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Anti-HIV-1 Activity of pepRF1, a Proteolysis-Resistant CXCR4 Antagonist Derived from Dengue Virus Capsid Protein

Abstract : There is an urgent need for the development of new anti-HIV drugs that can complement existing medicines to be used against resistant strains. Here, we report the anti-HIV-1 peptide pepRF1, a human serum-resistant peptide derived from the Dengue virus capsid protein. In vitro, pepRF1 shows a 50% inhibitory concentration of 1.5 nM with a potential therapeutic window higher than 53 000. This peptide is specific for CXCR4-tropic strains, preventing viral entry into target cells by binding to the viral coreceptor CXCR4, acting as an antagonist of this receptor. pepRF1 is more effective than T20, the only peptide-based HIV-1 entry inhibitor approved, and excels in inhibiting a HIV-1 strain resistant to T20. Potentially, pepRF1 can be used alone or in combination with other anti-HIV drugs. Furthermore, one can also envisage its use as a novel therapeutic strategy for other CXCR4-related diseases.
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https://www.hal.inserm.fr/inserm-03451808
Contributor : Fabrizio Mammano Connect in order to contact the contributor
Submitted on : Friday, November 26, 2021 - 4:17:18 PM
Last modification on : Wednesday, December 1, 2021 - 3:08:57 AM

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Iris Cadima-Couto, Alexandra Tauzin, João Freire, Tiago Figueira, Rúben Silva, et al.. Anti-HIV-1 Activity of pepRF1, a Proteolysis-Resistant CXCR4 Antagonist Derived from Dengue Virus Capsid Protein. ACS Infectious Diseases, American Chemical Society, 2021, 7 (1), pp.6-22. ⟨10.1021/acsinfecdis.9b00507⟩. ⟨inserm-03451808⟩

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