Recent advances in the discovery of zinc-binding motifs for the development of carbonic anhydrase inhibitors - Université de Montpellier Accéder directement au contenu
Article Dans Une Revue Journal of Enzyme Inhibition and Medicinal Chemistry Année : 2015

Recent advances in the discovery of zinc-binding motifs for the development of carbonic anhydrase inhibitors

Résumé

In addition to the sulfonamides and their isosteres, recently novel carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) which act by binding to the metal ion from the active site were discovered. Based on the X-ray crystal structure of the CA II-trithiocarbonate adduct, dithiocarbamates, xanthates and thioxanthates were shown to potently inhibit α- and β-CAs. The hydroxamates constitute another class of recently studied CAIs both against mammalian and protozoan enzymes. Another chemotype for which CA inhibitory properties were recently reported is the salicylaldoxime scaffold. X-ray crystal structures were reported for CA II complexed with dithiocarbamates and hydroxamates, whereas the xanthates and salicylaldoximes were investigated by kinetic measurements and docking studies. The dithiocarbamates and the xanthates showed potent antiglaucoma activity in animal models of the disease whereas some hydroxamates inhibited the growth of Trypanosoma cruzii probably by inhibiting the protozoan CA.

Domaines

Chimie
Fichier non déposé

Dates et versions

hal-03619503 , version 1 (25-03-2022)

Identifiants

Citer

Jean-Yves Winum, Claudiu Supuran. Recent advances in the discovery of zinc-binding motifs for the development of carbonic anhydrase inhibitors. Journal of Enzyme Inhibition and Medicinal Chemistry, 2015, 30 (2), pp.321-324. ⟨10.3109/14756366.2014.913587⟩. ⟨hal-03619503⟩
11 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More