SCHOLARLY PUBLICATION

Fully 2‘-Modified Oligonucleotide Duplexes with Improved in Vitro Potency and Stability Compared to Unmodified Small Interfering RNA

Charles R. Allerson, Namir B. Sioufi, Russell Jarres, Thazha P. Prakash, Nishant Naik, Andrés Berdeja, Lisa Wanders, Richard H. Griffey, Eric E. Swayze, Balkrishen Bhat

📖 Journal of Medicinal Chemistry → 📅 2005-01-20 🔗 DOI: 10.1021/jm049167j

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📄 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.

📄 Abstract

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