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Comparative Study
. 2005 Feb 24;48(4):901-4.
doi: 10.1021/jm049167j.

Fully 2'-modified oligonucleotide duplexes with improved in vitro potency and stability compared to unmodified small interfering RNA

Charles R Allerson  1 , Namir Sioufi, Russell Jarres, Thazha P Prakash, Nishant Naik, Andres Berdeja, Lisa Wanders, Richard H Griffey, Eric E Swayze, Balkrishen Bhat
Affiliations
Comparative Study

Fully 2'-modified oligonucleotide duplexes with improved in vitro potency and stability compared to unmodified small interfering RNA

Charles R Allerson et al. J Med Chem. .

Abstract

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.

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