New catechol-containing chemical entities have been investigated as matrix metalloproteinase inhibitors as well as antioxidant molecules. The combination of the two properties could represent a useful feature due to the potential application in all the pathological processes characterized by increased proteolytic activity and radical oxygen species (ROS) production, such as inflammation and photoaging. A series of catechol-based molecules were synthesized and tested for both proteolytic and oxidative inhibitory activity, and the detailed binding mode was assessed by crystal structure determination of the complex between a catechol derivative and the matrix metalloproteinase-8. Surprisingly, X-ray structure reveals that the catechol oxygens do not coordinates the zinc atom.
Scheda prodotto non validato
Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo
|Titolo:||Catechol-based matrix metalloproteinase inhibitors with additional antioxidative activity|
|Data di pubblicazione:||2016|
|Citazione:||Catechol-based matrix metalloproteinase inhibitors with additional antioxidative activity / Tauro, Marilena; Laghezza, Antonio; Loiodice, Fulvio; Piemontese, Luca; Caradonna, Alessia; Capelli, Davide; Montanari, Roberta; Pochetti, Giorgio; Di Pizio, Antonella; Agamennone, Mariangela; Campestre, Cristina; Tortorella, Paolo. - In: JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY. - ISSN 1475-6366. - 31:S4(2016), pp. 25-37.|
|Appare nelle tipologie:||1.1 Articolo in rivista|