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Synthesis of 2'-O-modified adenosine building blocks and application for RNA interference

Publikation: Bidrag til tidsskrift/Konferencebidrag i tidsskrift /Bidrag til avis › Tidsskriftartikel › Forskning › peer review

DOI

  • Dalibor Odadzic, Institute for Organic Chemistry, and Chemical Biology, Tyskland
  • Jesper B Bramsen
  • Romualdas Smicius, Institute for Organic Chemistry, and Chemical Biology, Tyskland
  • Claus Bus
  • Jørgen Kjems
  • Joachim W Engels, Institute for Organic Chemistry, and Chemical Biology, Tyskland
RNA-interference has been recognized as a powerful tool to control gene function and has been used for gene silencing by knocking down mRNA. Chemically modified RNAs, especially 2'-O-modification, successfully improved their physicochemical and pharmaceutical properties such as stability, nuclease resistance and delivery. Here, we report the synthesis of adenosine building blocks with different 2'-tethered modifications like aminoethyl and guanidinoethyl and show that they are compatible with RNAi function. They enhance the half life of the siRNA in serum suggesting that these modifications can enhance the pharmacokinetic properties and knock down activity of siRNAs in vivo.
OriginalsprogEngelsk
TidsskriftBioorganic & Medicinal Chemistry
Vol/bind16
Nummer1
Sider (fra-til)518-529
Antal sider12
ISSN0968-0896
DOI
StatusUdgivet - jan. 2008

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