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. All but the 3′-O-methyl carbocyclic analogue resulted in gene silencing activity better than the siRNA lacking a 5′ phosphate in cells and in mice.
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J. Kundu, D. Datta, M. Akabane-Nakata, S. Mandal, M. Krampert, M. Egli and M. Manoharan, RSC Chem. Biol., 2026, Advance Article , DOI: 10.1039/D6CB00038J
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