Low molecular weight antagonists of the myelin-associated glycoprotein: synthesis, docking, and biological evaluation

…, M Wittwer, S Rabbani, O Schwardt…

Index: Stokmaier, Daniela; Khorev, Oleg; Cutting, Brian; Born, Rita; Ricklin, Daniel; Ernst, Thomas O.G.; Boeni, Fabienne; Schwingruber, Kathrin; Gentner, Martin; Wittwer, Matthias; Spreafico, Morena; Vedani, Angelo; Rabbani, Said; Schwardt, Oliver; Ernst, Beat Bioorganic and Medicinal Chemistry, 2009 , vol. 17, # 20 p. 7254 - 7264

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Citation Number: 27

Abstract

The injured adult mammalian central nervous system is an inhibitory environment for axon regeneration due to specific inhibitors, among them the myelin-associated glycoprotein (MAG), a member of the Siglec family (sialic-acid binding immunoglobulin-like lectin). In earlier studies, we identified the lead structure 5, which shows a 250-fold improved in vitro affinity for MAG compared to the tetrasaccharide binding epitope of GQ1bα (1), the best ...