Author

Nicky de Koster

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Open access Oct 2026

Uridine Bisphosphonate-Carbagalactose: A Stabilized α‑1,4-Galactosyltransferase Inhibitor

Methylene and difluoromethylene uridine bisphosphonate carbagalactose were designed and synthesized as stable uridine diphosphate-galactose (UDP-Gal) mimics for probing α-1,4-galactosyltransferase (A4GALT). In these analogues, the labile glycosidic and pyrophosphate linkages of UDP-Gal are replaced by chemically and en...

Jian-Yun Guo, Nicky de Koster, Bob van Puffelen et al. · Organic Letters · 0 citations

Open access Aug 2026

Unraveling A4GALT Mechanism and Its Modulation With Adamantyl-Galactosylceramide Analogues: Advancing Fabry Disease Therapeutic Strategies.

The molecular mechanism of human A4GALT is revealed at atomic detail using QM/MM simulations, revealing a conformational rearrangement involving a 310-helix that stabilizes the donor substrate and promotes a front-face SNi-like catalytic mechanism, in which a short-lived oxocarbenium-ion intermediate forms.

Nicky de Koster, Òscar Vidal-Gironès, Rowan de Graaf et al. · Angewandte Chemie · 0 citations