Fully 2 '-modified oligonucleotide duplexes with improved in vitro potency and stability compared to unmodified small interfering RNA
CR Allerson, N Sioufi, R Jarres… - Journal of medicinal …, 2005 - ACS Publications
CR Allerson, N Sioufi, R Jarres, TP Prakash, N Naik, A Berdeja, L Wanders, RH Griffey…
Journal of medicinal chemistry, 2005•ACS PublicationsWe have identified a small interfering RNA (siRNA) motif, consisting entirely of 2 '-O-methyl
and 2 '-fluoro nucleotides, that displays enhanced plasma stability and increased in vitro
potency. At one site, this motif showed remarkable> 500-fold improvement in potency over
the unmodified siRNA. This marks the first report of such a potent fully modified motif, which
may represent a useful design for therapeutic oligonucleotides.
and 2 '-fluoro nucleotides, that displays enhanced plasma stability and increased in vitro
potency. At one site, this motif showed remarkable> 500-fold improvement in potency over
the unmodified siRNA. This marks the first report of such a potent fully modified motif, which
may represent a useful design for therapeutic oligonucleotides.
We have identified a small interfering RNA (siRNA) motif, consisting entirely of 2‘-O-methyl and 2‘-fluoro nucleotides, that displays enhanced plasma stability and increased in vitro potency. At one site, this motif showed remarkable >500-fold improvement in potency over the unmodified siRNA. This marks the first report of such a potent fully modified motif, which may represent a useful design for therapeutic oligonucleotides.
ACS Publications