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Enzymatic glycosylation and amidation reshapes polyene bioactivity
Saadia N Mirza1,2, Alberto Carella2, Joseph W Thompson1,2
1Department of Chemistry, Molecular Sciences Research Hub, Imperial College, London, UK.
Nature
|July 29, 2026
Summary
Researchers discovered new antifungal polyenes through fermentation and enzymatic routes. These novel compounds exhibit enhanced potency and reduced toxicity, addressing limitations of current treatments.
Area of Science:
- Biochemistry
- Natural Product Chemistry
- Antimicrobial Research
Background:
- Fungal infections pose a growing global health risk due to increasing antimicrobial resistance and a shortage of effective antifungal drugs.
- Polyenes are broad-spectrum antifungal agents, but their clinical application is hindered by significant toxicity and poor solubility.
- Existing methods for developing improved polyenes are often inefficient and costly.
Purpose of the Study:
- To discover and characterize novel polyene natural products with improved antifungal properties.
- To explore enzymatic modifications of polyene scaffolds for enhanced efficacy and safety.
- To develop sustainable and efficient production methods for new antifungal agents.
Main Methods:
- Discovery and characterization of biosynthetic pathways for novel polyenes.
- Utilizing glycosyltransferase enzymes to introduce sugar moieties onto polyene structures.
- Expanding the substrate scope of amidotransferase enzymes for polyene functionalization.
- Fermentation and enzymatic synthesis for producing modified polyenes.
Main Results:
- Identification of previously undescribed polyenes with unique structural features.
- Demonstration of enzymatic glycosylation and carboxylate modification of polyenes.
- Development of polyene derivatives with significantly increased antifungal potency.
- Reduced toxicity observed in the novel, modified polyene antifungals.
- Successful production of enhanced polyenes via fermentation and enzymatic processes.
Conclusions:
- Novel polyene antifungals with improved potency and safety profiles have been discovered.
- Enzymatic and fermentation-based strategies offer efficient and sustainable routes to these next-generation antifungal agents.
- These findings provide a promising avenue for addressing the urgent need for new treatments against fungal diseases.
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