Fluorinated rhamnosides inhibit cellular fucosylation

Johan F. A. Pijnenborg; Emiel Rossing; Jona Merx; Marek J. Noga; Willem H. C. Titulaer; Nienke Eerden; Raisa Veizaj; Paul B. White; Dirk J. Lefeber; Thomas J. Boltje

doi:10.1038/s41467-021-27355-9

Nature Communications (Dec 2021)

Fluorinated rhamnosides inhibit cellular fucosylation

Johan F. A. Pijnenborg,
Emiel Rossing,
Jona Merx,
Marek J. Noga,
Willem H. C. Titulaer,
Nienke Eerden,
Raisa Veizaj,
Paul B. White,
Dirk J. Lefeber,
Thomas J. Boltje

Affiliations

Johan F. A. Pijnenborg: Department of Synthetic Organic Chemistry, Institute for Molecules and Materials, Radboud University
Emiel Rossing: Department of Synthetic Organic Chemistry, Institute for Molecules and Materials, Radboud University
Jona Merx: Department of Synthetic Organic Chemistry, Institute for Molecules and Materials, Radboud University
Marek J. Noga: Department of Laboratory Medicine, Translational Metabolic Laboratory, Radboud University Medical Center
Willem H. C. Titulaer: Department of Synthetic Organic Chemistry, Institute for Molecules and Materials, Radboud University
Nienke Eerden: Department of Synthetic Organic Chemistry, Institute for Molecules and Materials, Radboud University
Raisa Veizaj: Department of Neurology, Donders Institute for Brain, Cognition and Behavior, Radboud University Medical Center
Paul B. White: Department of Synthetic Organic Chemistry, Institute for Molecules and Materials, Radboud University
Dirk J. Lefeber: Department of Laboratory Medicine, Translational Metabolic Laboratory, Radboud University Medical Center
Thomas J. Boltje: Department of Synthetic Organic Chemistry, Institute for Molecules and Materials, Radboud University

DOI: https://doi.org/10.1038/s41467-021-27355-9
Journal volume & issue: Vol. 12, no. 1
pp. 1 – 9

Abstract

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Aberrant expression of fucosylated glycans has been linked to several disease states. Control of fucose expression on live cells is needed to aid research and therapy development. Here the authors report on the development of a class of fucosylation metabolic prodrug inhibitors and demonstrated inhibition of cellular fucosylation.

Published in Nature Communications

ISSN: 2041-1723 (Online)
Publisher: Nature Portfolio
Country of publisher: United Kingdom
LCC subjects: Science
Website: https://www.nature.com/ncomms/

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