The incorporation of the modified nucleoside into the 3´-overhang regions of short interfering
RNAs (siRNAs) has been reported to enhance their nuclease resistance and improve RNA interference
activity. In this study, DNA 2-mers containing C5-polyamine-modified pyrimidine nucleosides
were synthesized and then ligated to the 3´-end of the RNA by T4 RNA ligase. The modification of the
base moiety with tris(2-aminoethyl)amine affected the ligation efficiency, but the DNA 2-mer containing
only one modified nucleoside was ligated with sufficient efficiency. We propose a novel synthetic
route to modified siRNA bearing various modified groups in the 3´-overhang region.
Keywords: C5-modified pyrimidine, siRNA, T4 RNA Ligase, tris(2-aminoethyl)amine, oligonucleotides, genes.
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