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2q7r

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[[Image:2q7r.jpg|left|200px]]<br /><applet load="2q7r" size="350" color="white" frame="true" align="right" spinBox="true"
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[[Image:2q7r.jpg|left|200px]]
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caption="2q7r, resolution 4.00&Aring;" />
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'''Crystal structure of human FLAP with an iodinated analog of MK-591'''<br />
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{{Structure
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|PDB= 2q7r |SIZE=350|CAPTION= <scene name='initialview01'>2q7r</scene>, resolution 4.00&Aring;
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|SITE=
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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>
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|ACTIVITY=
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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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'''Crystal structure of human FLAP with an iodinated analog of MK-591'''
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==Overview==
==Overview==
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==About this Structure==
==About this Structure==
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2Q7R is a [http://en.wikipedia.org/wiki/Single_protein Single protein] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens] with <scene name='pdbligand=3CS:'>3CS</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q7R OCA].
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2Q7R is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q7R OCA].
==Reference==
==Reference==
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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:[http://ispc.weizmann.ac.il//pmbin/getpm?pmid=17600184 17600184]
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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:[http://www.ncbi.nlm.nih.gov/pubmed/17600184 17600184]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
[[Category: Single protein]]
[[Category: Single protein]]
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[[Category: membrane protein]]
[[Category: membrane protein]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Feb 21 18:36:56 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 18:22:47 2008''

Revision as of 16:22, 20 March 2008


PDB ID 2q7r

Drag the structure with the mouse to rotate
, resolution 4.00Å
Ligands:
Gene: ALOX5AP, FLAP (Homo sapiens)
Coordinates: save as pdb, mmCIF, xml



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


Contents

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.

Disease

Known diseases associated with this structure: Myocardial infarction, susceptibility to OMIM:[603700], Stroke, susceptibility to OMIM:[603700]

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

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