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在其3'突出端区域具有苯磷酸骨架的核酸酶抗性小干扰RNA的合成。

Synthesis of nuclease-resistant siRNAs possessing benzene-phosphate backbones in their 3'-overhang regions.

作者信息

Ueno Yoshihito, Inoue Takumi, Yoshida Mahito, Yoshikawa Kayo, Shibata Aya, Kitamura Yoshiaki, Kitade Yukio

机构信息

Department of Biomolecular Science, Faculty of Engineering, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan.

出版信息

Bioorg Med Chem Lett. 2008 Oct 1;18(19):5194-6. doi: 10.1016/j.bmcl.2008.08.086. Epub 2008 Aug 28.

Abstract

We describe the synthesis and silencing activities of siRNA possessing N(1)-[3,5-bis(hydroxymethyl)phenyl]thymine (b(t)) in their 3'-overhang regions. We found that an siRNA possessing b(t) in the 3'-overhang region was more effective than an siRNA with natural nucleosides and the siRNA possessing 1,3-bis(hydroxymethyl)benzene (b) without a nucleobase at the 3'-overhang region in in vitro experiment using HeLa cells system. Furthermore, the RNA possessing b(t) at its 3'-end was more resistant to nucleolytic hydrolysis by snake venom phosphodiesterase (a 3'-exonuclease) than the RNA possessing the natural nucleoside 2'-deoxythymidine at the 3'-end. Thus, the compound b(t) will be a novel 3'-overhang moiety that can enhance the silencing activity and nuclease-resistant property of siRNAs.

摘要

我们描述了在其3'突出端区域含有N(1)-[3,5-双(羟甲基)苯基]胸腺嘧啶(b(t))的小干扰RNA(siRNA)的合成及沉默活性。我们发现,在使用HeLa细胞系统的体外实验中,3'突出端区域含有b(t)的siRNA比具有天然核苷的siRNA以及3'突出端区域含有无核苷碱基的1,3-双(羟甲基)苯(b)的siRNA更有效。此外,3'端含有b(t)的RNA比3'端含有天然核苷2'-脱氧胸腺嘧啶的RNA对蛇毒磷酸二酯酶(一种3'外切核酸酶)的核酸水解更具抗性。因此,化合物b(t)将是一种新型的3'突出端部分,可增强siRNA的沉默活性和核酸酶抗性。

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