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Introduction of 2-O-benzyl abasic nucleosides to the 3′-overhang regions of siRNAs greatly improves nuclease resistance
Bioorganic & Medicinal Chemistry Letters ( IF 2.7 ) Pub Date : 2017-10-28 , DOI: 10.1016/j.bmcl.2017.10.070
Yuki Nagaya , Yoshiaki Kitamura , Aya Shibata , Masato Ikeda , Yukihiro Akao , Yukio Kitade

Chemically modified siRNAs containing 2-O-benzyl-1-deoxy-d-ribofuranose (RHOBn) 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.



中文翻译:

将2- O-苄基无碱基核苷引入siRNA的3'-突出端区域可大大提高核酸酶的抗性

化学修饰的siRNA含有2- ø -苄基-1-脱氧d -ribofuranose(R ħ OBN)在它们的3'突出端区域分别朝向血清核酸酶具有比该区域中的天然核苷的siRNA显著更有抵抗力。这些修饰的siRNA与重组人Argonaute蛋白2(hAgo2)PAZ结构域的敲除效率和结合亲和力与在3'端带有胸苷二聚体的siRNA相当。

更新日期:2017-10-28
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