ArticleNature communications2017
Selective BET bromodomain inhibition as an antifungal therapeutic strategy.
Article in Nature communications, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 22 papers.
What it found
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The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
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Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
22 citing papers in PubMed, 46 citations in OpenAlex.
- Dual-Targeting, Hybrid Antifungal Agents Targeting Candida albicans-An Overview.Chemical biology & drug design · 2026Review
- Epoxy tetrahydrophthalimides as potential bioactive agents: synthesis and computational study.Pest management science · 2025Article
- Is a Fungal Apocalypse Inevitable or Just a Hallucination? An Overview of the Antifungal Armamentarium Used in the Fight against Pathogenic Fungi.ACS medicinal chemistry letters · 2025Review
- Humanized Candida and NanoBiT Assays Expedite Discovery of Bdf1 Bromodomain Inhibitors With Antifungal Potential.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Fungal diversity in the soil Mycobiome: Implications for ONE health.One health (Amsterdam, Netherlands) · 2024Review
- The C-terminal protein interaction domain of the chromatin reader Yaf9 is critical for pathogenesis ofmSphere · 2024Article
- Synthesis of the 1,5-Benzothiazepane Scaffold - Established Methods and New Developments.ChemistryOpen · 2023Review
- Toward more potent imidazopyridine inhibitors of Candida albicans Bdf1: Modeling the role of structural waters in selective ligand binding.Journal of computational chemistry · 2022Article
- The Role of Glycoside Hydrolases in S. gordonii and C. albicans Interactions.Applied and environmental microbiology · 2022Article
- Inhibition of bromodomain extraterminal histone readers alleviates skin fibrosis in experimental models of scleroderma.JCI insight · 2022Article
- Article
- The BET family in immunity and disease.Signal transduction and targeted therapy · 2021Review
- The Roles of Chromatin Accessibility in Regulating theJournal of fungi (Basel, Switzerland) · 2021Review
- Article
- The RSC (Remodels the Structure of Chromatin) complex of Candida albicans shows compositional divergence with distinct roles in regulating pathogenic traits.PLoS genetics · 2020Article
- The Groebke-Blackburn-Bienaymé Reaction.European journal of chemistry (Print) · 2019Article
- Bromodomain inhibitor I-BET151 suppresses immune responses during fungal-immune interaction.European journal of immunology · 2019Article
- Bromodomains: a new target class for drug development.Nature reviews. Drug discovery · 2019Review
- Screening and Antifungal Activity of aInternational journal of microbiology · 2019Article
- Potential targets for the development of new antifungal drugs.The Journal of antibiotics · 2018Review
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Authors and funding
18 authors at 5 institutions in 2 countries.
Funding
Abstract
Invasive fungal infections cause significant morbidity and mortality among immunocompromised individuals, posing an urgent need for new antifungal therapeutic strategies. Here we investigate a chromatin-interacting module, the bromodomain (BD) from the BET family of proteins, as a potential antifungal target in Candida albicans, a major human fungal pathogen. We show that the BET protein Bdf1 is essential in C. albicans and that mutations inactivating its two BDs result in a loss of viability in vitro and decreased virulence in mice. We report small-molecule compounds that inhibit C. albicans Bdf1 with high selectivity over human BDs. Crystal structures of the Bdf1 BDs reveal binding modes for these inhibitors that are sterically incompatible with the human BET-binding pockets. Furthermore, we report a dibenzothiazepinone compound that phenocopies the effects of a Bdf1 BD-inactivating mutation on C. albicans viability. These findings establish BET inhibition as a promising antifungal therapeutic strategy and identify Bdf1 as an antifungal drug target that can be selectively inhibited without antagonizing human BET function.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.