1  - Goy, Andrew
A1  - Guerrini, Marco
A1  - Müller, Lutz
A1  - Cinatl, Jindrich
A1  - Margitich, Victor
A1  - Velthuis, Aartjan J. W. te
T1  - Enisamium inhibits SARS-CoV-2 RNA synthesis
T2  - Biomedicines
N2  - 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.
KW  - COVID-19
KW  - SARS-CoV-2
KW  - molecular dynamics simulation
KW  - RNA polymerase
KW  - FAV00A
KW  - Amizon
Y1  - 2021
UR  - http://publikationen.ub.uni-frankfurt.de/frontdoor/index/index/docId/69253
UR  - https://nbn-resolving.org/urn:nbn:de:hebis:30:3-692539
SN  - 2227-9059
N1  - Part of this research was funded by Farmak Public Joint Stock Company, Kiev, Ukraine.
N1  - Data Availability Statement
Protein expression constructs are available upon request.
VL  - 9
IS  - 9, art. 1254
SP  - 1
EP  - 13
PB  - MDPI
CY  - Basel
ER  -