1. Fucosyltransferase-specific inhibition via next generation of fucose mimetics
- Author
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Thomas Hicks, Ana García-García, Francisco Corzana, Ramon Hurtado-Guerrero, Serena Monaco, Laura Ceballos-Laita, Kyle C. Martin, Barbara Richichi, Jesús Angulo, Jacopo Tricomi, and Robert Sackstein
- Subjects
Glycan ,Fucosyltransferase ,Cell ,01 natural sciences ,Catalysis ,Fucose ,Gene Expression Regulation, Enzymologic ,Fucosyltransferases ,03 medical and health sciences ,chemistry.chemical_compound ,Glycomimetic ,Cell Line, Tumor ,Materials Chemistry ,medicine ,Humans ,Binding site ,030304 developmental biology ,chemistry.chemical_classification ,0303 health sciences ,biology ,010405 organic chemistry ,Metals and Alloys ,Mesenchymal Stem Cells ,General Chemistry ,Precursor Cell Lymphoblastic Leukemia-Lymphoma ,0104 chemical sciences ,Surfaces, Coatings and Films ,Electronic, Optical and Magnetic Materials ,medicine.anatomical_structure ,Enzyme ,Biochemistry ,chemistry ,Ceramics and Composites ,biology.protein - Abstract
The ability to custom-modify cell surface glycans holds great promise for treatment of a variety of diseases. We propose a glycomimetic ofl-fucose that markedly inhibits the creation of sLeXby FTVI and FTVII, but has no effect on creation of LeXby FTIX. Our findings thus indicate that selective suppression of sLex display can be achieved, and STD-NMR studies surprisingly reveal that the mimetic does not compete with GDP-fucose at the enzymatic binding site.
- Published
- 2021
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