A Direct, Efficient Method for the Preparation of siRNAs Containing Ribo-like North Bicyclo[3.1.0]hexane Pseudosugars

An efficient method for the preparation of siRNAs modified with ribo-like North bicyclo[3.1.0]hexane pseudosugars is described. The combined use of 2′-O-(2-cyanoethoxymethyl) (CEM) and 2′-O-TBDMS protection was successfully employed for RNA synthesis with the added advantage that both groups were efficiently removed in a single step. The resulting North ribo-methanocarba-modified siRNAs are compatible with the intracellular RNAi machinery and can mediate specific degradation of target mRNA.This research was supported by the Spanish Ministry of Education (BFU2007-63287 and CTQ2010-20541-C03-01) and the Generalitat de Catalunya (2009/SGR/208) and the Instituto de Salud Carlos III. This work was funded in part by the Center for Cancer Research,NationalCancer Institute,NIH.M.T. acknowledges the Juan de la Cierva contract (MICINN, Spain) for financial support.Peer reviewe

A direct, efficient method for the preparation of siRNAs containing ribo like North [3.1.0]hexane pseudosugars

An efficient method for the preparation of siRNAs modified with ribo-like North bicyclo[3.1.0]hexane pseudosugars is described. The combined use of 2'-O-(2-cyanoethoxymethyl) (CEM) and 2'-O-TBDMS protection was successfully employed for RNA synthesis with the added advantage that both groups were efficiently removed in a single step. The resulting North ribo-methanocarba-modified siRNAs are compatible with the intracellular RNAi machinery and can mediate specific degradation of target mRNA