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- W4386985403 abstract "Targeting the early steps of the cell wall peptidoglycan biosynthesis by small molecules might lead to new bactericidal antibiotics. MurA catalyzes the first committed step in this highly conserved pathway and was validated as a target by the clinically used inhibitor fosfomycin. However, fosfomycin relies on irreversible binding to the catalytic cysteine residue in the MurA active site, which can be mutated to cause bacterial resistance against this drug. Since the early 2000s, research efforts were intensified to develop new inhibitors of MurA species. Numerous synthetic and natural compounds were identified by high-throughput wet screening of large chemical libraries or by in silico screening approaches. This review provides an overview of the currently known MurA inhibitors, the methods employed for hit finding, the mode of action and their antibacterial activity." @default.
- W4386985403 created "2023-09-24" @default.
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- W4386985403 date "2023-01-01" @default.
- W4386985403 modified "2023-10-18" @default.
- W4386985403 title "Inhibitors of the bacterial enzyme MurA as potential novel antibiotics" @default.
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- W4386985403 doi "https://doi.org/10.1016/bs.armc.2023.09.002" @default.
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