Article
Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates
Author/s | Vengut Climent, Empar
Terrazas, Montserrat Lucas Rodríguez, Ricardo Arévalo Ruiz, Matilde Eritja, Ramón Morales, Juan Carlos |
Department | Universidad de Sevilla. Departamento de Química Orgánica y Farmacéutica |
Publication Date | 2013 |
Deposit Date | 2022-07-12 |
Published in |
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Abstract | 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 ... 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. |
Funding agencies | Ministerio de Economía y Competitividad (MINECO). España Generalitat de Catalunya |
Project ID. | CTQ2009-13705
CTQ2010-20541 2009/SGR/208 |
Citation | Vengut Climent, E., Terrazas, M., Lucas Rodríguez, R., Arévalo Ruiz, M., Eritja, R. y Morales, J.C. (2013). Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates. Bioorganic and Medicinal Chemistry Letters, 23 (14), 4048-4051. |
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