Ligand-induced expansion of the S1' site in the anthrax toxin lethal factor
- Univ. of Minnesota, Minneapolis, MN (United States)
The Bacillus anthracis lethal factor (LF) is one component of a tripartite exotoxin partly responsible for persistent anthrax cytotoxicity after initial bacterial infection. Inhibitors of the zinc metalloproteinase have been investigated as potential therapeutic agents, but LF is a challenging target because inhibitors lack sufficient selectivity or possess poor pharmaceutical properties. Furthermore, these structural studies reveal an alternate conformation of the enzyme, induced upon binding of specific inhibitors, that opens a previously unobserved deep pocket termed S1'* which might afford new opportunities to design selective inhibitors that target this subsite.
- Research Organization:
- Argonne National Laboratory (ANL), Argonne, IL (United States)
- Sponsoring Organization:
- National Institutes of Health (NIH)
- Grant/Contract Number:
- R01 AI083234
- OSTI ID:
- 1237749
- Journal Information:
- FEBS Letters, Vol. 589, Issue 24PartB; ISSN 0014-5793
- Publisher:
- Federation of European Biochemical SocietiesCopyright Statement
- Country of Publication:
- United States
- Language:
- ENGLISH
Cited by: 4 works
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