Anti-viral guanosine-rich tetrad forming oligonucleotides

Details Anti-viral guanosine-rich tetrad forming oligonucleotides Anti-viral guanosine-rich tetrad forming oligonucleotides

C - Chemistry, Metallurgy

07

H

C07H 21/00 (2006.01) A61K 31/70 (2006.01) C07H 21/04 (2006.01) C12N 15/11 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2279488

Guanosine-rich oligonucleotides having sequences that favor the formation under physiological conditions of a stable four-stranded structure containing two stacked guanosine quartets (G4s) are disclosed. These oligonucleotides demonstrate enhanced nuclease resistance, cellular uptake and biological efficacy. Methods and composition for treating viral infection using these guanosine-rich oligonucleotides are also disclosed. Certain embodiments of the new oligonucleotides are 16-17 nucleotides long and contain at least one C-5 propynyl dU substitution. A method for designing anti-viral oligonucleotides is also disclosed.

On décrit des oligonucléotides riches en guanosine contenant des séquences qui favorisent la formation dans des conditions physiologiques d'une structure stable à quatre brins contenant deux quartets empilés (G4) de guanosine. Ces oligonucléotides présentent une meilleure résistance à la nucléase, une absorption cellulaire et une efficacité biologique accrues. Cette invention concerne également des procédés et une composition qui permettent de traiter des infections virales à l'aide de ces oligonucléotides riches en guanosine. Certaines formes de ces nouveaux oligonucléotides ont une longueur de 16-17 nucléotides et contiennent au moins une substitution propynyle dU en C-5. Un procédé de production de ces oligonucléotides antiviraux est également décrit.

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