1pwp

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{{STRUCTURE_1pwp| PDB=1pwp | SCENE= }}
{{STRUCTURE_1pwp| PDB=1pwp | SCENE= }}
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'''Crystal Structure of the Anthrax Lethal Factor complexed with Small Molecule Inhibitor NSC 12155'''
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===Crystal Structure of the Anthrax Lethal Factor complexed with Small Molecule Inhibitor NSC 12155===
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==Overview==
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The virulent spore-forming bacterium Bacillus anthracis secretes anthrax toxin composed of protective antigen (PA), lethal factor (LF) and edema factor (EF). LF is a Zn-dependent metalloprotease that inactivates key signaling molecules, such as mitogen-activated protein kinase kinases (MAPKK), to ultimately cause cell death. We report here the identification of small molecule (nonpeptidic) inhibitors of LF. Using a two-stage screening assay, we determined the LF inhibitory properties of 19 compounds. Here, we describe six inhibitors on the basis of a pharmacophoric relationship determined using X-ray crystallographic data, molecular docking studies and three-dimensional (3D) database mining from the US National Cancer Institute (NCI) chemical repository. Three of these compounds have K(i) values in the 0.5-5 microM range and show competitive inhibition. These molecular scaffolds may be used to develop therapeutically viable inhibitors of LF.
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(as it appears on PubMed at http://www.pubmed.gov), where 14718925 is the PubMed ID number.
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{{ABSTRACT_PUBMED_14718925}}
==About this Structure==
==About this Structure==
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[[Category: Lethal factor]]
[[Category: Lethal factor]]
[[Category: Small molecule inhibitor]]
[[Category: Small molecule inhibitor]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sat May 3 05:34:30 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 11:06:19 2008''

Revision as of 08:06, 28 July 2008

Image:1pwp.png

Template:STRUCTURE 1pwp

Crystal Structure of the Anthrax Lethal Factor complexed with Small Molecule Inhibitor NSC 12155

Template:ABSTRACT PUBMED 14718925

About this Structure

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

Reference

Identification of small molecule inhibitors of anthrax lethal factor., Panchal RG, Hermone AR, Nguyen TL, Wong TY, Schwarzenbacher R, Schmidt J, Lane D, McGrath C, Turk BE, Burnett J, Aman MJ, Little S, Sausville EA, Zaharevitz DW, Cantley LC, Liddington RC, Gussio R, Bavari S, Nat Struct Mol Biol. 2004 Jan;11(1):67-72. Epub 2003 Dec 29. PMID:14718925

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