Nuclease stability as dominant factor in the antiviral activity of oligonucleotides directed against HSV-1 IE110

Antiviral Res. 1997 Jan;33(2):135-9. doi: 10.1016/s0166-3542(96)01003-0.

Abstract

The anti-herpes simplex virus type 1 (anti-HSV-1) efficacy of a series of oligonucleotides was determined as a function of their chemical structure. All oligonucleotides consisted of the same sequence directed against the translation initiation codon of the HSV-1 immediate early gene. The oligonucleotides were modified with phosphorothioate linkage patterns according to various protection strategies against nucleolytic degradation. We show that nuclease resistance is the dominant factor that determines the antiviral efficacy in this series. A minimal protection strategy, consisting of end-capping and pyrimidine protection, has proven to be particularly useful, because it not only yields nuclease-resistant oligonucleotides but also minimizes non-sequence-specific effects.

MeSH terms

  • Animals
  • Antiviral Agents / pharmacology*
  • Chlorocebus aethiops
  • Deoxyribonucleases / metabolism*
  • Herpesvirus 1, Human / drug effects*
  • Humans
  • Oligodeoxyribonucleotides / chemistry
  • Oligodeoxyribonucleotides / pharmacology*
  • Structure-Activity Relationship
  • Vero Cells

Substances

  • Antiviral Agents
  • Oligodeoxyribonucleotides
  • Deoxyribonucleases