Sialyl Lewisx-liposomes as vehicles for site-directed, E-selectin-mediated drug transfer into activated endothelial cells |
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Authors: | R. Stahn C. Grittner R. Zeisig U. Karsten S. B. Felix K. Wenzel |
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Affiliation: | Max Delbrück Center for Molecular Medicine, Berlin, Germany. renate.stahn@nemod.com |
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Abstract: | E-selectin, exclusively expressed on activated endothelial cells, is a potential target for site-directed delivery of agents. We and others have shown that sialyl Lewisx-liposomes (sLex-liposomes) are recognized by E-selectin. We now report an approach employing sLex-liposomes to deliver antisense oligonucleotides (AS-ODNs) directed against the adhesion molecule ICAM-1 to activated vascular endothelial cells. ICAM-1 expression was analyzed at the protein level by immunofluorescence and a cell surface ELISA, and at the RNA level by RT-PCR. We have investigated two different AS-ODNs complementary to the 3′ untranslated region and the AUG translation initiation codon of ICAM-1 mRNA. Both inhibited protein expression, but did not influence the mRNA level, pointing to a hybridization of AS-ODNs with the mRNA in the cytoplasm. Our results demonstrate the feasibility of a novel approach for the delivery of agents to activated endothelial cells by glycoliposomes targeted to E-selectin. Received 16 October 2000; revised 29 November 2000; accepted 29 November 2000 |
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Keywords: | . E-selectin sLex-liposomes site-directed delivery antisense strategy ICAM-1. |
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