1zxv

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[[Image:1zxv.gif|left|200px]]
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{{STRUCTURE_1zxv| PDB=1zxv | SCENE= }}
{{STRUCTURE_1zxv| PDB=1zxv | SCENE= }}
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'''X-Ray Crystal Structure of the Anthrax Lethal Factor Bound to a Small Molecule Inhibitor, BI-MFM3, 3-{5-[5-(4-Chloro-phenyl)-furan-2-ylmethylene]-4-oxo-2-thioxo-thiazolidin-3-yl}-propionic acid.'''
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===X-Ray Crystal Structure of the Anthrax Lethal Factor Bound to a Small Molecule Inhibitor, BI-MFM3, 3-{5-[5-(4-Chloro-phenyl)-furan-2-ylmethylene]-4-oxo-2-thioxo-thiazolidin-3-yl}-propionic acid.===
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==Overview==
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Inhalation anthrax is a deadly disease for which there is currently no effective treatment. Bacillus anthracis lethal factor (LF) metalloproteinase is an integral component of the tripartite anthrax lethal toxin that is essential for the onset and progression of anthrax. We report here on a fragment-based approach that allowed us to develop inhibitors of LF. The small-molecule inhibitors we have designed, synthesized, and tested are highly potent and selective against LF in both in vitro tests and cell-based assays. These inhibitors do not affect the prototype human metalloproteinases that are structurally similar to LF. Initial in vivo evaluation of postexposure efficacy of our inhibitors combined with antibiotic ciprofloxacin against B. anthracis resulted in significant protection. Our data strongly indicate that the scaffold of inhibitors we have identified is the foundation for the development of novel, safe, and effective emergency therapy of postexposure inhalation anthrax.
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(as it appears on PubMed at http://www.pubmed.gov), where 15983377 is the PubMed ID number.
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{{ABSTRACT_PUBMED_15983377}}
==About this Structure==
==About this Structure==
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[[Category: Protein and small molecule inhibitor complex]]
[[Category: Protein and small molecule inhibitor complex]]
[[Category: Zinc metalloproteinase]]
[[Category: Zinc metalloproteinase]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 18:12:49 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 16:23:32 2008''

Revision as of 13:23, 28 July 2008

Image:1zxv.png

Template:STRUCTURE 1zxv

X-Ray Crystal Structure of the Anthrax Lethal Factor Bound to a Small Molecule Inhibitor, BI-MFM3, 3-{5-[5-(4-Chloro-phenyl)-furan-2-ylmethylene]-4-oxo-2-thioxo-thiazolidin-3-yl}-propionic acid.

Template:ABSTRACT PUBMED 15983377

About this Structure

1ZXV is a Single protein structure of sequence from Bacillus anthracis. Full crystallographic information is available from OCA.

Reference

Efficient synthetic inhibitors of anthrax lethal factor., Forino M, Johnson S, Wong TY, Rozanov DV, Savinov AY, Li W, Fattorusso R, Becattini B, Orry AJ, Jung D, Abagyan RA, Smith JW, Alibek K, Liddington RC, Strongin AY, Pellecchia M, Proc Natl Acad Sci U S A. 2005 Jul 5;102(27):9499-504. Epub 2005 Jun 27. PMID:15983377

Page seeded by OCA on Mon Jul 28 16:23:32 2008

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