Nucleosides, Nucleotides & Nucleic Acids ( IF 1.1 ) Pub Date : 2016-01-29 , DOI: 10.1080/15257770.2015.1114128 Yuki Nagaya 1 , Yoshiaki Kitamura 2, 3 , Remi Nakashima 2 , Aya Shibata 2, 3 , Masato Ikeda 1, 2, 3 , Yukio Kitade 1, 2, 3
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.
中文翻译:
1,2-二脱氧-d-呋喃核糖的实用可靠合成方法及其在RNAi研究中的应用。
我们开发了用于合成无碱基脱氧核糖核苷,1,2-二脱氧一个实际和可靠的方法d -ribofuranose(DR ħ通过消除从胸苷碱基的)。为了通过标准亚磷酰胺固相法合成带有dR H的寡核苷酸,将dR H转化为相应的亚磷酰胺衍生物,并连接到固相载体(可控孔玻璃树脂)上。合成了在其3'-突出端区域具有dR H的化学修饰的小干扰RNA(siRNA)。将dR H引入siRNA反义链的3'末端可降低其敲低效应。