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| Content Provider | World Health Organization (WHO)-Global Index Medicus |
|---|---|
| Author | Cousido-siah, Alexandra Izzo, Irene Tarnus, Céline Birck, Catherine Francois, Yannis-nicolas Schmitt, Marjorie Compain, Philippe Nguyen-huynh, Nha-thi Podjarny, Alberto Bodlenner, Anne Lepage, Mathieu L. Leize-wagner, Emmanuelle Schneider, Jérémy P. Meli, Alessandra De Riccardis, Francesco |
| Description | Author Affiliation: Lepage ML ( Laboratoire de Synthèse Organique et Molécules Bioactives Université de Strasbourg et CNRS (UMR 7509), Ecole Européenne de Chimie, Polymères et Matériaux, 25 rue Becquerel, 67087, Strasbourg, France.); Schneider JP ( Laboratoire de Synthèse Organique et Molécules Bioactives Université de Strasbourg et CNRS (UMR 7509), Ecole Européenne de Chimie, Polymères et Matériaux, 25 rue Becquerel, 67087, Strasbourg, France.); Bodlenner A ( Laboratoire de Synthèse Organique et Molécules Bioactives Université de Strasbourg et CNRS (UMR 7509), Ecole Européenne de Chimie, Polymères et Matériaux, 25 rue Becquerel, 67087, Strasbourg, France.); Meli A ( Department of Chemistry and Biology, University of Salerno, Via Giovanni Paolo II,132, 84084, Fisciano, Salerno, Italy.); De Riccardis F ( Department of Chemistry and Biology, University of Salerno, Via Giovanni Paolo II,132, 84084, Fisciano, Salerno, Italy.); Schmitt M ( Université de Haute Alsace, Laboratoire de Chimie Organique et Bioorganique (EA4466), ENSCMu, 3, rue Alfred Werner, 68093, Mulhouse Cedex, France.); Tarnus C ( Université de Haute Alsace, Laboratoire de Chimie Organique et Bioorganique (EA4466), ENSCMu, 3, rue Alfred Werner, 68093, Mulhouse Cedex, France.); Nguyen-Huynh NT ( Laboratoire de Spectrométrie de Masse des Interactions et des Systèmes, UMR CNRS 7140, Université de Strasbourg, 67008, Strasbourg, France.); Francois YN ( Laboratoire de Spectrométrie de Masse des Interactions et des Systèmes, UMR CNRS 7140, Université de Strasbourg, 67008, Strasbourg, France.); Leize-Wagner E ( Laboratoire de Spectrométrie de Masse des Interactions et des Systèmes, UMR CNRS 7140, Université de Strasbourg, 67008, Strasbourg, France.); Birck C ( Structural Biology Platform, CBI-IGBMC, 1 rue Laurent Fries, 67404, Illkirch, France.); Cousido-Siah A ( Department of Integrative Biology, Institut de Génétique et de Biologie Moléculaire et Cellulaire, CNRS, INSERM, UdS, 1 rue Laurent Fries, 67404, Illkirch CEDEX, France.); Podjarny A ( Department of Integrative Biology, Institut de Génétique et de Biologie Moléculaire et Cellulaire, CNRS, INSERM, UdS, 1 rue Laurent Fries, 67404, Illkirch CEDEX, France.); Izzo I ( Department of Chemistry and Biology, University of Salerno, Via Giovanni Paolo II,132, 84084, Fisciano, Salerno, Italy.); Compain P ( Laboratoire de Synthèse Organique et Molécules Bioactives Université de Strasbourg et CNRS (UMR 7509), Ecole Européenne de Chimie, Polymères et Matériaux, 25 rue Becquerel, 67087, Strasbourg, France. philippe.compain@unistra.fr.) |
| Abstract | 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. |
| ISSN | 09476539 |
| e-ISSN | 15213765 |
| Journal | Chemistry - A European Journal |
| Issue Number | 15 |
| Volume Number | 22 |
| Language | English |
| Publisher | Wiley-VCH;ChemPubSoc Europe |
| Publisher Date | 2016-04-04 |
| Publisher Place | Germany |
| Access Restriction | Open |
| Subject Keyword | Enzyme Inhibitors Chemistry Glycoside Hydrolases Antagonists & Inhibitors Imino Sugars Peptides, Cyclic Alpha-Mannosidase Pharmacology Ligands Research Support, Non-U.S. Gov't |
| Content Type | Text |
| Resource Type | Article |
| Subject | Organic Chemistry Catalysis |
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