Abstract
Oligonucleotides containing internal triazole-3'-LNA linkages bind to complementary RNA with similar affinity and specificity to unmodified oligonucleotides, and significantly better than oligonucleotides containing triazole alone. In contrast LNA on the 5'-side of the triazole does not stabilise duplexes. Triazole-LNA confers great resistance towards enzymatic degradation relative to LNA alone.
Highlights
Oligonucleotides containing internal triazole–30-Locked nucleic acid (LNA) linkages bind to complementary RNA with similar affinity and specificity to unmodified oligonucleotides, and significantly better than oligonucleotides containing triazole alone
The most intensively studied of these is the biocompatible triazole-linkage in Fig. 1a which has recently emerged as an important tool in the chemical synthesis of long pieces of DNA.[7]
ON’s containing LNA units display some resistance to enzymatic degradation, they still possess a natural phosphodiester linkage which is vulnerable to nucleases
Summary
Oligonucleotides containing internal triazole–30-LNA linkages bind to complementary RNA with similar affinity and specificity to unmodified oligonucleotides, and significantly better than oligonucleotides containing triazole alone. In this study we aimed to improve the binding affinity of triazole linked ON’s by introducing LNA sugars adjacent to the linkage.
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