Testing of potential glycan-based heparanase inhibitors in a fluorescence activity assay using either bacterial heparinase II or human heparanase.

Highlights: [•] A simple fluorimetric heparanase activity assay using the synthetic sulfated pentasaccharide fondaparinux as substrate. [•] The assay was used for testing potential heparanase inhibitors. [•] The inhibitory activity of sulfated glycans showed to be strongly dependent on their degree of sulfation as well as their basic glycan structure, but independent of their molecular mass. [•] The semisynthetic β-1,3-glucan sulfate PS3 showed the strongest inhibitory effect with an IC50 being 160 times lower than that of suramin. [ABSTRACT FROM AUTHOR]