Interfacing carbohdyrate, lipid and oligonucleotide technologies: Evolution of novel aptamers
Final Report Abstract
During this research period seven novel galactose/galactosamine-containing thymidine, LNA-T and 2ʹ-amino-LNA-T phosphoramidites have been synthesized and successfully used for solid supported automated synthesis of galactose/galactosamine-functionalized ONs. Especially, the galactose-modified LNA-T and 2ʹ-amino-LNA-T containing ONs showed high duplex stability and good base-pairing specificity. We have thus demonstrated that the 5-position of thymidine and LNA-T and the 2ʹ-position of 2ʹ-amino-LNA-T are highly suitable for attachment of carbohydrate moieties within high-affinity ONs for biomedical research. Attachment of other monosaccharides and oligosaccharides is possible together with evaluation of the novel constructs in the context of nucleic acid drug development e.g. antisense and aptamer technology.
Publications
- “Synthesis and biophysical investigations of oligonucleotides containing Galactose-Modified DNA, LNA, and 2′-Amino-LNA Monomers”. J. Org. Chem., 2016, 81 (22), pp 10845–10856
Annika Ries, Rajesh Kumar, Chenguang Lou, Tamer Kosbar, Empar Vengut-Climent, Per Trolle Jørgensen, Juan C. Morales, Jesper Wengel
(See online at https://doi.org/10.1021/acs.joc.6b01917) - Synthesis and Excellent Duplex Stability of Oligonucleotides Containing 2′-Amino-LNA Functionalized with Galactose Units”. Molecules 2017, 22(5), 852
Rajesh Kumar, Annika Ries, Jesper Wengel
(See online at https://doi.org/10.3390/molecules22050852)
