Fucosyltransferase-specific inhibition via next generation of fucose mimetics

利用新一代岩藻糖类似物实现岩藻糖基转移酶特异性抑制

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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 sLe(X) by FTVI and FTVII, but has no effect on creation of Le(X) 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.

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