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

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 absenc...

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Detalles Bibliográficos
Autores: Vengut-Climent, Empar, Terrazas, Montserrat, Lucas, Ricardo, Arévalo-Ruiz, Matilde, Eritja Casadellà, Ramón, Morales, Juan Carlos
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2013
País:España
Institución:Consejo Superior de Investigaciones Científicas (CSIC)
Repositorio:DIGITAL.CSIC. Repositorio Institucional del CSIC
OAI Identifier:oai:digital.csic.es:10261/125374
Acceso en línea:http://hdl.handle.net/10261/125374
Access Level:acceso abierto
Palabra clave:Carbohydrates
RNA
Lipophilic vector
siRNA
Modified siRNA
Phosphoramidite
Descripción
Sumario: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.