1pwq

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[[Image:1pwq.jpg|left|200px]]
[[Image:1pwq.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 1pwq |SIZE=350|CAPTION= <scene name='initialview01'>1pwq</scene>, resolution 3.52&Aring;
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The line below this paragraph, containing "STRUCTURE_1pwq", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=SD2:N-(SULFANYLACETYL)TYROSYLPROLYLMETHIONINAMIDE'>SD2</scene>, <scene name='pdbligand=ZN:ZINC+ION'>ZN</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY= <span class='plainlinks'>[http://en.wikipedia.org/wiki/Anthrax_lethal_factor_endopeptidase Anthrax lethal factor endopeptidase], with EC number [http://www.brenda-enzymes.info/php/result_flat.php4?ecno=3.4.24.83 3.4.24.83] </span>
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or leave the SCENE parameter empty for the default display.
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|GENE= LEF ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=1392 Bacillus anthracis])
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-->
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|DOMAIN=
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{{STRUCTURE_1pwq| PDB=1pwq | SCENE= }}
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|RELATEDENTRY=[[1pwp|1PWP]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=1pwq FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=1pwq OCA], [http://www.ebi.ac.uk/pdbsum/1pwq PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=1pwq RCSB]</span>
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}}
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'''Crystal structure of Anthrax Lethal Factor complexed with Thioacetyl-Tyr-Pro-Met-Amide, a metal-chelating peptidyl small molecule inhibitor'''
'''Crystal structure of Anthrax Lethal Factor complexed with Thioacetyl-Tyr-Pro-Met-Amide, a metal-chelating peptidyl small molecule inhibitor'''
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[[Category: Schwarzenbacher, R.]]
[[Category: Schwarzenbacher, R.]]
[[Category: Wong, T Y.]]
[[Category: Wong, T Y.]]
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[[Category: anthrax toxin]]
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[[Category: Anthrax toxin]]
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[[Category: lethal factor]]
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[[Category: Lethal factor]]
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[[Category: metal-chelator]]
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[[Category: Metal-chelator]]
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[[Category: small molecule peptidic inhibitor]]
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[[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 Sun Mar 30 23:05:35 2008''
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Revision as of 02:34, 3 May 2008

Image:1pwq.jpg

Template:STRUCTURE 1pwq

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


Overview

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.

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 Page seeded by OCA on Sat May 3 05:34:37 2008

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OCA

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