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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Institution: | 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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