2‘-O-{2-[N,N-(Dialkyl)aminooxy]ethyl}- Modified Antisense Oligonucleotides

Oligonucleotides with two novel modifications, 2‘-O-{2-[N,N-(dimethyl)aminooxy]ethyl} (2‘-O-DMAOE) and 2‘-O-{2-[N,N-(diethyl)aminooxy]ethyl} (2‘-O-DEAOE), have been synthesized. These modifications exhibit high binding affinity to target RNA (and not to DNA) and enhance the nuclease stability of oli...

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Bibliographic Details
Published inOrganic letters Vol. 2; no. 25; pp. 3995 - 3998
Main Authors Prakash, Thazha P, Manoharan, Muthiah, Kawasaki, Andrew M, Lesnik, Elena A, Owens, Stephen R, Vasquez, Guillermo
Format Journal Article
LanguageEnglish
Published WASHINGTON American Chemical Society 14.12.2000
Amer Chemical Soc
Subjects
Chemistry
Chemistry, Organic
Physical Sciences
Science & Technology
HYBRIDIZATION
DEPROTECTION
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Summary:Oligonucleotides with two novel modifications, 2‘-O-{2-[N,N-(dimethyl)aminooxy]ethyl} (2‘-O-DMAOE) and 2‘-O-{2-[N,N-(diethyl)aminooxy]ethyl} (2‘-O-DEAOE), have been synthesized. These modifications exhibit high binding affinity to target RNA (and not to DNA) and enhance the nuclease stability of oligonucleotides considerably with t 1/2 > 24 h as a phosphodiester.
ISSN:1523-7060
1523-7052
DOI:10.1021/ol006555g