- Title
- Antiviral Mechanisms of N-Phenyl Benzamides on Coxsackie Virus A9
- Creator
- Laajala, Mira
- Creator
- Kalander, Kerttu
- Creator
- Consalvi, Sara
- Creator
- Sheik Amamuddy, Olivier
- Creator
- Tastan Bishop, Özlem
- Creator
- Biava, Mariangela
- Creator
- Poce, Giovanna
- Creator
- Marjomäki, Varpu
- Subject
- To be catalogued
- Date Issued
- 2023
- Date
- 2023
- Type
- text
- Type
- article
- Identifier
- http://hdl.handle.net/10962/474448
- Identifier
- vital:77708
- Identifier
- https://doi.org/10.3390/pharmaceutics15031028
- Description
- Enteroviruses are one of the most abundant groups of viruses infecting humans, and yet there are no approved antivirals against them. To find effective antiviral compounds against enterovirus B group viruses, an in-house chemical library was screened. The most effective compounds against Coxsackieviruses B3 (CVB3) and A9 (CVA9) were CL212 and CL213, two N-phenyl benzamides. Both compounds were more effective against CVA9 and CL213 gave a better EC50 value of 1 µM with high a specificity index of 140. Both drugs were most effective when incubated directly with viruses suggesting that they mainly bound to the virions. A real-time uncoating assay showed that the compounds stabilized the virions and radioactive sucrose gradient as well as TEM confirmed that the viruses stayed intact. A docking assay, taking into account larger areas around the 2-and 3-fold axes of CVA9 and CVB3, suggested that the hydrophobic pocket gives the strongest binding to CVA9 but revealed another binding site around the 3-fold axis which could contribute to the binding of the compounds. Together, our data support a direct antiviral mechanism against the virus capsid and suggest that the compounds bind to the hydrophobic pocket and 3-fold axis area resulting in the stabilization of the virion
- Format
- 14 pages
- Format
- Language
- English
- Relation
- Pharmaceutics
- Relation
- Laajala M, Kalander K, Consalvi S, Amamuddy OS, Bishop ÖT, Biava M, Poce G, Marjomäki V. Antiviral Mechanisms of N-Phenyl Benzamides on Coxsackie Virus A9. Pharmaceutics. 2023; 15(3):1028. https://doi.org/10.3390/pharmaceutics15031028
- Relation
- Pharmaceutics volume 15 number 1028 2023 1999-4923
- Rights
- Author
- Rights
- Use of this resource is governed by the terms and conditions of the Creative Commons CC BY-NC-ND 4.0 License (Attribution-NonCommercial-NoDerivatives 4.0 International) https://creativecommons.org/licenses/by-nc-nd/4.0/
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Sheik Amamuddy, Olivier (Dr)
Tastan Bishop, Ozlem (Prof)
SDG 03. Good Health and Well-Being
RU Department of Biochemistry, Microbiology and Bioinformatics
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