Anti-HIV-1 Activity of pepRF1, a Proteolysis-Resistant CXCR4 Antagonist Derived from Dengue Virus Capsid Protein - Archive ouverte HAL Access content directly
Journal Articles ACS Infectious Diseases Year : 2021

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

(1) , (2) , (1) , (1) , (1) , (3) , (1) , (1) , (1, 4) , (1) , (1) , (1) , (2) , (3) , (1) , (1)
1
2
3
4
David Andreu

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.
Embargoed file
Embargoed file
Ne sera jamais visible

Dates and versions

inserm-03451808 , version 1 (26-11-2021)

Identifiers

Cite

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

Altmetric

Share

Gmail Facebook Twitter LinkedIn More