Synthesis and properties of triplex-forming oligonucleotides containing 2'-O-(2-methoxyethyl)-5-(3-aminoprop-1-ynyl)-uridine

Chenguang Lou, Qiang Xiao, Lavinia Brennan, Mark E Light, Nuria Vergara-Irigaray, Elizabeth M Atkinson, Lindy M Holden-Dye, Keith R Fox, Tom Brown

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Abstrakt

2'-O-(2-Methoxyethyl)-5-(3-aminoprop-1-ynyl)-uridine phosphoramidite (MEPU) has been synthesized from d-ribose and 5-iodouracil and incorporated into triplex-forming oligonucleotides (TFOs) by automated solid-phase oligonucleotide synthesis. The TFOs gave very high triplex stability with their target duplexes as measured by ultraviolet/fluorescence melting and DNase I footprinting. The incorporation of MEPU into TFOs renders them resistant to degradation by serum nucleases.
OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry Letters
Vol/bind18
Udgave nummer17
Sider (fra-til)6389-6397
ISSN0960-894X
DOI
StatusUdgivet - 2010

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