Resistance of morpholino phosphorodiamidate oligomers to enzymatic degradation

Antisense Nucleic Acid Drug Dev. Winter 1996;6(4):267-72. doi: 10.1089/oli.1.1996.6.267.

Abstract

Oligomers possessing the Morpholino phosphorodiamidate backbone were evaluated for resistance to a variety of enzymes and biologic fluids. A 25-mer was incubated with nucleases, proteases, esterases, and serum, and the reaction mixtures were directly analyzed by MALDI-TOF mass spectrometry. The 25-mer was completely resistant to 13 different hydrolases and serum and plasma. The excellent resistance of Morpholino phosphorodiamidates to enzymatic attack indicates their suitability for in vivo use.

Publication types

  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Blood Physiological Phenomena*
  • Deoxyribonucleases / chemistry
  • Drug Stability
  • Endopeptidases / chemistry
  • Esterases / chemistry
  • Hydrolases / chemistry*
  • Mass Spectrometry
  • Molecular Structure
  • Morpholines / chemistry*
  • Organophosphates / chemistry*
  • Plasma / physiology*
  • Ribonucleases / chemistry

Substances

  • Morpholines
  • Organophosphates
  • Hydrolases
  • Deoxyribonucleases
  • Esterases
  • Ribonucleases
  • Endopeptidases