Research Highlights
Structural Basis of α-Fucosidase Inhibition by Iminocyclitols with Ki Values in the Micro- to Picomolar Range

Two loops were found to move inward toward the α-fucosidase active site to produce a closed conformation of complexes with inhibitors with increasing Ki values from the micro- to nanomolar range. Although no further conformational changes in the two loops are observed for inhibitors with sub-nanomolar Ki values, the loops are additionally stabilized by hydrogen bonds and hydrophobic interactions.

Article link: https://doi.org/10.1002/anie.200905597

Authors: Wu HJ, Ho CW, Ko TP, Popat SD, Lin CH*, Wang AH*

Updated: 2010.01.08