Fiche publication
Date publication
avril 2016
Journal
Chemistry (Weinheim an der Bergstrasse, Germany)
Auteurs
Membres identifiés du Cancéropôle Est :
Dr BIRCK Catherine
Tous les auteurs :
Lepage ML, Schneider JP, Bodlenner A, Meli A, De Riccardis F, Schmitt M, Tarnus C, Nguyen-Huynh NT, Francois YN, Leize-Wagner E, Birck C, Cousido-Siah A, Podjarny A, Izzo I, Compain P
Lien Pubmed
Résumé
A series of cyclopeptoid-based iminosugar clusters has been evaluated to finely probe the ligand content-dependent increase in α-mannosidase inhibition. This study led to the largest binding enhancement ever reported for an enzyme inhibitor (up to 4700-fold on a valency-corrected basis), which represents a substantial advance over the multivalent glycosidase inhibitors previously reported. Electron microscopy imaging and analytical data support, for the best multivalent effects, the formation of a strong chelate complex in which two mannosidase molecules are cross-linked by one inhibitor.
Mots clés
Enzyme Inhibitors, chemistry, Glycoside Hydrolases, antagonists & inhibitors, Imino Sugars, chemistry, Ligands, Peptides, Cyclic, chemistry, alpha-Mannosidase, chemistry
Référence
Chemistry. 2016 Apr;22(15):5151-5
