A concise method for the preparation of peptide and arginine-rich peptide-conjugated antisense oligonucleotide

被引:27
作者
Chen, CP
Zhang, LR
Peng, YF
Wang, XB
Wang, SQ
Zhang, LH [1 ]
机构
[1] Peking Univ, Sch Pharmaceut Sci, Beijing 100083, Peoples R China
[2] Peking Univ, Sch Chem & Mol Engn, Beijing 100871, Peoples R China
[3] Beijing Inst Radiat Med, Beijing 100850, Peoples R China
关键词
D O I
10.1021/bc034004f
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Peptide-oligonucleotide conjugates were synthesized using two strategies: a mimetic signal peptide-conjugated oligonucleotide was assembled stepwise on CPG by using 2,2-dimethyl-3-hydroxypropionic acid as a linker. To solve the precipitation problem in the coupling reaction caused by the electrostatic interaction of arginine-rich peptides and oligonucleotide, oligonucleotides were absorbed on an anion-exchange resin, and then the on-resin fragment was applied for the conjugation with arginine-rich peptide. The peptide-antisense oligonucleotides showed permeability to the cell membrane of HepG-2 cells.
引用
收藏
页码:532 / 538
页数:7
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