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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Autores: Vengut Climent, Empar, Terrazas, Montserrat, Lucas Rodríguez, Ricardo, Arévalo Ruiz, Matilde, Eritja, Ramón, Morales, Juan Carlos
Tipo de recurso: artículo
Estado:Versión aceptada para publicación
Fecha de publicación:2013
País:España
Institución:Universidad de Sevilla (US)
Repositorio:idUS. Depósito de Investigación de la Universidad de Sevilla
OAI Identifier:oai:idus.us.es:11441/135277
Acceso en línea:https://hdl.handle.net/11441/135277
https://doi.org/10.1016/j.bmcl.2013.05.065
Access Level:acceso abierto
Palabra clave:Carbohydrate
Lipophilic vector
Modified siRNA
Phosphoramidite
siRNA
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spelling Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugatesVengut Climent, EmparTerrazas, MontserratLucas Rodríguez, RicardoArévalo Ruiz, MatildeEritja, RamónMorales, Juan CarlosCarbohydrateLipophilic vectorModified siRNAPhosphoramiditesiRNAOligoribonucleotide 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.Ministerio de Economía y Competitividad CTQ2009-13705, CTQ2010-20541Generalitat de Catalunya 2009/SGR/208ElsevierQuímica Orgánica y FarmacéuticaMinisterio de Economía y Competitividad (MINECO). EspañaGeneralitat de Catalunya2013info:eu-repo/semantics/articleinfo:eu-repo/semantics/acceptedVersionapplication/pdfapplication/pdfhttps://hdl.handle.net/11441/135277https://doi.org/10.1016/j.bmcl.2013.05.065reponame:idUS. Depósito de Investigación de la Universidad de Sevillainstname:Universidad de Sevilla (US)InglésBioorganic and Medicinal Chemistry Letters, 23 (14), 4048-4051.CTQ2009-13705CTQ2010-205412009/SGR/208https://doi.org/10.1016/j.bmcl.2013.05.065info:eu-repo/semantics/openAccessoai:idus.us.es:11441/1352772026-06-17T12:51:07Z
dc.title.none.fl_str_mv Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates
title Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates
spellingShingle Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates
Vengut Climent, Empar
Carbohydrate
Lipophilic vector
Modified siRNA
Phosphoramidite
siRNA
title_short Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates
title_full Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates
title_fullStr Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates
title_full_unstemmed Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates
title_sort Synthesis, RNAi activity and nuclease-resistant properties of apolar carbohydrates siRNA conjugates
dc.creator.none.fl_str_mv Vengut Climent, Empar
Terrazas, Montserrat
Lucas Rodríguez, Ricardo
Arévalo Ruiz, Matilde
Eritja, Ramón
Morales, Juan Carlos
author Vengut Climent, Empar
author_facet Vengut Climent, Empar
Terrazas, Montserrat
Lucas Rodríguez, Ricardo
Arévalo Ruiz, Matilde
Eritja, Ramón
Morales, Juan Carlos
author_role author
author2 Terrazas, Montserrat
Lucas Rodríguez, Ricardo
Arévalo Ruiz, Matilde
Eritja, Ramón
Morales, Juan Carlos
author2_role author
author
author
author
author
dc.contributor.none.fl_str_mv Química Orgánica y Farmacéutica
Ministerio de Economía y Competitividad (MINECO). España
Generalitat de Catalunya
dc.subject.none.fl_str_mv Carbohydrate
Lipophilic vector
Modified siRNA
Phosphoramidite
siRNA
topic Carbohydrate
Lipophilic vector
Modified siRNA
Phosphoramidite
siRNA
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.
publishDate 2013
dc.date.none.fl_str_mv 2013
dc.type.none.fl_str_mv info:eu-repo/semantics/article
info:eu-repo/semantics/acceptedVersion
format article
status_str acceptedVersion
dc.identifier.none.fl_str_mv https://hdl.handle.net/11441/135277
https://doi.org/10.1016/j.bmcl.2013.05.065
url https://hdl.handle.net/11441/135277
https://doi.org/10.1016/j.bmcl.2013.05.065
dc.language.none.fl_str_mv Inglés
language_invalid_str_mv Inglés
dc.relation.none.fl_str_mv Bioorganic and Medicinal Chemistry Letters, 23 (14), 4048-4051.
CTQ2009-13705
CTQ2010-20541
2009/SGR/208
https://doi.org/10.1016/j.bmcl.2013.05.065
dc.rights.none.fl_str_mv info:eu-repo/semantics/openAccess
eu_rights_str_mv openAccess
dc.format.none.fl_str_mv application/pdf
application/pdf
dc.publisher.none.fl_str_mv Elsevier
publisher.none.fl_str_mv Elsevier
dc.source.none.fl_str_mv reponame:idUS. Depósito de Investigación de la Universidad de Sevilla
instname:Universidad de Sevilla (US)
instname_str Universidad de Sevilla (US)
reponame_str idUS. Depósito de Investigación de la Universidad de Sevilla
collection idUS. Depósito de Investigación de la Universidad de Sevilla
repository.name.fl_str_mv
repository.mail.fl_str_mv
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score 15,300724

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