caa a22 4500 445878657 CHVBK 20180317145535.0 cr unu---uuuuu 170323e20110801xx s 000 0 eng 10.1007/s11030-011-9305-6 doi (NATIONALLICENCE)springer-10.1007/s11030-011-9305-6 Synthesis and in vitro inhibition properties of siRNA conjugates carrying glucose and galactose with different presentations [Elektronische Daten] [Anna Aviñó, Sandra Ocampo, Ricardo Lucas, José Reina, Juan Morales, José Perales, Ramon Eritja] Oligoribonucleotide conjugates and the corresponding siRNA duplexes against tumor necrosis factor carrying one, two, or four glucose and galactose residues at the 5′-end have been prepared using phosphoramidite chemistry. Carbohydrate-modified siRNA duplexes have similar inhibitory properties than unmodified RNA duplexes in HeLa cells transfected with oligofectamine. When HeLa cells were treated with siRNA carrying one, two, or four glucose residues without oligofectamine, no inhibition was observed. The inhibitory properties of siRNA carrying galactose residues without transfecting agent were tested on HuH-7 cells that have abundant asialoglycoprotein receptors. In these cells siRNA carrying galactose residues have slight anti-TNF inhibitory properties (25% in the best case) that are eliminated if the receptors are blocked with a competitor. These results demonstrate receptor-mediated uptake of siRNA carrying galactose residues, although the efficacy of the process is not enough for efficient RNA interference experiments. Springer Science+Business Media B.V., 2011 siRNA nationallicence Oligonucleotide-carbohydrate conjugates nationallicence RNA interference nationallicence Tumor necrosis factor nationallicence Oligonucleotide synthesis nationallicence Aviñó Anna Institute for Research in Biomedicine (IRB Barcelona), Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Networking Centre on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Baldiri Reixac 10, 08028, Barcelona, Spain aut Ocampo Sandra Institute for Research in Biomedicine (IRB Barcelona), Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Networking Centre on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Baldiri Reixac 10, 08028, Barcelona, Spain aut Lucas Ricardo Instituto de Investigaciones Químicas, CSIC-Universidad de Sevilla, 49 Americo Vespucio, 41092, Sevilla, Spain aut Reina José Instituto de Investigaciones Químicas, CSIC-Universidad de Sevilla, 49 Americo Vespucio, 41092, Sevilla, Spain aut Morales Juan Instituto de Investigaciones Químicas, CSIC-Universidad de Sevilla, 49 Americo Vespucio, 41092, Sevilla, Spain aut Perales José Department of Ciencies Fisiológiques, School of Medicine, University of Barcelona (Campus Belvitge), C/Feixa Llarga, L'Hospitalet de Llobregat, 08907, Barcelona, Spain aut Eritja Ramon Institute for Research in Biomedicine (IRB Barcelona), Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Networking Centre on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Baldiri Reixac 10, 08028, Barcelona, Spain aut Molecular Diversity Springer Netherlands 15/3(2011-08-01), 751-757 1381-1991 15:3<751 2011 15 11030 https://doi.org/10.1007/s11030-011-9305-6 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/s11030-011-9305-6 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Aviñó Anna Institute for Research in Biomedicine (IRB Barcelona), Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Networking Centre on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Baldiri Reixac 10, 08028, Barcelona, Spain aut NATIONALLICENCE 700 1- Ocampo Sandra Institute for Research in Biomedicine (IRB Barcelona), Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Networking Centre on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Baldiri Reixac 10, 08028, Barcelona, Spain aut NATIONALLICENCE 700 1- Lucas Ricardo Instituto de Investigaciones Químicas, CSIC-Universidad de Sevilla, 49 Americo Vespucio, 41092, Sevilla, Spain aut NATIONALLICENCE 700 1- Reina José Instituto de Investigaciones Químicas, CSIC-Universidad de Sevilla, 49 Americo Vespucio, 41092, Sevilla, Spain aut NATIONALLICENCE 700 1- Morales Juan Instituto de Investigaciones Químicas, CSIC-Universidad de Sevilla, 49 Americo Vespucio, 41092, Sevilla, Spain aut NATIONALLICENCE 700 1- Perales José Department of Ciencies Fisiológiques, School of Medicine, University of Barcelona (Campus Belvitge), C/Feixa Llarga, L'Hospitalet de Llobregat, 08907, Barcelona, Spain aut NATIONALLICENCE 700 1- Eritja Ramon Institute for Research in Biomedicine (IRB Barcelona), Institute for Advanced Chemistry of Catalonia (IQAC-CSIC), Networking Centre on Bioengineering, Biomaterials and Nanomedicine (CIBER-BBN), Baldiri Reixac 10, 08028, Barcelona, Spain aut NATIONALLICENCE 773 0- Molecular Diversity Springer Netherlands 15/3(2011-08-01), 751-757 1381-1991 15:3<751 2011 15 11030 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer