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  • Inhibition of nonessential bacterial targets : discovery of a novel serine O-acetyltransferase inhibitor
    Magalhães, Joana ...
    In [ypsilon]-proteobacteria and Actinomycetales, cysteine biosynthetic enzymes are indispensable during persistence and become dispensable during growth or acute infection. The biosynthetic machinery ... required to convert inorganic sulfur into cysteine is absent in mammals; therefore, it is a suitable drug target. We searched for inhibitors of Salmonella serine acetyltransferase (SAT), the enzyme that catalyzes the rate-limiting step of l-cysteine biosynthesis. The virtual screening of three ChemDiv focused libraries containing 91-243 compounds was performed to identify potential SAT inhibitors. Scaffold similarity and the analysis of the overall physicochemical properties allowed the selection of 73 compounds that were purchased and evaluated on the recombinant enzyme. Six compounds displaying an IC50 <100 [micro]M were identified via an indirect assay using Ellman's reagent and then tested on a Gram-negative model organism, with one of them being able to interfere with bacterial growth via SAT inhibition.
    Vir: ACS Medicinal Chemistry Letters. - ISSN 1948-5875 (Vol. 11, iss. 5, 2020, str. 790-797)
    Vrsta gradiva - članek, sestavni del ; neleposlovje za odrasle
    Leto - 2020
    Jezik - angleški
    COBISS.SI-ID - 80263939

    Povezava(-e):

    https://pubs.acs.org/doi/10.1021/acsmedchemlett.9b00627
    DOI

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