Low molecular weight inhibitors of the protease anthrax lethal factor.
Anthrax Lethal Factor (LF) is a zinc-dependent metalloprotease that together with the protective antigen constitute the anthrax lethal toxin, the most prominent virulence factor of the disease anthrax. This review summarizes the current knowledge on anthrax toxicity and defense in relation to LF. Particular emphasis is placed on the structural aspects of LF, the properties of its substrates and the achievements in the design of low molecular weight inhibitors of the catalytic activity of the metalloenzyme.
Dalkas
Georgios A
GA
Department of Pharmacy, University of Patras, Panepistimioupoli - Rion, GR-26504, Patras, Greece.
Papakyriakou
Athanasios
A
Vlamis-Gardikas
Alexios
A
Spyroulias
Georgios A
GA
D000818:Animals; D000942:Antigens, Bacterial / Q000737:chemistry / Q000378:metabolism; D001427:Bacterial Toxins / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000378:metabolism; D002614:Chelating Agents / Q000737:chemistry / Q000494:pharmacology; D004791:Enzyme Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D020929:Mitogen-Activated Protein Kinase Kinases / Q000378:metabolism; D008970:Molecular Weight; D013329:Structure-Activity Relationship
D000942:Antigens, Bacterial; D001427:Bacterial Toxins; D002614:Chelating Agents; D004791:Enzyme Inhibitors; C030325:anthrax toxin; D020929:Mitogen-Activated Protein Kinase Kinases