Synthesis and cellular uptake of fluorescently labeled multivalent hyaluronan disaccharide conjugates of oligonucleotides
: Karskela M, Virta P, Malinen M, Urtti A, Lonnberg H
: 2008
Collection Symposium Series
CHEMISTRY OF NUCLEIC ACID COMPONENTS
: COLL SYMPOS SERIES
: 10
: 369
: 371
: 3
: 978-80-86241-29-6
Clustered hyaluronan disaccharides were studied as mediators of cellular delivery of antisense oligonucleotides through receptor mediated endocytosis. A synthetic route for preparation of an appropriately protected hyaluronic acid dimer was devised. Three fluorescein-labeled phosphorothioate oligonucleotide glycoconjugates containing two, four or six hyaluronan disaccharides were prepared. The influence of the hyaluronan moieties on the cellular uptake of the thioated oligonucleotides was tested in a cell line expressing the hyaluronan receptor CD44.