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• W4310702954 abstract "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." @default.
• W4310702954 created "2022-12-16" @default.
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• W4310702954 date "2022-11-29" @default.
• W4310702954 modified "2023-09-27" @default.
• W4310702954 title "Discovery of a fragment hit compound targeting D-Ala:D-Ala ligase of bacterial peptidoglycan biosynthesis" @default.
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• W4310702954 doi "https://doi.org/10.1080/14756366.2022.2149745" @default.
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