Iminosugar glycosidase inhibitors: structural and thermodynamic dissection of the binding of isofagomine and 1-deoxynojirimycin to beta-glucosidases.

@article{Zechel2003IminosugarGI,
  title={Iminosugar glycosidase inhibitors: structural and thermodynamic dissection of the binding of isofagomine and 1-deoxynojirimycin to beta-glucosidases.},
  author={David L. Zechel and Alisdair Bennett Boraston and Tracey M Gloster and Catherine M Boraston and James M Macdonald and D Matthew G Tilbrook and Robert V Stick and Gideon J Davies},
  journal={Journal of the American Chemical Society},
  year={2003},
  volume={125 47},
  pages={14313-23}
}
The design and synthesis of transition-state mimics reflects the growing need both to understand enzymatic catalysis and to influence strategies for therapeutic intervention. Iminosugars are among the most potent inhibitors of glycosidases. Here, the binding of 1-deoxynojirimycin and (+)-isofagomine to the "family GH-1" beta-glucosidase of Thermotoga maritima is investigated by kinetic analysis, isothermal titration calorimetry, and X-ray crystallography. The binding of both of these iminosugar… CONTINUE READING