ArticleAntimicrobial agents and chemotherapy2015
Structural Insights into Binding of the Antifungal Drug Fluconazole to Saccharomyces cerevisiae Lanosterol 14α-Demethylase.
Article in Antimicrobial agents and chemotherapy, 2015. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 115 papers.
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115 citing papers in PubMed, 198 citations in OpenAlex.
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- Protease-Mediated Dual Action Against Rice Blast: Suppression of Magnaporthe oryzae Ergosterol Biosynthesis Pathway and Enhancement of Rice Disease Resistance by Bacillus amyloliquefaciens SN16-1.Plant, cell & environment · 2026Article
- Click Chemistry Approach to Derivatisation of Fluconazole.Molecules (Basel, Switzerland) · 2026Article
- Prochelators modulate azole activity againstRSC chemical biology · 2026Article
- Variable ectopic heterochromatin islands provide an alternative route to antifungal heteroresistance inbioRxiv : the preprint server for biology · 2026Article
- Candicidal Effect of a Nanoemulsion Based on the Essential Oil of the Medicinal PlantPharmaceuticals (Basel, Switzerland) · 2026Article
- The dual role of azoles: lifesaving antifungals and drivers of resistance - a One Health perspective.Nature communications · 2026Review
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- The molecular basis of intrinsic resistance to azoles inAntimicrobial agents and chemotherapy · 2026Article
- Discovery of a Caffeic Acid Thioamide with Potent Activity against Pathogenic Fungi and Fluconazole Tolerance-Eliminating Effects inDrug design, development and therapy · 2026Article
- Novel molecular targets and natural drug candidates for the antifungal therapy of seborrheic dermatitis.Frontiers in cellular and infection microbiology · 2026Review
- In Silico Evaluation of Acalypha indica Phytochemicals as Potential Antifungal Agents Targeting Saccharomyces cerevisiae Lanosterol 14-Alpha Demethylase.Cell biochemistry and biophysics · 2025Article
- Multidrug efflux pumps and innate azole resistance of Mucor lusitanicus.The Journal of antimicrobial chemotherapy · 2025Article
- Antimicrobial and Antibiofilm Activities of Some Antioxidant 3,4-Dihydroxyphenyl-Thiazole-Coumarin Hybrid Compounds: In Silico and In Vitro Evaluation.Antibiotics (Basel, Switzerland) · 2025Article
- Effects of novel organoantimony compounds on the fungal pathogenJournal of medical microbiology · 2025Article
- Impairing the interaction between Erg11 and cytochrome P450 reductase Ncp1 enhances azoles' antifungal activities.Nature communications · 2025Article
55 more citing papers are in PubMed but not listed here.
Corrections and comments
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Authors and funding
5 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Infections by fungal pathogens such as Candida albicans and Aspergillus fumigatus and their resistance to triazole drugs are major concerns. Fungal lanosterol 14α-demethylase belongs to the CYP51 class in the cytochrome P450 superfamily of enzymes. This monospanning bitopic membrane protein is involved in ergosterol biosynthesis and is the primary target of azole antifungal drugs, including fluconazole. The lack of high-resolution structural information for this drug target from fungal pathogens has been a limiting factor for the design of modified triazole drugs that will overcome resistance. Here we report the X-ray structure of full-length Saccharomyces cerevisiae lanosterol 14α-demethylase in complex with fluconazole at a resolution of 2.05 Å. This structure shows the key interactions involved in fluconazole binding and provides insight into resistance mechanisms by revealing a water-mediated hydrogen bonding network between the drug and tyrosine 140, a residue frequently found mutated to histidine or phenylalanine in resistant clinical isolates.
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