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- W4311302216 abstract "New Delhi metallo-β-lactamase 1 (NDM-1) can hydrolyze most β-lactam antibiotics, which is the major factor for drug resistance of Gram-negative bacteria. The binding of most reversible inhibitors to NDM-1 is relatively weak due to the shallow active pocket of NDM-1. Alternatively, irreversible covalent inhibitors can prevent their dissociation from the target, leading to permanent inactivation of the protein. Herein, we report a series of irreversible covalent inhibitors of NDM-1 targeting the conserved Lys211 in the active pocket. Several methods, including mass spectrometry, sodium dodecyl sulfate-polyacrylamide gel electrophoresis, fluorescent labeling, and coumarin probe were used to demonstrate that pentafluorophenyl ester formed a covalent bond with Lys211. Moreover, our target inhibitor, in combination with meropenem, achieved an antibacterial effect on drug-resistant bacteria, along with an excellent safety profile. Our new strategy in designing lysine-targeted irreversible covalent NDM-1 inhibitors provides a potential option for the clinical treatment of Gram-negative bacteria." @default.
- W4311302216 created "2022-12-25" @default.
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- W4311302216 date "2023-07-01" @default.
- W4311302216 modified "2023-09-27" @default.
- W4311302216 title "Strategic design of lysine-targeted irreversible covalent NDM-1 inhibitors" @default.
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- W4311302216 doi "https://doi.org/10.1016/j.cclet.2022.108072" @default.
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