Oligonucleotides comprised of alternating 2'-deoxy-2'-fluoro-beta-D-arabinonucleosides and D-2'-deoxyribonucleosides (2'F-ANA/DNA 'altimers') induce efficient RNA cleavage mediated by RNase H

Bioorg Med Chem Lett. 2002 Sep 16;12(18):2651-4. doi: 10.1016/s0960-894x(02)00439-0.

Abstract

Chimeric oligonucleotides comprised of alternating residues of 2'-deoxy-2'-fluoro-D-arabinonucleic acid (2'F-ANA) and DNA were synthesized and evaluated for an important antisense property-the ability to elicit ribonuclease H (RNase H) degradation of complementary RNA. Experiments used both human RNase HII and Escherichia coli RNase HI. Mixed backbone oligomers comprising alternating three-nucleotide segments of 2'F-ANA and three-nucleotide segments of DNA were the most efficient at eliciting RNase H degradation of target RNA, and were significantly better than oligonucleotides entirely composed of DNA, suggesting that these mixed backbone oligonucleotides may be potent antisense agents.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Arabinonucleosides / chemistry*
  • Hydrolysis
  • Oligonucleotides, Antisense / chemistry
  • Oligonucleotides, Antisense / pharmacology*
  • RNA / metabolism*
  • Ribonuclease H / metabolism*

Substances

  • Arabinonucleosides
  • Oligonucleotides, Antisense
  • RNA
  • Ribonuclease H