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

Synthesis of modified siRNA bearing C-5 polyamine-substituted pyrimidine nucleoside in their 3'-overhang regions and its RNAi activity
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3-突出端带有 C-5 多胺取代嘧啶核苷的修饰 siRNA 的合成及其 RNAi 活性

DOI:
10.1016/j.bmcl.2010.11.125
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发表时间:
2011
期刊:
Bioorg. Med. Chem. Lett
影响因子:
--
通讯作者:
and and Ozaki H.
and and Ozaki H.
中科院分区:
--
文献类型:
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作者:
Masud MM;Masuda T;Inoue Y;Kuwahara M;Sawai H;and and Ozaki H.

文献摘要

相似文献

短干扰RNA(siRNA)通过RNA干扰(RNAi)途径诱导特异性基因沉默。siRNA的3′-突出端区域中的核苷被5-双(氨乙基)氨乙基氨甲酰基甲基-2 ′-脱氧尿苷或胸苷取代。与含胸苷的siRNA相比,含修饰核苷的siRNA对肝细胞核因子4α(HNF 4 α)基因表达的抑制作用更强。
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.