Literature summary for 3.4.24.83 extracted from

Moayeri, M.; Crown, D.; Jiao, G.; Kim, S.; Johnson, A.; Leysath, C.; Leppla, S.
Small-molecule inhibitors of lethal factor protease activity protect against anthrax infection (2013), Antimicrob. Agents Chemother., 57, 4139-4145.

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Application

Application	Comment	Organism
medicine	administration of lethal factor proteases early in the infection inhibits dissemination of vegetative bacteria to the organs in the first 32 h following infection. Neutralizing antibodies against edema factor also inhibit bacterial dissemination with similar efficacy	Bacillus anthracis

Inhibitors

Inhibitors	Comment	Organism	Structure
(2S)-6-[(1R)-N-1-(4-fluorophenyl)propan]aminoamino-2-(4-fluoro-3,5-dimethylbenzyl)-N-hydroxyhexanamide	inhibitor provides protection against lethal infection when administered as a monotherapy. Two doses (10 mg/kg) administered at 2 h and 8 h after spore infection are sufficient to provide a significant survival benefit in infected mice	Bacillus anthracis
(2S)-6-[N-1-(4-fluorophenyl)propan]amino-2-[(2R)-2-(4-fluorophenyl)-2-methoxyethyl]-N-hydroxyhexanamide	inhibitor provides protection against lethal infection when administered as a monotherapy. Two doses (10 mg/kg) administered at 2 h and 8 h after spore infection are sufficient to provide a significant survival benefit in infected mice	Bacillus anthracis

Organism

Organism	UniProt	Comment	Textmining
Bacillus anthracis	P15917	-	-

Ki Value [mM]

Ki Value [mM]	Ki Value maximum [mM]	Inhibitor	Comment	Organism	Structure
0.000000042	-	(2S)-6-[(1R)-N-1-(4-fluorophenyl)propan]aminoamino-2-(4-fluoro-3,5-dimethylbenzyl)-N-hydroxyhexanamide	pH not specified in the publication, temperature not specified in the publication	Bacillus anthracis
0.00000033	-	(2S)-6-[N-1-(4-fluorophenyl)propan]amino-2-[(2R)-2-(4-fluorophenyl)-2-methoxyethyl]-N-hydroxyhexanamide	pH not specified in the publication, temperature not specified in the publication	Bacillus anthracis

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Release 2023.1 (January 2023)