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Peptide-oligonucleotide phosphorothioate conjugates with membrane translocation and nuclear localization properties
M Antopolsky1, E Azhayeva, U Tengvall
1Department of Pharmaceutical Chemistry, University of Kuopio, FIN-70211 Kuopio, Finland.
Bioconjugate Chemistry
|July 20, 1999
Abstract:
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.