Antidotes to anthrax lethal factor intoxication. Part 1: Discovery of potent lethal factor inhibitors with in vivo efficacy.
Sub-nanomolar small molecule inhibitors of anthrax lethal factor have been identified using SAR and Merck L915 (4) as a model compound. One of these compounds (16) provided 100% protection in a rat lethal toxin model of anthrax disease.
Jiao
Guan-Sheng
GS
PanThera Biopharma, LLC, Aiea, HI 96701, USA.
Kim
Seongjin
S
Moayeri
Mahtab
M
Cregar-Hernandez
Lynne
L
McKasson
Linda
L
Margosiak
Stephen A
SA
Leppla
Stephen H
SH
Johnson
Alan T
AT
D000818:Animals; D000931:Antidotes / Q000737:chemistry / Q000494:pharmacology*; D000942:Antigens, Bacterial; D001427:Bacterial Toxins / Q000037:antagonists & inhibitors*; D051381:Rats; D013329:Structure-Activity Relationship
D000931:Antidotes; D000942:Antigens, Bacterial; D001427:Bacterial Toxins; C030325:anthrax toxin