Synthesis and biological properties of DNA-sugar conjugates

Nucleic Acids Res Suppl. 2001:(1):73-4. doi: 10.1093/nass/1.1.73.

Abstract

In order to improve the pharmacological properties of antisense and antigene oligonucleotides, oligodeoxynucleotides conjugated with amino sugars at the 5'-terminus were synthesized by solid phase fragment condensation (SPFC) method. The obtained DNA-sugar conjugates were evaluated in their chemical and biological activities to show that 5'-end modification of oligonucleotides with sugars enhanced the thermal stability of the hybrid duplex with complementary DNA, the resistance against nuclease digestion and the membrane permeability of the conjugates.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Sugars / chemistry*
  • Cell Membrane Permeability
  • DNA / chemistry
  • Endonucleases / metabolism
  • Nucleic Acid Hybridization
  • Oligodeoxyribonucleotides, Antisense / chemical synthesis*
  • Oligodeoxyribonucleotides, Antisense / chemistry*
  • Oligodeoxyribonucleotides, Antisense / metabolism

Substances

  • Amino Sugars
  • Oligodeoxyribonucleotides, Antisense
  • DNA
  • Endonucleases