2q7r

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[[Image:2q7r.jpg|left|200px]]
[[Image:2q7r.jpg|left|200px]]
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{{Structure
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<!--
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|PDB= 2q7r |SIZE=350|CAPTION= <scene name='initialview01'>2q7r</scene>, resolution 4.00&Aring;
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The line below this paragraph, containing "STRUCTURE_2q7r", 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=3CS:3-[3-(3,3-DIMETHYLBUTANOYL)-1-(4-IODOBENZYL)-5-(QUINOLIN-2-YLMETHOXY)-1H-INDOL-2-YL]-2,2-DIMETHYLPROPANOIC+ACID'>3CS</scene>, <scene name='pdbligand=MSE:SELENOMETHIONINE'>MSE</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=
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or leave the SCENE parameter empty for the default display.
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|GENE= ALOX5AP, FLAP ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2q7r| PDB=2q7r | SCENE= }}
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|RELATEDENTRY=[[2q7m|2q7m]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2q7r FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2q7r OCA], [http://www.ebi.ac.uk/pdbsum/2q7r PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2q7r RCSB]</span>
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}}
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'''Crystal structure of human FLAP with an iodinated analog of MK-591'''
'''Crystal structure of human FLAP with an iodinated analog of MK-591'''
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[[Category: Single protein]]
[[Category: Single protein]]
[[Category: Ferguson, A D.]]
[[Category: Ferguson, A D.]]
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[[Category: flap]]
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[[Category: Flap]]
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[[Category: lipid transport]]
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[[Category: Lipid transport]]
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[[Category: mapeg]]
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[[Category: Mapeg]]
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[[Category: membrane protein]]
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[[Category: Membrane protein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:29:41 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:45:57 2008''
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Revision as of 11:29, 4 May 2008

Image:2q7r.jpg

Template:STRUCTURE 2q7r

Crystal structure of human FLAP with an iodinated analog of MK-591


Overview

Leukotrienes are proinflammatory products of arachidonic acid oxidation by 5-lipoxygenase that have been shown to be involved in respiratory and cardiovascular diseases. The integral membrane protein FLAP is essential for leukotriene biosynthesis. We describe the x-ray crystal structures of human FLAP in complex with two leukotriene biosynthesis inhibitors at 4.0 and 4.2 angstrom resolution, respectively. The structures show that inhibitors bind in membrane-embedded pockets of FLAP, which suggests how these inhibitors prevent arachidonic acid from binding to FLAP and subsequently being transferred to 5-lipoxygenase, thereby preventing leukotriene biosynthesis. This structural information provides a platform for the development of therapeutics for respiratory and cardiovascular diseases.

About this Structure

2Q7R is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

Crystal structure of inhibitor-bound human 5-lipoxygenase-activating protein., Ferguson AD, McKeever BM, Xu S, Wisniewski D, Miller DK, Yamin TT, Spencer RH, Chu L, Ujjainwalla F, Cunningham BR, Evans JF, Becker JW, Science. 2007 Jul 27;317(5837):510-2. Epub 2007 Jun 28. PMID:17600184 Page seeded by OCA on Sun May 4 14:29:41 2008

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