Media and strain studies for the scaled production of cis-enone resorcylic acid lactones as feedstocks for semisynthesis.

ABSTRACT: Resorcylic acid lactones (RALs) with a cis-enone moiety, represented by hypothemycin (1) and (5Z)-7-oxozeaenol (2), are fungal secondary metabolites with irreversible inhibitory activity against protein kinases, with particularly selective activity for inhibition of TAK1 (transforming growth factor beta-activated kinase 1). Gram-scale quantities of these compounds were needed as feedstock for semi-synthesizing RAL-analogues in a step-economical fashion. To do so, this study had three primary goals: identifying fungi that biosynthesized 1 and 2, enhancing their production by optimizing the fermentation conditions on the lab scale, and developing straight forward purification processes. After evaluating 536 fungal extracts via an in-house dereplication protocol, three strains were identified

SUBMITTER: Al Subeh ZY 

PROVIDER: S-EPMC8313427 | biostudies-literature | 2021 Aug

REPOSITORIES: biostudies-literature