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Interfacing carbohdyrate, lipid and oligonucleotide technologies: Evolution of novel aptamers

Applicant Dr. Annika Ries
Subject Area Biological and Biomimetic Chemistry
Term from 2014 to 2016
Project identifier Deutsche Forschungsgemeinschaft (DFG) - Project number 256834823
 
Final Report Year 2016

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.

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