Effect of the extent of thiolation and introduction of phosphorothioate internucleotide linkages on the anti-HIV activity of Suligovir [(s4dU)35].
Suligovir is a 35-mer homo-oligonucleotide, containing exclusively 4-thio deoxyuridylate, proved to be a potent inhibitor of HIV entry. In this paper, we described the effect of extent of thiolation and the introduction of nuclease-resistant phosphorothioate linkages on the anti-HIV activity of Suligovir. We found that the decreased thiolated nucleotide content decreases the anti-HIV potency of the compound and the introduction of phosphorothioate linkages does not improve its antiviral activity.
Horváth
András
A
Department of Biochemistry and Molecular Biology, Medical and Health Science Center, Faculty of Medicine University of Debrecen, Life Science Building, Egyetem ter 1, Debrecen H-4010, Hungary.
Beck
Zoltán
Z
Bardos
Thomas J
TJ
Dunn
Joseph A
JA
Aradi
Janos
J
D019380:Anti-HIV Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D003856:Deoxyuracil Nucleotides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D006678:HIV / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D009841:Oligonucleotides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013873:Thionucleotides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology
C500998:(s4dU)35; D019380:Anti-HIV Agents; D003856:Deoxyuracil Nucleotides; D009841:Oligonucleotides; D013873:Thionucleotides