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Cellular Fucosylation Inhibitors Based on Fluorinated Fucose-1-Phosphates
preprintsubmitted on 09.11.2020, 21:48 and posted on 10.11.2020, 12:24 by Johan Pijnenborg, eline visser, Marek Noga, Emiel Rossing, Raisa Veizaj, Dirk J. Lefeber, Christian Büll, Thomas Boltje
Fucosylation of glycans impacts a myriad of physiological and pathological processes. Inhibition of fucose expression emerges as a potential therapeutic avenue for example in cancer, inflammation, and infection. In this study, we found that protected 2-fluorofucose 1-phosphate efficiently inhibits cellular fucosylation with a four to seven times higher potency than known inhibitor 2FF, independently of the anomeric stereochemistry. Nucleotide sugar analysis revealed that both the α- and β-GDP-2FF anomers are formed inside the cell. In conclusion, we developed A2FF1P and B2FF1P as potent new tools for studying the role of fucosylation in health and disease and they are potential therapeutic candidates.
Read the published paper
in Chemistry – A European Journal