1. Cellular Fucosylation Inhibitors Based on Fluorinated Fucose-1-phosphates*.
- Author
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Pijnenborg JFA, Visser EA, Noga M, Rossing E, Veizaj R, Lefeber DJ, Büll C, and Boltje TJ
- Subjects
- Cell Line, Tumor, Glycosylation, Phosphates, Fucose, Polysaccharides
- Abstract
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., (© 2020 The Authors. Chemistry - A European Journal published by Wiley-VCH GmbH.)
- Published
- 2021
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