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Anti-HIV-1 activity of the G-quadruplex ligand BRACO-19
Author(s) -
Rosalba Perrone,
Elena Butovskaya,
Dirk Daelemans,
Giorgio Palù,
Christophe Pannecouque,
Sara N. Richter
Publication year - 2014
Publication title -
journal of antimicrobial chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.124
H-Index - 194
eISSN - 1460-2091
pISSN - 0305-7453
DOI - 10.1093/jac/dku280
Subject(s) - biology , reverse transcriptase , dna , transcription (linguistics) , g quadruplex , rna , microbiology and biotechnology , virology , biochemistry , gene , linguistics , philosophy
A dynamic G-quadruplex region has been previously shown to form in the long terminal repeat (LTR) promoter of the HIV-1 integrated DNA genome. Inhibition of promoter activity and antiviral effects have been observed when this region was stabilized by BRACO-19, a trisubstituted acridine derivative that binds G-quadruplexes. Here, we aimed at characterizing the antiviral mechanism of action of BRACO-19 by analysing its activity towards a broad range of HIV-1 strains, host cells and infection modes.

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