title: Inhibitors of anthrax lethal factor.
abstract: An inhibitor of anthrax lethal toxin mediated cell death (1) was identified by a medium throughput cell-based screen. This compound was determined to specifically inhibit anthrax lethal factor (LF), and subsequent SAR studies produced an even more potent inhibitor (4). Mechanistic studies identified these agents as uncompetitive inhibitors of LF with Ki values of 3.0 and 1.7 microM, respectively, with good cell potency and low cytotoxicity.
authors.affiliation: Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
authors.forename: Brandon D
authors.initials: BD
authors.lastname: Gaddis
authors.forename: Larisa V
authors.initials: LV
authors.lastname: Avramova
authors.forename: Jean
authors.initials: J
authors.lastname: Chmielewski
mesh_terms: D000942:Antigens, Bacterial; D001427:Bacterial Toxins / Q000037:antagonists & inhibitors*; D004298:Dopamine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology; D008968:Molecular Conformation; D013329:Structure-Activity Relationship
chemical_list: D000942:Antigens, Bacterial; D001427:Bacterial Toxins; C030325:anthrax toxin; C488796:N-oleoyldopamine; D004298:Dopamine