Amido-bridged nucleic acids with small hydrophobic residues enhance hepatic tropism of antisense oligonucleotides in vivoElectronic supplementary information (ESI) available. See DOI: 10.1039/c5ob00242g

High scalability of a novel bicyclic nucleoside building block, amido-bridged nucleic acid (AmNA), to diversify pharmacokinetic properties of therapeutic antisense oligonucleotides is described. N 2′-functionalization of AmNA with a variety of hydrophobic groups is straightforward. Combinations of t...

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Bibliographic Details
Main Authors: Yamamoto, Tsuyoshi, Yahara, Aiko, Waki, Reiko, Yasuhara, Hidenori, Wada, Fumito, Harada-Shiba, Mariko, Obika, Satoshi
Format: Article
Language:English
Online Access:Get full text
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Summary:High scalability of a novel bicyclic nucleoside building block, amido-bridged nucleic acid (AmNA), to diversify pharmacokinetic properties of therapeutic antisense oligonucleotides is described. N 2′-functionalization of AmNA with a variety of hydrophobic groups is straightforward. Combinations of these modules display similar antisense knockdown effects and improve cellular uptake, relative to sequence-matched conventional 2′,4′-bridged nucleic acid (2′,4′-BNA) in vivo . High scalability of a novel bicyclic nucleoside building block, amido-bridged nucleic acid (AmNA), to diversify pharmacokinetic properties of therapeutic antisense oligonucleotides is described.
ISSN:1477-0520
1477-0539
DOI:10.1039/c5ob00242g