Modification of oligonucleotides by isonucleosides incorporation and peptides conjugation  

异核苷掺入和肽缀合修饰的寡核苷酸(英文)

作　　者：黄野[1] 王晓锋[1] 杨振军[1] 张礼和[1] 

机构地区：[1]北京大学医学部天然药物及仿生药物国家重点实验室,北京100191

出　　处：《Journal of Chinese Pharmaceutical Sciences》2012年第6期499-508,共10页中国药学（英文版）

基　　金：National Natural Science Foundation (Grant No.20932001);the Ministry of Science and Technology (Grant No.2012CB720604)

摘　　要：Synthetic oligonucleotides including antisense oligonucleotides and siRNA have shown promising therapeutic potential.However,to realize the therapeutic potential of synthetic oligonucleotides,many obstacles have to be overcome,such as their poor biological stability,non-specific activity and inadequate cell membrane permeability.In this paper,the achievements by Lihe Zhang＇s group in the study of isonucleotide modified oligonucleotides and oligonucleotides conjugated with cell penetrating peptides are summarized.人工合成的寡核苷酸, 包括反义寡核苷酸、干扰RNA等, 显示了优异的临床潜在应用价值。但要实现合成的寡核苷酸的广泛临床应用, 必须要克服一些障碍性问题, 如该类结构的不稳定性、非特异性作用及难以跨膜吸收等。本文综述了张礼和院士课题组在异核苷掺入及肽缀合寡核苷酸方面的研究成果。

关 键 词：Synthetic oligonucleotide Isonucleoside Cell penetrating peptide SIRNA 

分 类 号：R914[医药卫生—药物化学]