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Short antisense oligonucleotides with novel 2'-4' conformationaly restricted nucleoside analogues show improved potency without increased toxicity in animals.

Abstract：

:The potency of second generation antisense oligonucleotides (ASOs) in animals was increased 3- to 5 -fold (ED(50) approximately 2-5 mg/kg) without producing hepatotoxicity, by reducing ASO length (20-mer to 14-mer) and by employing novel nucleoside modifications that combine structural elements of 2'-O-methoxyethyl residues and locked nucleic acid. The ability to achieve this level of potency without any formulation agents is remarkable and likely to have a significant impact on the future design of ASOs as therapeutic agents.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Seth PP,Siwkowski A,Allerson CR,Vasquez G,Lee S,Prakash TP,Wancewicz EV,Witchell D,Swayze EE

doi

10.1021/jm801294h

subject

Has Abstract

pub_date

2009-01-08 00:00:00

pages

10-3

issue

1

eissn

0022-2623

issn

1520-4804

pii

10.1021/jm801294h

journal_volume

52

pub_type

杂志文章

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