Solid phase synthesis of peptide–siRNA conjugates containing disulfde bond unit  

作　　者：Xiao-Feng Wang Xian-Tao Yang Yue Chen Yang Liu Lang Zou Zhen-Jun Yang Li-He Zhang 

机构地区：[1]State Key Laboratory of Natural and Biomimetic Drugs,School of Pharmaceutical Sciences,Peking University

出　　处：《Chinese Chemical Letters》2013年第10期873-876,共4页中国化学快报（英文版）

基　　金：supported by the National Natural Science Foundation of China(No.20932001);the Ministry of Science and Technology of China(Nos.2012CB720604,2012AA022501)

摘　　要：A disulfide-modified nucleoside was designed and synthesized. After loading the modified nucleoside on controlled pore glass （CPG）, solid phase synthesis strategy was used to prepare peptide-oligonucleotide conjugates （N-3＇） containing disulfide bond unit. The 3＇-sense strand peptide-siRNA conjugate （VII） maintained good gene silencing activity, while that of the 3＇-antisense strand conjugate decreased somewhat. And the sense strand off-target effect of VII decreased remarkably.A disulfide-modified nucleoside was designed and synthesized. After loading the modified nucleoside on controlled pore glass （CPG）, solid phase synthesis strategy was used to prepare peptide-oligonucleotide conjugates （N-3＇） containing disulfide bond unit. The 3＇-sense strand peptide-siRNA conjugate （VII） maintained good gene silencing activity, while that of the 3＇-antisense strand conjugate decreased somewhat. And the sense strand off-target effect of VII decreased remarkably.

关 键 词：siRNA Solid synthesis Disulfide bond Peptide Conjugate 

分 类 号：O629[理学—有机化学]