Stability, specific binding activity, and plasma concentration in mice of an oligodeoxynucleotide modified at 5'-terminal with poly(ethylene glycol)

Biol Pharm Bull. 1995 Mar;18(3):474-6. doi: 10.1248/bpb.18.474.

Abstract

Oligodeoxynucleotide (ODN) composed of 15 nucleotides was modified at 5'-terminal phosphate with hexylamine linker and chemically activated poly(ethylene glycol). This derivative showed improved characteristics in terms of enzymatic stability, binding activity, and in vivo retention in mouse. The data are discussed in comparison with those of corresponding unmodified and phosphorothioate ODNs.

MeSH terms

  • Animals
  • Base Sequence
  • Drug Stability
  • Humans
  • Injections, Intravenous
  • Male
  • Mice
  • Mice, Inbred Strains
  • Molecular Sequence Data
  • Oligonucleotides / blood*
  • Oligonucleotides / metabolism
  • Oligonucleotides, Antisense / metabolism
  • Polyethylene Glycols / pharmacology*
  • Sensitivity and Specificity
  • Single-Strand Specific DNA and RNA Endonucleases / metabolism

Substances

  • Oligonucleotides
  • Oligonucleotides, Antisense
  • Polyethylene Glycols
  • Single-Strand Specific DNA and RNA Endonucleases