将2'-O-苄基无碱基核苷引入小干扰RNA的3'突出端区域可大大提高核酸酶抗性。
Introduction of 2-O-benzyl abasic nucleosides to the 3'-overhang regions of siRNAs greatly improves nuclease resistance.
作者信息
Nagaya Yuki, Kitamura Yoshiaki, Shibata Aya, Ikeda Masato, Akao Yukihiro, Kitade Yukio
机构信息
United Graduate School of Drug Discovery and Medical Information Sciences, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan.
Department of Chemistry and Biomolecular Science, Faculty of Engineering, Gifu University, 1-1 Yanagido, Gifu 501-1193, Japan.
出版信息
Bioorg Med Chem Lett. 2017 Dec 15;27(24):5454-5456. doi: 10.1016/j.bmcl.2017.10.070. Epub 2017 Oct 28.
Chemically modified siRNAs containing 2-O-benzyl-1-deoxy-d-ribofuranose (R) in their 3'-overhang region were significantly more resistant towards serum nucleases than siRNAs possessing the natural nucleoside in this region. The knockdown efficacies and binding affinities of these modified siRNAs to the recombinant human Argonaute protein 2 (hAgo2) PAZ domain were comparable with that of siRNA with a thymidine dimer at the 3'-end.
在其3'突出端区域含有2-O-苄基-1-脱氧-D-核糖呋喃糖（R）的化学修饰的小干扰RNA（siRNA）比在该区域具有天然核苷的siRNA对血清核酸酶的抗性明显更强。这些修饰的siRNA对重组人AGO2蛋白PAZ结构域的敲低效率和结合亲和力与3'端具有胸腺嘧啶二聚体的siRNA相当。
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