Inhibitors of anthrax lethal factor.
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.
Gaddis
Brandon D
BD
Department of Chemistry, Purdue University, West Lafayette, IN 47907, USA.
Avramova
Larisa V
LV
Chmielewski
Jean
J
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
D000942:Antigens, Bacterial; D001427:Bacterial Toxins; C030325:anthrax toxin; C488796:N-oleoyldopamine; D004298:Dopamine