Comparing in vitro and in vivo activity of 2′-O-[2-(methylamino)-2-oxoethyl]-and 2′-O-methoxyethyl-modified antisense oligonucleotides

TP Prakash, AM Kawasaki, EV Wancewicz…

Index: Prakash, Thazha P.; Kawasaki, Andrew M.; Wancewicz, Edward V.; Shen, Lijiang; Monia, Brett P.; Ross, Bruce S.; Bhat, Balkrishen; Manoharan, Muthiah Journal of Medicinal Chemistry, 2008 , vol. 51, # 9 p. 2766 - 2776

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Citation Number: 34

Abstract

A number of 2′-O-modified antisense oligonucleotides have been reported for their potential use in oligonucleotide-based therapeutics. To date, most of the in vivo data has been generated for 2′-O-MOE (2′-O-methoxyethyl)-and 2′-O-Me (2′-O-methyl)- modified ASOs (antisense oligonucleotides). We now report the synthesis and biological activity of another 2′-O-modification, namely 2′-O-[2-(methylamino)-2-oxoethyl](2′-O- ...