Short antisense oligonucleotide-mediated inhibition is strongly dependent on oligo length and concentration but almost independent of location of the target sequence

J Biol Chem. 1994 Jun 10;269(23):16187-94.

Abstract

The inhibitory effect of short antisense oligodeoxynucleotides (aODNs) on cRNA expression in Xenopus oocytes was measured using an electrophysiological assay based on subunit-specific block of cloned alpha-amino-3-hydroxy-5-methyl-4-isoxazole-propionate receptors. The effect of both phosphorothioate-modified (PS) and phosphodiester (PO) aODNs was strongly length dependent with a half-maximal inhibition calculated for an oligo length of 7.6 nucleotides (nt) and 9.9 nt, respectively. More than 95% inhibition was mediated by a PS aODN of 12 nt and by PO aODNs > or = 15 nt. At a given length PS and PO aODNs showed differential dependence of their inhibitory effect on the injected aODN concentration (half-maximal inhibition at 18 ng/microliter for a PO 12-mer and at 0.19 ng/microliter for a PS 12-mer) and differential saturation behavior. The inhibitory effect of aODNs, even as short as 8 nt for PS oligomers, was highly sequence specific, but almost independent of the position of the respective target site on the cRNA (for PS 8-mers, > or = 70% expression inhibition throughout the tested target sites from the translation initiation to the 3'-untranslated region). Thus, short PS aODNs can be reliably used in order to specifically inhibit protein expression in experiments addressing physiological, molecular biological, and perhaps even therapeutical issues.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Base Sequence
  • DNA, Antisense / pharmacology*
  • Dose-Response Relationship, Drug
  • Electric Conductivity
  • Indoleacetic Acids
  • Molecular Sequence Data
  • Oligonucleotides, Antisense / pharmacology*
  • Oocytes
  • Phenylacetates / pharmacology
  • Polyamines / pharmacology
  • Protein Biosynthesis / drug effects*
  • RNA, Complementary
  • Receptors, AMPA / classification
  • Receptors, AMPA / genetics*
  • Structure-Activity Relationship
  • Thionucleotides
  • Xenopus / genetics

Substances

  • DNA, Antisense
  • Indoleacetic Acids
  • Oligonucleotides, Antisense
  • Phenylacetates
  • Polyamines
  • RNA, Complementary
  • Receptors, AMPA
  • Thionucleotides
  • argiotoxin-636