ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans
Willmen Youngsaye,Cathy L Hartland,Barbara J. Morgan,Amal Ting,Partha P. Nag,Benjamin Vincent,Carrie A Mosher,Joshua A. Bittker,Sivaraman Dandapani,Michelle Palmer,Luke Whitesell,Susan Lindquist,Stuart L. Schreiber,Benito Munoz +13 more
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TLDR
The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates and initial investigation of structure–activity relationships led to the discovery of ML212.Abstract:
The National Institutes of Health Molecular Libraries and Probe Production Centers Network (NIH-MLPCN) screened >300,000 compounds to evaluate their ability to restore fluconazole susceptibility in resistant Candida albicans isolates. Additional counter screens were incorporated to remove substances inherently toxic to either mammalian or fungal cells. A substituted indazole possessing the desired bioactivity profile was selected for further development, and initial investigation of structure-activity relationships led to the discovery of ML212.read more
Citations
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Targeting efflux pumps to overcome antifungal drug resistance
Ann R. Holmes,Tony S. Cardno,J. Jacob Strouse,Irena Ivnitski-Steele,Mikhail V. Keniya,Kurt Lackovic,Brian C. Monk,Larry A. Sklar,Richard D. Cannon +8 more
TL;DR: Drug discovery targeting fungal efflux pumps could result in the development of azole-enhancing combination therapy, and a variety of medium- and high-throughput screens have been used to identify a number of chemical entities that inhibit fungalefflux pumps.
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Quercetin Sensitizes Fluconazole-Resistant Candida albicans To Induce Apoptotic Cell Death by Modulating Quorum Sensing
Bikarma Singh,Dalip K. Upreti,Braj Raj Singh,Garima Pandey,Shikhar Verma,Sudeep Roy,Asghar Naqvi,Aks Rawat +7 more
TL;DR: Results show that at much lower concentrations, quercetin (QC), a dietary flavonoid isolated from an edible lichen, can be implemented as a sensitizing agent for FCZ-resistant C. albicans NBC099, enhancing the efficacy of FCZ.
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Promising antifungal agents: A minireview.
TL;DR: This review discusses the various methodology of drug design, structure activity relationships (SARs), and mode of action of variety of new antifungal agents.
Journal ArticleDOI
Synergistic Effects and Mechanisms of Budesonide in Combination with Fluconazole against Resistant Candida albicans.
TL;DR: It is demonstrated, for the first time, that the combination of fluconazole and budesonide can reverse the resistance of Candida albicans by inhibiting the function of drug transporters, reducing the formation of biofilms, promoting apoptosis and inhibitors the activity of extracellular phospholipases.
Journal ArticleDOI
Antifungal effects of indolicidin-conjugated gold nanoparticles against fluconazole-resistant strains of Candida albicans isolated from patients with burn infection.
TL;DR: Investigation of anticandidal effects of indolicidin, as a representative of host defense peptide, conjugated with gold nanoparticles in fluconazole-resistant clinical isolates of C. albicans indicated that the nanocomplex was nontoxic for the fibroblast cells and erythrocytes.
References
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