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• W2003426535 abstract "Ilicicolin H is a polyketide-nonribosomal peptide synthase (NRPS)-natural product isolated from Gliocadium roseum, which exhibits potent and broad spectrum antifungal activity, with sub-μg/mL MICs against Candida spp., Aspergillus fumigatus, and Cryptococcus spp. It showed a novel mode of action, potent inhibition (IC50 = 2-3 ng/mL) of the mitochondrial cytochrome bc1 reductase, and over 1000-fold selectivity relative to rat liver cytochrome bc1 reductase. Ilicicolin H exhibited in vivo efficacy in murine models of Candida albicans and Cryptococcus neoformans infections, but efficacy may have been limited by high plasma protein binding. Systematic structural modification of ilicicolin H was undertaken to understand the structural requirement for the antifungal activity. The details of the biological activity of ilicicolin H and structural modification of some of the key parts of the molecule and resulting activity of the derivatives are discussed. These data suggest that the β-keto group is critical for the antifungal activity." @default.
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• W2003426535 date "2012-09-07" @default.
• W2003426535 modified "2023-09-30" @default.
• W2003426535 title "Antifungal Spectrum, In Vivo Efficacy, and Structure–Activity Relationship of Ilicicolin H" @default.
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• W2003426535 doi "https://doi.org/10.1021/ml300173e" @default.
• W2003426535 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/4025731" @default.
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