Biological activity and biotechnological aspects of locked nucleic acids

Adv Genet. 2013;82:47-107. doi: 10.1016/B978-0-12-407676-1.00002-0.


Locked nucleic acid (LNA) is one of the most promising new nucleic acid analogues that has been produced under the past two decades. In this chapter, we have tried to cover many of the different areas, where this molecule has been used to improve the function of synthetic oligonucleotides (ONs). The use of LNA in antisense ONs, including gapmers, splice-switching ONs, and siLNA, as well as antigene ONs, is reviewed. Pharmacokinetics as well as pharmacodynamics of LNA ONs and a description of selected compounds in, or close to, clinical testing are described. In addition, new LNA modifications and the adaptation of enzymes for LNA incorporation are reviewed. Such enzymes may become important for the development of stabilized LNA-containing aptamers.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Animals
  • Aptamers, Nucleotide / chemistry
  • Aptamers, Nucleotide / genetics
  • DNA, Antisense / chemistry
  • DNA, Antisense / genetics
  • Humans
  • MicroRNAs / antagonists & inhibitors
  • MicroRNAs / genetics
  • Oligonucleotides / chemistry
  • Oligonucleotides / genetics*
  • Oligonucleotides / pharmacology*
  • RNA Splicing
  • RNA, Small Interfering / metabolism


  • Aptamers, Nucleotide
  • DNA, Antisense
  • MicroRNAs
  • Oligonucleotides
  • RNA, Small Interfering
  • locked nucleic acid