Triple helix formation in oligonucleotide therapy

Details Triple helix formation in oligonucleotide therapy Triple helix formation in oligonucleotide therapy

C - Chemistry, Metallurgy

12

Q

C12Q 1/68 (2006.01) A61K 31/70 (2006.01) A61K 48/00 (2006.01) C07H 21/00 (2006.01) C12N 15/11 (2006.01)

Patent

CA 2071536

Oligonucleotides having tandem sequences of inverted polarity, i.e., oligonucleotides comprising regions of the formula: 3'-----5'--C--5'-----3' or 5'-----3'--C--3'-----5', wherein -C- symbolizes any method of coupling the nucleotide sequence of opposite polarity, are useful for forming an extended triple helix with a double- helical nucleotide duplex. Single or mixed motif oligomers may be used. The inverted polarity also stabilizes the single-strand oligonucleotides to exonuclease degradation.

Des oligonucléotides possédant des séquences en tandem à polarité inversée, c'est-à-dire des oligonucléotides comprenant des régions dont la formule est: 3'-----5'--C--5'-----3' ou 5'-----3'--C--3'-----5', où -C- symbolise tout procédé de couplage de la séquence nucléotidique à polarité opposée, sont utiles à la formation d'une triple chaîne hélicoïdale possédant un duplex nucléotidique à double hélice. On peut utiliser des oligomères à motifs simples ou mélangés. La polarité inversée sert également à rendre les oligonucléotides monocaténaires résistants à la dégradation par exonucléase.

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