Are enzymes sensitive to the multivalent effect? Emerging evidence with glycosidases. Issue 49 (7th December 2016)

• Record Type: Journal Article
• Authors: Matassini, Camilla; Parmeggiani, Camilla; Cardona, Francesca; Goti, Andrea
• Is Part Of: Tetrahedron letters. Volume 57:Issue 49(2016)
• Page Start: 5407
• Page End: 5415
• Publication Date: 2016-12-07
• Subjects: Multivalency -- Glycosidases -- Inhibitors -- Iminosugars -- Synthesis; Chemistry, Organic -- Periodicals; 547.005
• DOI: 10.1016/j.tetlet.2016.10.080
• Languages: English
• ISSNs: 0040-4039

Abstract

Graphical abstract: Highlights: The concept of multivalency can be successfully applied to glycosidase inhibition. Special attention has been devoted to enzymes of therapeutic interest. A classification by glycosidic enzyme type is proposed. Structure/activity relationship of multivalent iminosugars is critically analyzed. Abstract: The multivalent effect in glycosidase inhibition is rapidly emerging as a hot topic of the research. In the last five years, several iminosugar-based inhibitors showed remarkable multivalent effects towards specific glycosidases, thus demonstrating that the concept of multivalency goes far beyond the interaction among protein receptors, as lectins, and carbohydrates and can be involved also for enzymes bearing a single active site. This critical overview aims to illustrate and discuss both cases of glycosidases prone to accept inhibitors with a multivalent presentation of the bioactive molecule as well as enzymes displaying a controversial behavior.