Targeting G-quadruplex in SARS-CoV-2 RNA Genome with Tetraphenylethene Derivatives for Antiviral Therapy

05 June 2023, Version 1


Targeting genomic RNA conformations that are crucial for SARS-CoV-2 replication is a promising antiviral strategy. Herein we have developed tetraphenylethene (TPE) derivatives to target RNA G-quadruplexes (RGQs) present in the SARS-CoV-2 nucleocapsid gene ORF. Our EMSA, fluorescence and CD data suggests the binding of two TPE derivatives i.e., TPE−MePy and TPE-AllylPy, with RGQ derived from SARS-CoV-2 nucleocapsid gene. In addition, in vitro luciferase assay demonstrated suppression in translation efficiency by 3.86-fold and 2.89-fold in presence of TPE-MePy and TPE-AllylPy, respectively. Subsequently, the cytotoxicity and immunofluorescence-based antiviral assay in VeroE6 cells indicated 82% inhibition in SARS-CoV-2 nucleocapsid gene expression without any effect on cell viability. These results highlight the promising use of TPE derivatives as an antiviral drug to alter the crucial genes expression in SARS-CoV-2 as well as other viruses.


Supplementary materials

Supporting information
Supporting information contains synthesis procedure details, NMR characterisation data, EMSA, Fluorescence, CD, and immunofluorescence-based antiviral screening assay protocols.


Comments are not moderated before they are posted, but they can be removed by the site moderators if they are found to be in contravention of our Commenting Policy [opens in a new tab] - please read this policy before you post. Comments should be used for scholarly discussion of the content in question. You can find more information about how to use the commenting feature here [opens in a new tab] .
This site is protected by reCAPTCHA and the Google Privacy Policy [opens in a new tab] and Terms of Service [opens in a new tab] apply.