Comparison of anti-SARS-CoV-2 activity and intracellular metabolism of remdesivir and its parent nucleoside.
ACE2, angiotensin-converting enzyme 2
Anti-SARS-CoV-2
Antiviral agents
CES1, carboxylesterase 1
COVID-19
COVID-19, coronavirus disease 2019
CatA, cathepsin A
Coronavirus
DP, diphosphate
GS-441524
HAE, human airway epithelial
HCoV-OC43
HINT1, histidine triad nucleotide-binding protein 1
MP, monophosphate
NTP, nucleoside triphosphate
Pharmacology
Remdesivir
SARS-CoV-2, severe acute respiratory syndrome coronavirus 2
TP, triphosphate
WHO, World Health Organization
icSARS-CoV-2-mNG, SARS-CoV-2 infectious clone virus containing mNeonGreen reporter
Journal
Current research in pharmacology and drug discovery
ISSN: 2590-2571
Titre abrégé: Curr Res Pharmacol Drug Discov
Pays: Netherlands
ID NLM: 9918300982506676
Informations de publication
Date de publication:
2021
2021
Historique:
received:
30
06
2021
revised:
05
08
2021
accepted:
08
08
2021
entrez:
6
12
2021
pubmed:
7
12
2021
medline:
7
12
2021
Statut:
ppublish
Résumé
Remdesivir, a monophosphate prodrug of nucleoside analog GS-441524, is widely used for the treatment of moderate to severe COVID-19. It has been suggested to use GS-441524 instead of remdesivir in the clinic and in new inhalation formulations. Thus, we compared the anti-SARS-CoV-2 activity of remdesivir and GS-441524 in Vero E6, Vero CCL-81, Calu-3, Caco-2 cells, and anti-HCoV-OC43 activity in Huh-7 cells. We also compared the cellular pharmacology of these two compounds in Vero E6, Vero CCL-81, Calu-3, Caco-2, Huh-7, 293T, BHK-21, 3T3 and human airway epithelial (HAE) cells. Overall, remdesivir exhibited greater potency and superior intracellular metabolism than GS-441524 except in Vero E6 and Vero CCL-81 cells.
Identifiants
pubmed: 34870151
doi: 10.1016/j.crphar.2021.100045
pii: S2590-2571(21)00032-8
pmc: PMC8357487
doi:
Types de publication
Journal Article
Langues
eng
Pagination
100045Subventions
Organisme : NIAID NIH HHS
ID : P30 AI050409
Pays : United States
Organisme : NIAID NIH HHS
ID : R01 AI121315
Pays : United States
Organisme : NIAID NIH HHS
ID : R01 AI141327
Pays : United States
Informations de copyright
© 2021 The Authors.
Déclaration de conflit d'intérêts
The authors declare that they have no known competing financial interests or personal relationships that could have appeared to influence the work reported in this paper.
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