1362317-63-2Relevant academic research and scientific papers
Efficient synthesis and cell-based silencing activity of siRNAS that contain triazole backbone linkages
Efthymiou, Tim C.,Huynh, Vanthi,Oentoro, Jaymie,Peel, Brandon,Desaulniers, Jean-Paul
, p. 1722 - 1726 (2012/04/04)
An efficient synthesis of siRNAs modified at the backbone with a triazole functionality is reported. Through the use of 4,4×-dimethoxytrityl (DMT) phosphoramidite chemistry, triazole backbone dimmers were site-specifically incorporated throughout various siRNAs targeting both firefly luciferase and glyceraldehyde- 3-phosphate dehydrogenase (GAPDH) gene transcripts as representatives of an exogenous and endogenous gene, respectively. Following the successful silencing of the firefly luciferase reporter gene, triazole-modified siRNAs were also found to be capable of silencing GAPDH in a dose-dependent manner. Backbone modifications approaching the 3×-end on the sense strand were tolerated without compromising siRNA potency. This study highlights the compatibility of triazole-modified siRNAs within the RNAi pathway, and the modification's potential to impart favorable properties to siRNAs designed to target other endogenous genes.
