Synthesis of modified siRNA bearing C-5 polyamine-substituted pyrimidine nucleoside in their 3'-overhang regions and its RNAi activity.

Bioorg Med Chem Lett

Department of Chemistry and Chemical Biology, Graduate School of Engineering, Gunma University, Tenjin-cho 1-5-1, Kiryu, Gunma 376-8515, Japan.

Published: January 2011

Short interfering RNA (siRNA) induces specific gene silencing by the RNA interference (RNAi) pathway. Nucleosides in the 3'-overhang regions of siRNAs were replaced with 5-bis(aminoethyl)aminoethylcarbamoylmethyl-2'-deoxyuridine or thymidine. siRNA bearing modified nucleoside was more active in silencing the gene expression of hepatocyte nuclear factor 4α (HNF4α) compared with siRNA bearing thymidine.

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http://dx.doi.org/10.1016/j.bmcl.2010.11.125DOI Listing

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