在 3'突出端修饰含有 C-5 聚胺取代嘧啶核苷的 siRNA 的合成及其 RNAi 活性。
Synthesis of modified siRNA bearing C-5 polyamine-substituted pyrimidine nucleoside in their 3'-overhang regions and its RNAi activity.
机构信息
Department of Chemistry and Chemical Biology, Graduate School of Engineering, Gunma University, Tenjin-cho 1-5-1, Kiryu, Gunma 376-8515, Japan.
出版信息
Bioorg Med Chem Lett. 2011 Jan 15;21(2):715-7. doi: 10.1016/j.bmcl.2010.11.125. Epub 2010 Dec 5.
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.
短干扰 RNA（siRNA）通过 RNA 干扰（RNAi）途径诱导特定基因沉默。siRNA 3'-突出末端区域的核苷被 5-双（氨乙基）氨基乙基羰甲基-2'-脱氧尿苷或胸苷取代。与含有胸苷的 siRNA 相比，含有修饰核苷的 siRNA 更能有效抑制肝细胞核因子 4α（HNF4α）的基因表达。
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