Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates

Description

Oligoribonucleotide conjugates carrying apolar carbohydrates at the 5′-end and the corresponding siRNA duplexes have been prepared using phosphoramidite chemistry. All the carbohydrate-siRNA derivatives were compatible with RNA interference machinery if transfected with oligofectamine. In the absence of a transfection agent, some of them exerted certain reduction of gene expression. Double-tailed permethylated glucose conjugated to siRNA through a long spacer inhibited gene expression up to 26% compared to the scrambled duplex. Such modifications contribute positively to the stability of oligoribonucleotides against 5′-exonuclease degradation.

Abstract

Ministerio de Economía y Competitividad CTQ2009-13705, CTQ2010-20541

Abstract

Generalitat de Catalunya 2009/SGR/208

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