Oligonucleotide n3'.fwdarw.p5' thiophosphoramidates: their...

Details Oligonucleotide n3'.fwdarw.p5' thiophosphoramidates: their... Oligonucleotide n3'.fwdarw.p5' thiophosphoramidates: their...

C - Chemistry, Metallurgy

07

H

C07H 21/00 (2006.01) A61K 31/7125 (2006.01) A61P 31/12 (2006.01) A61P 35/00 (2006.01) C12N 15/10 (2006.01) C12N 15/11 (2006.01) C12Q 1/68 (2006.01)

Patent

CA 2382521

Oligonucleotides with a novel sugar-phosphate backbone containing at least one internucleoside 3'-NHP(O)(S-)O-5' linkage, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive thiophosphoramidate oligonucleotides were found to retain the high RNA binding affinity of the parent oligonucleotide N3'.fwdarw.P5' phosphoramidates and to exhibit a much higher acid stability.

L'invention concerne des oligonucléotides comprenant un nouveau squelette phosphate-sucre contenant au moins une liaison 3'-NHP(O)(S<->)O-5' internucléosidique, et des méthodes de synthèse et d'utilisation des oligonucléotides de l'invention. Les oligonucléotides de thiophosphoramidate de l'invention conservent la grande affinité de liaison à l'ARN des phosphoramidates N3'}P5' oligonucléotidiques parents, et présentent une stabilité acide beaucoup plus élevée.

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