Are enzymes sensitive to the multivalent effect? Emerging evidence with glycosidases

Year: 2016

Authors: Matassini C., Parmeggiani C., Cardona F., Goti A.

Autors Affiliation: Univ Florence, Dipartimento Chim Ugo Schiff, Via Lastruccia 3-13, I-50019 Sesto Fiorentino, Italy; UOS Sesto Fiorentino, CNR INO, Via Nello Carrara 1, I-50019 Sesto Fiorentino, Italy; LENS, Via Nello Carrara 1, I-50019 Sesto Fiorentino, Italy.

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. (C) 2016 Elsevier Ltd. All rights reserved.

Journal/Review: TETRAHEDRON LETTERS

Volume: 57 (49)      Pages from: 5407  to: 5415

More Information: The Italian Ministry of Health (grant Ricerca Finalizzata RF-2011-02347694) and MIUR-Italy (PRIN 2010-2011, 2010L9SH3K 006) are gratefully acknowledged for financial support. Ente Cassa di Risparmio di Firenze is acknowledged for a fellowship to CM (grant No 2013/0366). CP also thanks the European Research Council (ERC Grant agreement 291349).
KeyWords: Multivalency; Glycosidases; Inhibitors; Iminosugars; Synthesis
DOI: 10.1016/j.tetlet.2016.10.080

Citations: 50
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