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- W3204802982 abstract "The aromatic polyketide tetracenomycin X (TcmX) was recently found to be a potent inhibitor of protein synthesis, whose binding site is located in a unique locus within the tunnel of the large ribosomal subunit. The distinct mode of action makes this relatively narrow class of macrolides promising for drug development, in our quest to prevent the spread of drug resistant pathogens. Here we report the isolation and structure elucidation of novel natural tetracenomycin X congener – 6-hydroxytetraceonomycin X (6-OH-TcmX). In contrast to TcmX, 6-OH-TcmX exhibited lower antimicrobial and cytotoxic activity, but comparable in vitro protein synthesis inhibition ability. A survey on spectral properties of tetracenomycins showed profound differences in both UV-absorption and fluorescence spectra of TcmX and 6-OH-TcmX, suggesting the significant influence of 6-hydroxylation on tetracenomycin chromophore. Nonetheless, characteristic spectral properties of tetracenomycins make them suitable candidates as a foundation for semi-synthetic drug development (e.g., for targeted delivery, theranostics or cell imaging)." @default.
- W3204802982 created "2021-10-11" @default.
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- W3204802982 date "2021-07-28" @default.
- W3204802982 modified "2023-09-24" @default.
- W3204802982 title "Biological evaluation and spectral characterization of novel tetracenomycin X congener" @default.
- W3204802982 doi "https://doi.org/10.33774/chemrxiv-2021-b9vg4" @default.
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