title: Ebselen as a potent covalent inhibitor of New Delhi metallo-β-lactamase (NDM-1).
abstract: We report the discovery of a promising NDM-1 inhibitor, ebselen, through a cell-based screening approach. Enzymatic kinetic study and ESI-MS analysis suggested that ebselen could bind to NDM-1 by forming a S-Se bond with the Cys(221) residue at the active site, thereby exhibiting a new inhibition mechanism with broad spectrum inhibitory potential.
authors.affiliation: Shenzhen Key Laboratory for Food Biological Safety Control, Food Safety and Technology Research Centre, The Hong Kong Polytechnic University, Shenzhen Research Institute, Shenzhen, P.R. China. sheng.chen@polyu.edu.hk.
authors.forename: Jiachi
authors.initials: J
authors.lastname: Chiou
authors.forename: Shengbiao
authors.initials: S
authors.lastname: Wan
authors.forename: Kin-Fai
authors.initials: KF
authors.lastname: Chan
authors.forename: Pui-Kin
authors.initials: PK
authors.lastname: So
authors.forename: Dandan
authors.initials: D
authors.lastname: He
authors.forename: Edward Wai-chi
authors.initials: EW
authors.lastname: Chan
authors.forename: Tak-hang
authors.initials: TH
authors.lastname: Chan
authors.forename: Kwok-yin
authors.initials: KY
authors.lastname: Wong
authors.forename: Jiang
authors.initials: J
authors.lastname: Tao
authors.forename: Sheng
authors.initials: S
authors.lastname: Chen
mesh_terms: D000667:Ampicillin / Q000494:pharmacology; D000900:Anti-Bacterial Agents / Q000494:pharmacology; D001393:Azoles / Q000494:pharmacology*; D004926:Escherichia coli / Q000187:drug effects / Q000235:genetics / Q000378:metabolism; D054833:Isoindoles; D000077731:Meropenem; D008826:Microbial Sensitivity Tests; D016566:Organoselenium Compounds / Q000494:pharmacology*; D013845:Thienamycins / Q000494:pharmacology; D065093:beta-Lactamase Inhibitors / Q000494:pharmacology*; D001618:beta-Lactamases / Q000235:genetics / Q000378:metabolism*
chemical_list: D000900:Anti-Bacterial Agents; D001393:Azoles; D054833:Isoindoles; D016566:Organoselenium Compounds; D013845:Thienamycins; D065093:beta-Lactamase Inhibitors; C042986:ebselen; D000667:Ampicillin; D001618:beta-Lactamases; C552864:beta-lactamase NDM-1; D000077731:Meropenem