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Accueil > Publications > Recherche par années > Années 1990 > 1996

Stewart, AJ ; Pichon, C ; Meunier, L ; Midoux, P ; Monsigny, M ; Roche, AC

Enhanced biological activity of antisense oligonucleotides complexed with glycosylated poly-L-lysine

Molecular Pharmacology 50 (6) 1487-1494

par Administrateur - publié le

Abstract :

We sought to exploit glycosylated poly-L-lysine (pLK) to increase the uptake and biological antisense activity of a phosphorothioate oligonucleotide (pt-odn) [pt-odn complementary to the 3’ noncoding region of intercellular adhesion molecule-1 ICAM-1)(odn(ICAM-1))] complementary to the 3’-noncoding region of ICAM-1 in A549 cells. Dose-dependent inhibition of ICAM-1 expression was obtained (IC50 = 500 nM) through treatment of cells with odn(ICAM-1) complexed with pLK carrying fucose residues in the presence of 100 mu M chloroquine. Alteration in the charge ratio between fucosylated pLK and pt-odn had a significant effect on the efficacy of inhibition (optimal conditions, charge ratio = 1.1).