Unique Gene-Silencing and Structural Properties of 2′-Fluoro-Modified siRNAs (pages 2284–2288)
Dr. Muthiah Manoharan, Dr. Akin Akinc, Dr. Rajendra K. Pandey, June Qin, Dr. Philipp Hadwiger, Dr. Matthias John, Kathy Mills, Dr. Klaus Charisse, Dr. Martin A. Maier, Dr. Lubomir Nechev, Emily M. Greene, Dr. Pradeep S. Pallan, Prof. Eriks Rozners, Dr. Kallanthottathil G. Rajeev and Prof. Martin Egli
Article first published online: 31 JAN 2011 | DOI: 10.1002/anie.201006519
With little or no negative impact on the activity of small interfering RNAs (siRNAs), regardless of the number of modifications or the positions within the strand, the 2′-deoxy-2′-fluoro (2′-F) modification is unique. Furthermore, the 2′-F-modified siRNA (see crystal structure) was thermodynamically more stable and more nuclease-resistant than the parent siRNA, and produced no immunostimulatory response.