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Cross‐species discovery of syncretic drug combinations that potentiate the antifungal fluconazole

Authors: M. Spitzer; E. Griffiths; K. M. Blakely; J. Wildenhain; L. Ejim; L. Rossi; G. De Pascale; +4 Authors

Cross‐species discovery of syncretic drug combinations that potentiate the antifungal fluconazole

Abstract

Resistance to widely used fungistatic drugs, particularly to the ergosterol biosynthesis inhibitor fluconazole, threatens millions of immunocompromised patients susceptible to invasive fungal infections. The dense network structure of synthetic lethal genetic interactions in yeast suggests that combinatorial network inhibition may afford increased drug efficacy and specificity. We carried out systematic screens with a bioactive library enriched for off-patent drugs to identify compounds that potentiate fluconazole action in pathogenic Candida and Cryptococcus strains and the model yeast Saccharomyces. Many compounds exhibited species- or genus-specific synergism, and often improved fluconazole from fungistatic to fungicidal activity. Mode of action studies revealed two classes of synergistic compound, which either perturbed membrane permeability or inhibited sphingolipid biosynthesis. Synergistic drug interactions were rationalized by global genetic interaction networks and, notably, higher order drug combinations further potentiated the activity of fluconazole. Synergistic combinations were active against fluconazole-resistant clinical isolates and an in vivo model of Cryptococcus infection. The systematic repurposing of approved drugs against a spectrum of pathogens thus identifies network vulnerabilities that may be exploited to increase the activity and repertoire of antifungal agents.

Keywords

Medicine (General), Antifungal Agents, Insecta, QH301-705.5, /dk/atira/pure/subjectarea/asjc/2600/2604, Microbial Sensitivity Tests, Article, resistance, /dk/atira/pure/subjectarea/asjc/1300, Saccharomyces, R5-920, Species Specificity, Drug Resistance, Fungal, Immunology and Microbiology(all), synergism, Ergosterol, /dk/atira/pure/subjectarea/asjc/1100, /dk/atira/pure/subjectarea/asjc/1700/1710, Animals, Biology (General), Fluconazole, Candida, Medicine(all), combination, Agricultural and Biological Sciences(all), Biochemistry, Genetics and Molecular Biology(all), Applied Mathematics, Gene Expression Profiling, Computational Biology, Drug Synergism, /dk/atira/pure/subjectarea/asjc/2400, Cryptococcus, Computational Theory and Mathematics, /dk/atira/pure/subjectarea/asjc/1700/1703, /dk/atira/pure/subjectarea/asjc/2700, antifungal, Information Systems, pathogen

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    citations
    This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
    160
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    This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
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    influence
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    Top 10%
    impulse
    This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
    Top 1%
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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
160
Top 1%
Top 10%
Top 1%
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