Benzylic Dehydroxylation of Echinocandin Antifungal Drugs Restores Efficacy against Resistance Conferred by Mutated Glucan Synthase
Dana Logviniuk, Qais Z. Jaber, Roman Dobrovetsky, Noga Kozer, Ewa Księżopolska, Toni Gabaldón, Shmuel Carmeli, Micha Fridman
Abstract
2 genes of the parental strains, identified amino acids of the Fks proteins that are likely to reside in proximity to the l-homotyrosine residue of the bound drug. This study describes the first example of a chemical modification strategy to restore the efficacy of echinocandin drugs, which have a critical place in the arsenal of antifungal drugs, against resistant fungal pathogens.
Topics & Concepts
EchinocandinsEchinocandinAnidulafunginChemistryMicrobiologyGlucanAntifungal drugBiochemistryPharmacologyBiologyAntifungalCaspofunginAmphotericin BFluconazoleAntifungal resistance and susceptibilityPlant-Microbe Interactions and ImmunityFungal Biology and Applications