Synthesis, radiolabeling with fluorine-18 and preliminary in vivo evaluation of a heparan sulphate mimetic as potent angiogenesis and heparanase inhibitor for cancer applications. Issue 6 (13th January 2016)

• Record Type: Journal Article
• Authors: Kuhnast, B.; El Hadri, A.; Boisgard, R.; Hinnen, F.; Richard, S.; Caravano, A.; Nancy-Portebois, V.; Petitou, M.; Tavitian, B.; Dollé, F.
• Is Part Of: Organic & biomolecular chemistry. Volume 14:Issue 6(2016)
• Page Start: 1915
• Page End: 1920
• Publication Date: 2016-01-13
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c5ob02513c
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : A rationally designed, fully synthetic, octasaccharide-based, HS mimetic has been synthesized, in vitro characterized, labeled with fluorine-18, and in vivo imaged with PET in rats. Abstract : Heparan Sulfate (HS) mimetics are able to block crucial interactions of the components of the extracellular matrix in angiogenic processes and as such, represent a valuable class of original candidates for cancer therapy. Here we first report the synthesis and in vitro angiogenic inhibition properties of a conjugated, novel and rationally-designed octasaccharide-based HS mimetic. We also herein report its labeling with fluorine-18 and present the preliminary in vivo Positron Emission Tomography imaging data in rats. This constitutes one of the rare examples of labeling and in vivo evaluation of a synthetic, polysaccharide-based, macromolecule.