Selective alkylation and bioactivity of phosphorothioated nucleolin aptamer AS1411

作     者：张光普 邓家荔 杨先桃 朱月洁 关注 张礼和 杨振军 Guangpu Zhang;Jiali Deng;Xiantao Yang;Yuejie Zhu;Zhu Guan;Lihe Zhang;Zhenjun Yang

作者机构：北京大学医学部药学院天然药物及仿生药物国家重点实验室北京100191 

出 版 物：《Journal of Chinese Pharmaceutical Sciences》 (中国药学（英文版）)

年 卷 期：2017年第26卷第1期

页      面：23-30页

核心收录：

学科分类：1007[医学-药学(可授医学、理学学位)] 100701[医学-药物化学] 10[医学] 

基　　金：the Ministry of Science and Technology of China(Grant No.2012CB720604) National Natural Science Foundation of China(Grant No.21332010) 

主　　题：Phosphorothioated nucleotide Alkylation Aptamer AS 1411 Nucleolin 

摘      要：An operationally simple and efficient method for the synthesis of a wide range of alkylated nucleotides under mild conditions was developed. This improved method furnishes alkylated nucleotides fi＇om both single nucleotides and oligonucleotides, and were prepared in high yields of 81% to 91%. Alkyl modified aptamer AS1411s were synthesized using this method and the biological activity screening results demonstrated that alkylation at the 1^st P-S site on yielded stronger target protein binding capacity, greater growth suppression effects against K562 and HL-60 cell lines, and improved serum stability, as compared with AS1411. This modified aptamer may be useful in tumor detection and treatment.