Title of article :
Probing the aglycon binding site of a β-glucosidase: a collection of C-1-modified 2,5-dideoxy-2,5-imino-d-mannitol derivatives and their structure–activity relationships as competitive inhibitors Original Research Article
Author/Authors :
Tanja M. Wrodnigg، نويسنده , , Frederik Diness، نويسنده , , Christoph Gruber، نويسنده , , Herwig H?usler، نويسنده , , Inge Lundt، نويسنده , , Karen Rupitz، نويسنده , , Andreas J. Steiner، نويسنده , , Arnold E. Stütz، نويسنده , , Chris A. Tarling، نويسنده , , Stephen G. Withers and Pedro M. Alzari، نويسنده , , Heidrun W?lfler، نويسنده ,
Abstract :
A range of new C-1 modified derivatives of the powerful glucosidase inhibitor 2,5-dideoxy-2,5-imino-d-mannitol has been synthesised and their biological activities probed with the β-glucosidase from Agrobacterium sp. Ki values are compared with those of previously prepared close relatives. Findings suggest dramatic effects exerted by the aglycon binding site on substrate/inhibitor binding.