CHOLIC-ACID OLIGONUCLEOTIDE CONJUGATES FOR ANTISENSE APPLICATIONS

被引:27
|
作者
MANOHARAN, M
JOHNSON, LK
BENNETT, CF
VICKERS, TA
ECKER, DJ
COWSERT, LM
FREIER, SM
COOK, PD
机构
[1] Isis Pharmaceuticals, Carlsbad, CA 92008
关键词
D O I
10.1016/S0960-894X(01)80680-6
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
To improve the pharmacokinetics of antisense oligonucleotides, cholic acid was conjugated to several biologically active sequences. Physical and biological properties of the conjugates were examined. While the cholic acid conjugation changes the lipophilicity of the oligonucleotides, the in vitro biological activity observed was dependent on the disease target, cell lines and the method of oligonucleotide treatment.
引用
收藏
页码:1053 / 1060
页数:8
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