1pwq

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{{STRUCTURE_1pwq| PDB=1pwq | SCENE= }}
{{STRUCTURE_1pwq| PDB=1pwq | SCENE= }}
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'''Crystal structure of Anthrax Lethal Factor complexed with Thioacetyl-Tyr-Pro-Met-Amide, a metal-chelating peptidyl small molecule inhibitor'''
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===Crystal structure of Anthrax Lethal Factor complexed with Thioacetyl-Tyr-Pro-Met-Amide, a metal-chelating peptidyl small molecule inhibitor===
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==Overview==
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Recent events have created an urgent need for new therapeutic strategies to treat anthrax. We have applied a mixture-based peptide library approach to rapidly determine the optimal peptide substrate for the anthrax lethal factor (LF), a metalloproteinase with an important role in the pathogenesis of the disease. Using this approach we have identified peptide analogs that inhibit the enzyme in vitro and that protect cultured macrophages from LF-mediated cytolysis. The crystal structures of LF bound to an optimized peptide substrate and to peptide-based inhibitors provide a rationale for the observed selectivity and may be exploited in the design of future generations of LF inhibitors.
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(as it appears on PubMed at http://www.pubmed.gov), where 14718924 is the PubMed ID number.
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{{ABSTRACT_PUBMED_14718924}}
==About this Structure==
==About this Structure==
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[[Category: Metal-chelator]]
[[Category: Metal-chelator]]
[[Category: Small molecule peptidic inhibitor]]
[[Category: Small molecule peptidic inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:34:37 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 15:52:05 2008''

Revision as of 12:52, 28 July 2008

Image:1pwq.png

Template:STRUCTURE 1pwq

Crystal structure of Anthrax Lethal Factor complexed with Thioacetyl-Tyr-Pro-Met-Amide, a metal-chelating peptidyl small molecule inhibitor

Template:ABSTRACT PUBMED 14718924

About this Structure

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

Reference

The structural basis for substrate and inhibitor selectivity of the anthrax lethal factor., Turk BE, Wong TY, Schwarzenbacher R, Jarrell ET, Leppla SH, Collier RJ, Liddington RC, Cantley LC, Nat Struct Mol Biol. 2004 Jan;11(1):60-6. Epub 2003 Dec 29. PMID:14718924

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