Abstract
Over the past 10-15 years LNA (Locked Nucleic Acid) has taken a central position in nucleic acid chemistry and biology. The enhanced hybridization properties against both DNA and RNA have become a new reference in the field and proven to be enabling for many application in life sciences. For therapeutic use as RNA targeting drugs LNA enable the design of potent antisense oligonucleotides. Much effort has been dedicated to get efficient delivery of RNA targeting drugs, but in contrast to e.g. siRNA duplexes it has been demonstrated that LNA oligonucleotides are taken up by cells without added deliver vehicles in an active state (gymnotic delivery). Here, the fundamental properties of LNA are reviewed together with the recent and most advanced pre-clinical/clinical LNA data.
Keywords: LNA (Locked Nucleic Acid), Antisense, hybridization, Bicyclic, Nucleoside structure, Property space, Gymnosis, Drug discovery, Pharmacokinetics, Pharmacodynamics, Non-human primate, Pre-clinical, ApoB, PCSK9, HCV, Clinical
Current Physical Chemistry
Title:LNA Antisense: A Review
Volume: 3 Issue: 1
Author(s): Troels Koch
Affiliation:
Keywords: LNA (Locked Nucleic Acid), Antisense, hybridization, Bicyclic, Nucleoside structure, Property space, Gymnosis, Drug discovery, Pharmacokinetics, Pharmacodynamics, Non-human primate, Pre-clinical, ApoB, PCSK9, HCV, Clinical
Abstract: Over the past 10-15 years LNA (Locked Nucleic Acid) has taken a central position in nucleic acid chemistry and biology. The enhanced hybridization properties against both DNA and RNA have become a new reference in the field and proven to be enabling for many application in life sciences. For therapeutic use as RNA targeting drugs LNA enable the design of potent antisense oligonucleotides. Much effort has been dedicated to get efficient delivery of RNA targeting drugs, but in contrast to e.g. siRNA duplexes it has been demonstrated that LNA oligonucleotides are taken up by cells without added deliver vehicles in an active state (gymnotic delivery). Here, the fundamental properties of LNA are reviewed together with the recent and most advanced pre-clinical/clinical LNA data.
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Cite this article as:
Koch Troels, LNA Antisense: A Review, Current Physical Chemistry 2013; 3 (1) . https://dx.doi.org/10.2174/1877946811303010009
DOI https://dx.doi.org/10.2174/1877946811303010009 |
Print ISSN 1877-9468 |
Publisher Name Bentham Science Publisher |
Online ISSN 1877-9476 |
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