Novel oligonucleotides modified with non-nucleotide bridging...

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) A61K 31/70 (2006.01) A61K 48/00 (2006.01)

Patent

CA 2153057

An oligonucleotide having a structural formula selected from the group consisting of (a) and (b). S1, S2, S3, S4, and S5 are oligonucleotide strands, and each of X1 and X2 is a bridging moiety which may be a nucleotide strand or a non-nucleotide bridging moiety. Each of X1 and X2 may be the same or different, with the proviso that when one of X1 and X2 is a nucleotide strand, the other of X1 and X2 is a non-nucleotide bridging moiety. Each of X1 and X2 independently is a bridging moiety having first and second termini that each binds independently with a nucleotide phosphate moiety or a nucleotide hydroxyl moiety. Such oligonucleotides are designed to have increased resistance to exonucleases and endonucleases, greater thermal stabilities, improved cellular uptake, and improved binding to target proteins and nucleic acids.

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