Hoshika Shuichi, Minakawa Noriaki, Kamiya Hiroyuki, Harashima Hideyoshi, Matsuda Akira
Graduate School of Pharmaceutical Sciences, Hokkaido University, Kita-12, Nishi-6, Kita-Ku, Sapporo 060-0812, Japan.
FEBS Lett. 2005 Jun 6;579(14):3115-8. doi: 10.1016/j.febslet.2005.04.073.
Short interfering RNAs (siRNAs) variously modified with 4'-thioribonucleosides against the Photinus luciferase gene were tested for their induction of the RNA interference (RNAi) activity in cultured NIH/3T3 cells. Results indicated that modifications at the sense-strand were well tolerated for RNAi activity except for full modification with 4'-thioribonucleosides. However, the activity of siRNAs modified at the antisense-strand was dependent on the position and the number of modifications with 4'-thioribonucleosides. Since modifications of siRNAs with 4'-thioribonucleosides were well tolerated in RNAi activity compared with that of 2'-O-methyl nucleosides, 4'-thioribonucleosides might be potentially useful in the development of novel and effective chemically modified siRNAs.
针对萤火虫荧光素酶基因，测试了用4'-硫代核糖核苷进行各种修饰的短干扰RNA（siRNA）在培养的NIH/3T3细胞中诱导RNA干扰（RNAi）活性的情况。结果表明，除了用4'-硫代核糖核苷进行完全修饰外，正义链上的修饰对RNAi活性具有良好的耐受性。然而，反义链上修饰的siRNA的活性取决于4'-硫代核糖核苷修饰的位置和数量。由于与2'-O-甲基核苷相比，用4'-硫代核糖核苷修饰的siRNA在RNAi活性方面具有良好的耐受性，因此4'-硫代核糖核苷可能在新型有效化学修饰siRNA的开发中具有潜在用途。
