Nature Communications (Aug 2018)

Revealing the mechanism for covalent inhibition of glycoside hydrolases by carbasugars at an atomic level

  • Weiwu Ren,
  • Robert Pengelly,
  • Marco Farren-Dai,
  • Saeideh Shamsi Kazem Abadi,
  • Verena Oehler,
  • Oluwafemi Akintola,
  • Jason Draper,
  • Michael Meanwell,
  • Saswati Chakladar,
  • Katarzyna Świderek,
  • Vicent Moliner,
  • Robert Britton,
  • Tracey M. Gloster,
  • Andrew J. Bennet

DOI
https://doi.org/10.1038/s41467-018-05702-7
Journal volume & issue
Vol. 9, no. 1
pp. 1 – 12

Abstract

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Mechanism-based inhibitors of glycoside hydrolases are useful probes for basic research and represent potential drug candidates. Here, the authors present a series of mechanism-based covalent α-galactosidase inhibitors and elucidate the kinetic and structural basis of their inhibitory activity.