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Issue 9, 2021
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Fucosyltransferase-specific inhibition via next generation of fucose mimetics

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Abstract

The ability to custom-modify cell surface glycans holds great promise for treatment of a variety of diseases. We propose a glycomimetic of L-fucose that markedly inhibits the creation of sLeX by FTVI and FTVII, but has no effect on creation of LeX by 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.

Graphical abstract: Fucosyltransferase-specific inhibition via next generation of fucose mimetics

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Supplementary files

Article information


Submitted
16 Jul 2020
Accepted
25 Sep 2020
First published
07 Jan 2021

Chem. Commun., 2021,57, 1145-1148
Article type
Communication

Fucosyltransferase-specific inhibition via next generation of fucose mimetics

K. C. Martin, J. Tricomi, F. Corzana, A. García-García, L. Ceballos-Laita, T. Hicks, S. Monaco, J. Angulo, R. Hurtado-Guerrero, B. Richichi and R. Sackstein, Chem. Commun., 2021, 57, 1145 DOI: 10.1039/D0CC04847J

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