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Alnylam and Collaborators at CNRS - Université de Montpellier Publish Paper on Novel Synthetic Method for Bi-functional 3p-siRNAs

par Bergogne Marie-Christine - publié le , mis à jour le

CAMBRIDGE, Mass., Apr 30, 2010 —Alnylam Pharmaceuticals, Inc. (Nasdaq : ALNY), a leading RNAi therapeutics company, and collaborators from the Institut des Biomolécules Max Mousseron at CNRS - Université de Montpellier, France, have reported a new synthetic method for bi-functional 3p-siRNAs. 3p-siRNAs were first described by Alnylam scientists and collaborators (Poeck et al., Nature Medicine, 14 : 1256-1263, 2008) and are designed to achieve both silencing of target genes and activation of desired immunostimulatory pathways. These new data on synthesis of 3p-siRNAs were published in the American Chemical Society’s journal, Organic Letters (DOI : 10.1021/ol1004214.)

« Alnylam’s scientific leadership is marked by our advancement of our development programs, our progress on delivery, but also our excellence in oligonucleotide chemistry, » said Muthiah Manoharan, Ph.D., Senior Vice President, Drug Discovery at Alnylam. « We are pleased to report on this new synthetic method for 3p-siRNAs, and believe that this new chemical strategy will enable the advancement of these bi-functional RNAi medicines. »

The new paper describes novel chemistries and constructs for 3p-siRNAs that may have the potential for increased efficacy because of their bi-functional mode of action, especially against cancer and viral therapeutic targets. 3p-siRNAs are characterized by the presence of a 5’-end triphosphate moiety and the ability to activate retinoic acid-induced gene I, RIG-I, a cytoplasmic immunoreceptor. The new synthetic approach utilizes H-phosphonate intermediates for the synthesis of the 5’-triphosphate. The reported synthetic procedure represents a highly efficient alternative to the few examples described in the literature to date. Alnylam is evaluating the use of bi-functional 3p-siRNAs as potential therapeutics.

Contacts : Françoise Debart, François Morvan, Jean-Jacques Vasseur

Alnylam Pharmaceuticals, Inc. : http://www.alnylam.com/