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...

Full description

Saved in:
Bibliographic Details
Main Authors Yamamoto, Tsuyoshi, Yahara, Aiko, Waki, Reiko, Yasuhara, Hidenori, Wada, Fumito, Harada-Shiba, Mariko, Obika, Satoshi
Format Journal Article
LanguageEnglish
Published 11.03.2015
Online AccessGet full text

Cover

More Information
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.
Bibliography:10.1039/c5ob00242g
Electronic supplementary information (ESI) available. See DOI
ISSN:1477-0520
1477-0539
DOI:10.1039/c5ob00242g