The aim is to investigate the synthesis of siRNAs containing carbocyclic nucleotides and their effects on RNA interference (RNAi).
Incorporation of 5′-(E)- and 5′-(Z)-vinylphosphonate carbocyclic DNA into siRNAs
Incorporation of 5′-(E)-vinylphosphonate 2′- and 3′-O-methyl carbocyclic RNAs
Modification of 5′ termini of antisense strands
Successful synthesis of siRNAs with carbocyclic nucleotide modifications
Demonstrated varying effects on RNAi activity based on structural conformation
Highlighted the importance of cyclopentane conformation in enhancing RNAi effects
Abstract
5′-( E )- and 5′-( Z )-vinylphosphonate carbocyclic DNA and 5′-( E )-vinylphosphonate 2′- and 3′- O -methyl carbocyclic RNAs were incorporated at 5′ termini of antisense strands of small interfering RNAs.