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

Authors :
Schoenfeld, Ann-Kathrin
Vierfuß, Simone
LÃ?hn, Susanne
Alban, Susanne
Source :
Journal of Pharmaceutical & Biomedical Analysis. Jul2014, Vol. 95, p130-138. 9p.
Publication Year :
2014

Abstract

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]

Details

Language :
English
ISSN :
07317085
Volume :
95
Database :
Academic Search Index
Journal :
Journal of Pharmaceutical & Biomedical Analysis
Publication Type :
Academic Journal
Accession number :
95504320
Full Text :
https://doi.org/10.1016/j.jpba.2014.02.021