Unique Gene‐Silencing and Structural Properties of 2′‐Fluoro‐Modified siRNAs

Muthiah Manoharan(Alnylam Pharmaceuticals (United States)), Akin Akinc(Alnylam Pharmaceuticals (United States)), Rajendra K. Pandey(Alnylam Pharmaceuticals (United States)), June Qin(Alnylam Pharmaceuticals (United States)), Philipp Hadwiger(Alnylam Pharmaceuticals (United States)), Matthias John(Alnylam Pharmaceuticals (United States)), Kathy Mills(Alnylam Pharmaceuticals (United States)), Klaus Charissé(Alnylam Pharmaceuticals (United States)), Martin A. Maier(Alnylam Pharmaceuticals (United States)), Lubomir V. Nechev(Alnylam Pharmaceuticals (United States)), Emily M. Greene(Binghamton University), Pradeep S. Pallan(Vanderbilt University), Eriks Rozners(Binghamton University), Kallanthottathil G. Rajeev(Alnylam Pharmaceuticals (United States)), Martin Egli(Alnylam Pharmaceuticals (United States))
Angewandte Chemie International Edition
January 31, 2011
Cited by 184

Abstract

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. Detailed facts of importance to specialist readers are published as ”Supporting Information”. Such documents are peer-reviewed, but not copy-edited or typeset. They are made available as submitted by the authors. Please note: The publisher is not responsible for the content or functionality of any supporting information supplied by the authors. Any queries (other than missing content) should be directed to the corresponding author for the article.


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