Peptide-oligonucleotide phosphorothioate conjugates with membrane translocation and nuclear localization properties

被引:74
作者
Antopolsky, M
Azhayeva, E
Tengvall, U
Auriola, S
Jääskeläinen, I
Rönkkö, S
Honkakoski, P
Urtti, A
Lönnberg, H
Azhayev, A [1 ]
机构
[1] Univ Kuopio, Dept Pharmaceut Chem, FIN-70211 Kuopio, Finland
[2] Univ Kuopio, Dept Pharmaceut, FIN-70211 Kuopio, Finland
[3] Univ Turku, Dept Chem, FIN-20014 Turku, Finland
关键词
D O I
10.1021/bc980133y
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
Eighteen peptide - oligonucleotide phosphorothioate conjugates were prepared in good yield and thoroughly characterized with electrospray ionization mass spectra. When applied to the living cells, conjugates exhibiting membrane translocation and nuclear localization properties displayed efficient intracellular penetration but failed to show any serious antisense effect. Studies on the intracellular distribution of the fluorescein-labeled conjugates revealed their trapping in endosomes.
引用
收藏
页码:598 / 606
页数:9
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