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Title: Ligand-induced expansion of the S1' site in the anthrax toxin lethal factor

Abstract

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. 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.

Authors:
; ; ; ;
Publication Date:
Research Org.:
Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
Sponsoring Org.:
National Institutes of Health (NIH)
OSTI Identifier:
1237749
Resource Type:
Journal Article
Resource Relation:
Journal Name: FEBS Letters; Journal Volume: 589; Journal Issue: 24PartB
Country of Publication:
United States
Language:
ENGLISH
Subject:
59 BASIC BIOLOGICAL SCIENCES

Citation Formats

Maize, Kimberly M., Kurbanov, Elbek K., Johnson, Rodney L., Amin, Elizabeth Ambrose, and Finzel, Barry C.. Ligand-induced expansion of the S1' site in the anthrax toxin lethal factor. United States: N. p., 2016. Web. doi:10.1016/j.febslet.2015.11.005.
Maize, Kimberly M., Kurbanov, Elbek K., Johnson, Rodney L., Amin, Elizabeth Ambrose, & Finzel, Barry C.. Ligand-induced expansion of the S1' site in the anthrax toxin lethal factor. United States. doi:10.1016/j.febslet.2015.11.005.
Maize, Kimberly M., Kurbanov, Elbek K., Johnson, Rodney L., Amin, Elizabeth Ambrose, and Finzel, Barry C.. Tue . "Ligand-induced expansion of the S1' site in the anthrax toxin lethal factor". United States. doi:10.1016/j.febslet.2015.11.005.
@article{osti_1237749,
title = {Ligand-induced expansion of the S1' site in the anthrax toxin lethal factor},
author = {Maize, Kimberly M. and Kurbanov, Elbek K. and Johnson, Rodney L. and Amin, Elizabeth Ambrose and Finzel, Barry C.},
abstractNote = {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. 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.},
doi = {10.1016/j.febslet.2015.11.005},
journal = {FEBS Letters},
number = 24PartB,
volume = 589,
place = {United States},
year = {Tue Jul 05 00:00:00 EDT 2016},
month = {Tue Jul 05 00:00:00 EDT 2016}
}