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  • Discovery of a fragment hit compound targeting D-Ala [Elektronski vir] : D-Ala ligase of bacterial peptidoglycan biosynthesis
    Proj, Matic ...
    Bacterial resistance is an increasing threat to healthcare systems, highlighting the need for discovering new antibacterial agents. An established technique, fragment-based drug discovery, was used ... to target a bacterial enzyme Ddl involved in the biosynthesis of peptidoglycan. We assembled general and focused fragment libraries that were screened in a biochemical inhibition assay. Screening revealed a new fragment-hit inhibitor of DdlB with a Ki value of 20.7 ± 4.5 µM. Binding to the enzyme was confirmed by an orthogonal biophysical method, surface plasmon resonance, making the hit a promising starting point for fragment development.
    Source: Journal of enzyme inhibition and medicinal chemistry. - ISSN 1475-6374 (Vol. 38, iss. 1, 2023, str. 387-397)
    Type of material - e-article ; adult, serious
    Publish date - 2023
    Language - english
    COBISS.SI-ID - 132472579

    Link(s):

    https://www.tandfonline.com/doi/full/10.1080/14756366.2022.2149745
    Repository of the University of Ljubljana – RUL
    DOI

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