Comparative inhibition of ras p21 protein synthesis with phosphorus-modified antisense oligonucleotides

Anticancer Drug Des. 1989 Oct;4(3):221-32.

Abstract

A rabbit reticulocyte lysate translation assay was used to quantitatively compare a series of antisense oligodeoxyribonucleotides (11-mers) having different internucleoside linkages and various degrees of complementarity (100-80%) with the start codon and downstream 8 bases of Balb-ras p21 mRNA. The oligomers had either contiguous phosphodiester, or alternating methylphosphonate-phosphodiester, or contiguous methylphosphonate, or contiguous phosphorothioate linkages. Under the conditions used for the assay, all of the test compounds when present in about 10(3)-10(4) excess over mRNA (15 nM mRNA) inhibited protein synthesis to a degree which was dependent on both the concentration and sequence of the oligomer. At low concentrations (12.5-25 microM), the phosphorothioate analogs were the most potent inhibitors of p21 protein synthesis; however, a sequence non-specific effect for these oligomers was dominant at higher concentrations of oligomer (100-200 microM). The methylphosphonate oligomers appeared to be slightly more discriminant. Relative hybridization strengths were assessed by melting (Tm) studies using a DNA oligomer target to mimic the mRNA.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Gene Expression Regulation / drug effects
  • In Vitro Techniques
  • Mice
  • Mice, Inbred BALB C / genetics
  • Nucleic Acid Hybridization
  • Oligonucleotides / chemical synthesis
  • Oligonucleotides / pharmacology*
  • Oligonucleotides, Antisense
  • Oncogene Protein p21(ras) / genetics*
  • Organophosphonates
  • Plasmids
  • Protein Biosynthesis / drug effects
  • Structure-Activity Relationship
  • Temperature
  • Transcription, Genetic / drug effects

Substances

  • Oligonucleotides
  • Oligonucleotides, Antisense
  • Organophosphonates
  • Oncogene Protein p21(ras)