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  • Evaluation of the published kinase inhibitor set to identify multiple inhibitors of bacterial ATP-dependent mur ligases
    Hrast, Martina ...
    The Mur ligases form a series of consecutive enzymes that participate in the intracellular steps of bacterial peptidoglycan biosynthesis. They therefore represent interesting targets for ... antibacterial drug discovery. MurC, D, E and F are all ATP-dependent ligases. Accordingly, with the aim being to find multiple inhibitors of these enzymes, we screened a collection of ATP-competitive kinase inhibitors, on Escherichia coli MurC, D and F, and identified five promising scaffolds that inhibited at least two of these ligases. Compounds 1, 2, 4 and 5 are multiple inhibitors of the whole MurC to MurF cascade that act in the micromolar range (IC50, 32 - 368 microM). NMR-assisted binding studies and steady-state kinetics studies performed on aza-stilbene derivative 1 showed, surprisingly, that it acts as a competitive inhibitor of MurD activity towards D-glutamic acid, and additionally, that its binding to the D-glutamic acid binding site is independent of the enzyme closure promoted by ATP.
    Vir: Journal of enzyme inhibition and medicinal chemistry. - ISSN 1475-6366 (Vol. 34, iss. 1, 2019, str. 1010-1017)
    Vrsta gradiva - članek, sestavni del
    Leto - 2019
    Jezik - angleški
    COBISS.SI-ID - 4715633

    Povezava(-e):

    https://www.tandfonline.com/doi/full/10.1080/14756366.2019.1608981
    DOI

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