Biological activity and biotechnological aspects of locked nucleic acids

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  • Karin E Lundin, Clinical Research Center, Department of Laboratory Medicine, Karolinska Institutet, Sverige
  • Torben Højland, NanoCAN, Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Danmark
  • Bo Hansen, Santaris Pharma A/S, Danmark
  • Robert Persson, Santaris Pharma A/S, Danmark
  • Jesper B Bramsen
  • Jørgen Kjems
  • Troels Koch, Santaris Pharma A/S, Danmark
  • Jesper Wengel, NanoCAN, Department of Physics, Chemistry and Pharmacy, University of Southern Denmark, Danmark
  • C I Edvard Smith, Clinical Research Center, Department of Laboratory Medicine, Karolinska Institutet, Sverige
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.
OriginalsprogEngelsk
BogserieAdvances in Genetics
Vol/bind82
Sider (fra-til)47-107
Antal sider61
ISSN0065-2660
DOI
StatusUdgivet - 2013

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