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  • A new cell-based AI-2-mediated quorum sensing interference assay in screening of LsrK-targeted inhibitors [Elektronski vir]
    Gatta, Viviana ...
    Quorum sensing (QS), a bacterial communication strategy, has been recognized as one of the control mechanisms of virulence in bacteria. Thus, targeting QS offers an interesting opportunity to impair ... bacterial pathogenicity and develop antivirulence agents. Aiming to enhance the discovery of QS inhibitors, we developed a bioreporter E. coli JW5505 pET-Plsrlux and set up a cell-based assay for identifying inhibitors of autoinducer-2 (AI-2) -mediated QS. A comparative study on the performance of target-based and cell-based assay was performed. 91 compounds selected with the potential to target the ATP binding pocket of LsrK, a key enzyme in AI-2 processing, were tested in a LsrK inhibition assay providing 36 hits. The same set of compounds was tested by the AI-2-mediated QS interference assay resulting in 24 active compounds. Among those, 6 compounds were also active against LsrK whereas 18 may target other components of the pathway. Thus, the AI-2-mediated QS interference cell-based assay is an effective tool for complementing target-based assays but also as independent assay for primary screening.
    Vir: ChemBioChem. - ISSN 1439-7633 (Vol. 21, iss. 13, 2020, str. 1918-1922)
    Vrsta gradiva - e-članek
    Leto - 2020
    Jezik - angleški
    COBISS.SI-ID - 4879729