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- W2024244702 abstract "Insufficient efficacy and/or specificity of antisense oligonucleotides limit their in vivo usefulness. We demonstrate here that a high-affinity DNA analog, locked nucleic acid (LNA), confers several desired properties to antisense agents. Unlike DNA, LNA/DNA copolymers were not degraded readily in blood serum and cell extracts. However, like DNA, the LNA/DNA copolymers were capable of activating RNase H, an important antisense mechanism of action. In contrast to phosphorothioate-containing oligonucleotides, isosequential LNA analogs did not cause detectable toxic reactions in rat brain. LNA/DNA copolymers exhibited potent antisense activity on assay systems as disparate as a G-protein-coupled receptor in living rat brain and an Escherichia coli reporter gene. LNA-containing oligonucleotides will likely be useful for many antisense applications." @default.
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- W2024244702 date "2000-05-09" @default.
- W2024244702 modified "2023-09-30" @default.
- W2024244702 title "Potent and nontoxic antisense oligonucleotides containing locked nucleic acids" @default.
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- W2024244702 doi "https://doi.org/10.1073/pnas.97.10.5633" @default.
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