Article

Projet
Protéines ABC, membranes et passage membranaire  
Ahcène BOUMENDJEL,   
Titre
Modulators of the Efflux Pump Cdr1p of Candida albicans: Mechanisms of Action and Chemical Features.  
[Full paper ]
Auteurs
V. K. Tran-Nguyen, R. Prasad, P. Falson, A. Boumendjel
Edition
Curr. Med. Chem. 2017, 24, 3242-3253.
Année
2017
Résumé
The multicomponent primary active ATP-binding cassette transporter Cdr1p in the structure of the pathogenic yeast Candida albicans is among the culprits of antifungal agent resistance reported in recent decades. So far, various potential novel inhibitors/ modulators of this protein have been purified, synthesized, and biologically tested, with results showing their ability to effectively reverse CaCdr1p-mediated drug resistance phenomenon. These compounds are of diverse origins, possess non-identical structural features and adopt different mechanisms of action. In this article, six possible mechanisms with which a molecule can manifest their activity against the efflux pump are described, and a list of nearly 50 CaCdr1p modulators found in literatures along with their respective mechanism(s) (if already identified) is provided, summarizing the results obtained so far in the search of new inhibitors of the drug extrusion transporter that can enhance the potency of commonly used antifungal agents.