Biological activity and biotechnological aspects of locked nucleic acids.

Karin E Lundin, Torben Højland, Bo R Hansen, Robert Persson, Jesper B Bramsen, Jørgen Kjems, Troels Koch, Jesper Wengel, C I Edvard Smith

Clinical Research Center, Department of Laboratory Medicine, Karolinska Institutet, Novum, Huddinge, Stockholm, Sweden. karin.lundin@ki.se

Advances in genetics 2013

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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. Copyright © 2013 Elsevier Inc. All rights reserved.

Citation

Karin E Lundin, Torben Højland, Bo R Hansen, Robert Persson, Jesper B Bramsen, Jørgen Kjems, Troels Koch, Jesper Wengel, C I Edvard Smith. Biological activity and biotechnological aspects of locked nucleic acids. Advances in genetics. 2013;82:47-107