Amido-bridged nucleic acids with small hydrophobic residues enhance hepatic tropism of antisense oligonucleotides 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. N2'-functionalization of AmNA with a variety of hydrophobic groups is straightforward. Combinations...

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Veröffentlicht in:	Organic & biomolecular chemistry 2015-03, Vol.13 (12), p.3757-3765
Hauptverfasser:	Yamamoto, Tsuyoshi, Yahara, Aiko, Waki, Reiko, Yasuhara, Hidenori, Wada, Fumito, Harada-Shiba, Mariko, Obika, Satoshi
Format:	Artikel
Sprache:	eng
Schlagworte:	Amines - chemistry Animals Apolipoprotein C-III - genetics Apolipoprotein C-III - metabolism Drug Delivery Systems Enzyme-Linked Immunosorbent Assay Hydrophobic and Hydrophilic Interactions Liver - metabolism Mice Oligonucleotides, Antisense - administration & dosage Oligonucleotides, Antisense - chemistry Oligonucleotides, Antisense - pharmacokinetics Organophosphorus Compounds - chemical synthesis Organophosphorus Compounds - chemistry RNA, Messenger - genetics RNA, Messenger - metabolism
Online-Zugang:	Volltext
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