Post-synthetic orthogonal amidation plus metal catalyzed azide-alkyne cycloaddition click chemistry on siRNA

摘要

#$%^&*AU2018223027B220200326.pdf#####Abstract This invention relates to the post-synthetic chemical modifications of RNA at the 2'-position in the ribose 5 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 posttranscriptional gene silencing found in fungi, plants and 10 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. C:NRPortblGHMattersMICHELES10612979_1.docx 30/08/181/70 0la 0 O0f 0 0/ %O/%0 = ~ 0 0 0 0 0~ ~ 00 0 O0 /D t CI m0 0 C. 0 0 0 00 Cif 42QL 0 C4 :m~ = / 0 0cJU 0/ 0 = 000? 00 00 0 % 0= %,Q ="04 0 _ a004 00 0 0D 0- 0cmI "00