Morpholino antisense oligomers: design, preparation, and properties

Antisense Nucleic Acid Drug Dev. 1997 Jun;7(3):187-95. doi: 10.1089/oli.1.1997.7.187.


Antisense promised major advances in treating a broad range of intractable diseases, but in recent years progress has been stymied by technical problems, most notably inadequate specificity, ineffective delivery into the proper subcellular compartment, and unpredictable activity within cells. Herein is an overview of the design, preparation, and properties of Morpholino oligos, a novel antisense structural type that solves the sequence specificity problem and provides high and predictable activity in cells. Morpholino oligos also exhibit little or no nonantisense activity, afford good water solubility, are immune to nucleases, and are designed to have low production costs.

Publication types

  • Review

MeSH terms

  • Animals
  • Cell-Free System
  • Cells, Cultured
  • Endocytosis
  • Mice
  • Molecular Structure
  • Morpholines* / chemical synthesis
  • Morpholines* / isolation & purification
  • Morpholines* / pharmacology
  • Nucleic Acid Denaturation
  • Oligonucleotides, Antisense* / chemistry
  • Oligonucleotides, Antisense* / isolation & purification
  • Oligonucleotides, Antisense* / pharmacology
  • Rats
  • Solubility
  • Structure-Activity Relationship
  • Water


  • Morpholines
  • Oligonucleotides, Antisense
  • Water