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Biosynthesis of the Antifungal Polyhydroxy-Polyketide Acrophialocinol

Carsten Wieder, Moritz Künzer, Rainer Wiechert, Kevin Seipp, Karsten Andresen, P. A. Stark, Anja Schüffler, Till Opatz, Eckhard Thines

2025Organic Letters10 citationsDOIOpen Access PDF

Abstract

High Resolution Image Download MS PowerPoint Slide Bioactivity-guided isolation identified the main antifungal compounds produced by Acrophialophora levis as the new polyhydroxy-polyketides acrophialocinol ( 1 ) and acrophialocin ( 2 ). Their biosynthesis was elucidated by heterologous reconstitution in Aspergillus oryzae and involves an α-ketoglutarate-dependent dioxygenase-catalyzed α-hydroxylation, resulting in the formation of a tertiary alcohol that is indispensable for antifungal activity. Furthermore, self-resistance toward the polyhydroxy-polyketides is mediated by a conserved RTA1-like protein encoded in the acr biosynthetic gene cluster.

Topics & Concepts

Gene clusterChemistryPolyketideBiosynthesisAntifungalAspergillus oryzaeHydroxylationStereochemistryHeterologousBiochemistryGeneEnzymeMicrobiologyBiologyMicrobial Natural Products and BiosynthesisPlant Pathogens and Fungal DiseasesFungal Biology and Applications