0000000000563649
AUTHOR
Dirk Dr Seiffge
Oligosaccharide recognition by selectins: Synthesis and biological activity of multivalent sialyl lewis-X ligands
Abstract Trivalent sialyl Lewis-X ligands 6–8 anchored onto flexible templates have been synthesized and evaluated as inhibitors of E-selectin and P-selectin mediated cell adhesion in cell culture assays and in vivo. Biological activities in vitro correlated with spacer length and lead to ligands with 3-fold (E-selectin) and 5-fold (P-selectin) improved receptor binding avidity per single tetrasaccharide moiety.
Synthesis and biological activity of novel sialyl-lewisX conjugates
Abstract Novel sialyl Lewis X conjugates have been synthesized and evaluated as inhibitors of E- and P-selectin mediated cell adhesion in cell culture assays. The most potent conjugate in the static inhibition assays exhibited a significant and dose-dependent pharmacological potency as inhibitor of the edotoxin-induced leukocyte adhesion to the endothelium of postcapillary venules in rats.