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Humanized Candida and NanoBiT Assays Expedite Discovery of Bdf1 Bromodomain Inhibitors With Antifungal Potential.
Adv Sci (Weinh)
January 2025
Univ. Grenoble Alpes, Inserm, CNRS, Institute for Advanced Biosciences (IAB), Grenoble, 38000, France.
The fungal Bromodomain and Extra-Terminal (BET) protein Bdf1 is a potential antifungal target against invasive fungal infections. However, the need to selectively inhibit both Bdf1 bromodomains (BDs) over human orthologs and the lack of molecular tools to assess on-target antifungal efficacy hamper efforts to develop Bdf1 BD inhibitors as antifungal therapeutics. This study reports a phenyltriazine compound that inhibits both Bdf1 BDs from the human fungal pathogen Candida glabrata with selectivity over the orthologous BDs from the human BET protein Brd4.
View Article and Find Full Text PDFSynthesis, characterization and biological profile of some new dihydropyrimidinone derivaties.
Heliyon
January 2025
Department of Pharmaceutical Chemistry, Riphah Institute of Pharmaceutical Sciences, Riphah International University, Islamabad, Pakistan, 44000.
Objective: The rise of drug-resistant bacteria, viruses, and fungi has prompted the search for new drugs without cross-resistance to current treatments. As a result, the aim of this research was to synthesize various types of dihydropyrimidinones heterocyclic compounds and screened them for their antibiotic properties.
Methodology: Newly synthesized dihydropyrimidinone derivatives were characterized spectroscopically using proton NMR (HNMR), and FT-IR.
Background: Candidiasis can be present as a cutaneous, mucosal, or deep-seated organ infection, which is caused by more than 20 types of Candida spp., with C. albicans being the most common.
View Article and Find Full Text PDFA Novel and Robust Method for Investigating Fungal Biofilm.
Bio Protoc
January 2025
Laboratory of Protein Translation and Fungal Pathogenesis, Regional Centre for Biotechnology, Faridabad, India.
, labeled an urgent threat by the CDC, shows significant resilience to treatments and disinfectants via biofilm formation, complicating treatment/disease management. The inconsistencies in biofilm architecture observed across studies hinder the understanding of its role in pathogenesis. Our novel in vitro technique cultivates biofilms on gelatin-coated coverslips, reliably producing multilayer biofilms with extracellular polymeric substances (EPS).
View Article and Find Full Text PDFEvaluation of antifungal effect of amphotericin B in comparison with nystatin on Candida species derived from patients undergoing head-and-neck radiotherapy.
Dent Res J (Isfahan)
December 2024
Department of Endodontics, Kashan University of Medical Sciences, Kashan, Iran.
Background: There is ample evidence showing the development of nystatin-resistant strains in patients undergoing malignancy treatment. Amphotericin B is a polyene antifungal drug that combines with ergosterol to cause cell death and is more effective on fungal species than routine antifungals such as nystatin. This study aimed to compare the effect of nystatin and amphotericin B on fungal species isolated from patients before and during head-and-neck radiotherapy.
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