POST-SYNTHETIC ORTHOGONAL AMIDATION PLUS METAL CATALYZED AZIDE-ALKYNE CYCLOADDITION CLICK CHEMISTRY ON siRNA

摘要

This invention relates to the post-synthetic chemical modifications of RNA at the 2' -position on the ribose rings via orthogonal chemistry involving amidation reactions plus metal catalyzed alkyne-azide cycloaddition (click) reactions. RNA interference (RNAi) is an evolutionarily conserved cellular mechanism of post-transcriptional gene silencing found in fungi, plants and animals that uses small RNA molecules to inhibit gene expression in a sequence-specific manner. The RNAi machinery can be harnessed to destruct any mRNA of a known sequence.