Synthesis of 3′-S-phosphorothiolate oligonucleotides for their potential use in RNA interference
Synthesis of 3′-S-phosphorothiolate oligonucleotides for their potential use in RNA interference
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DOI：
10.1080/15257770701490753
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发表时间：
2007-01-01
影响因子：
1.3
通讯作者：
Cosstick, Rick
中科院分区：
文献类型：
--
作者：
Gaynor, James W.;Brazier, John;Cosstick, Rick
毫无疑问，通过对小干扰RNA (siRNA)进行化学修饰可以提高RNA干扰(RNAi)的效力。通过将 3'-S-硫代磷酸酯修饰掺入 RNA 链中，希望能够稳定 siRNA 双链体的特定区域，以增强所选反义链与激活的 RNA 诱导沉默复合物 (RISC*) 的靶标结合亲和力。完全由这种修饰组成的寡核苷酸是理想的，因此研究了非常规的 5 -> 3' 合成，并证明初始溶液相测试是成功的。固相合成所需的亚磷酰胺单体也已生产出来。
The potency of RNA interference (RNAi) undoubtedly can be improved through chemical modifications to the small interfering RNAs (siRNA). By incorporation of the 3'-S-phosphorothiolate modification into strands of RNA, it is hoped that specific regions of a siRNA duplex can be stabilised to enhance the target binding affinity of a selected antisense strand into the activated RNA-induced silencing complex (RISC*). Oligonucleotides composed entirely of this modification are desirable so unconventional 5 -> 3' synthesis is investigated, with initial solution-phase testing proving successful. The phosphoroamidite monomer required for solid-phase synthesis has also been produced.