Practical and Reliable Synthesis of 1,2-Dideoxy-d-ribofuranose and its Application in RNAi Studies

Y. Nagaya, Y. Kitamura, Remi Nakashima, Aya Shibata, M. Ikeda, Y. Kitade
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引用次数: 7

Abstract

ABSTRACT We developed a practical and reliable method for synthesizing an abasic deoxyribonucleoside, 1,2-dideoxy-d-ribofuranose (dRH) via elimination of nucleobase from thymidine. To synthesize oligonucleotides bearing dRH by the standard phosphoramidite solid-phase method, dRH was converted to the corresponding phosphoramidite derivative and linked to a solid support (controlled pore glass resin). Chemically modified small interfering RNAs (siRNAs) possessing dRH at their 3′-overhang regions were synthesized. Introducing dRH to the 3′-end of the antisense strand of siRNA reduced its knockdown effect.
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实用可靠的1,2-二脱氧核糖呋喃糖的合成及其在RNAi研究中的应用
摘要:本文建立了一种实用可靠的方法,通过消除胸腺嘧啶的核碱基,合成了一种碱性脱氧核糖核苷- 1,2-二脱氧-d-核糖呋喃糖(dRH)。为了通过标准的酰胺磷固相法合成含dRH的寡核苷酸,将dRH转化为相应的酰胺磷衍生物,并连接到固体载体(受控孔玻璃树脂)上。化学修饰的小干扰rna (sirna)在其3 ' -悬垂区具有dRH。将dRH引入到siRNA反义链的3 '端可以降低其敲低作用。
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