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




Antopolsky M, Azhayeva E, Tengvall U, Auriola S, Jaaskelainen I, Ronkko S, Honkakoski P, Urtti A, Lonnberg H, Azhayev A

PublisherAMER CHEMICAL SOC

1999

Bioconjugate Chemistry

BIOCONJUGATE CHEMISTRY

BIOCONJUGATE CHEM

10

4

598

606

9

1043-1802

DOIhttps://doi.org/10.1021/bc980133y



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.



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