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2q7r
From Proteopedia
(New page: 200px<br /> <applet load="2q7r" size="450" color="white" frame="true" align="right" spinBox="true" caption="2q7r, resolution 4.00Å" /> '''Crystal structure o...) |
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| - | [[Image:2q7r. | + | [[Image:2q7r.jpg|left|200px]]<br /><applet load="2q7r" size="350" color="white" frame="true" align="right" spinBox="true" |
| - | <applet load="2q7r" size=" | + | |
caption="2q7r, resolution 4.00Å" /> | caption="2q7r, resolution 4.00Å" /> | ||
'''Crystal structure of human FLAP with an iodinated analog of MK-591'''<br /> | '''Crystal structure of human FLAP with an iodinated analog of MK-591'''<br /> | ||
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==Overview== | ==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. | 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. | ||
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| - | ==Disease== | ||
| - | Known diseases associated with this structure: Myocardial infarction, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=603700 603700]], Stroke, susceptibility to OMIM:[[http://www.ncbi.nlm.nih.gov/entrez/dispomim.cgi?id=603700 603700]] | ||
==About this Structure== | ==About this Structure== | ||
| - | 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 3CS as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http:// | + | 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]. |
==Reference== | ==Reference== | ||
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[[Category: membrane protein]] | [[Category: membrane protein]] | ||
| - | ''Page seeded by [http:// | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Wed Jan 23 14:03:19 2008'' |
Revision as of 12:03, 23 January 2008
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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 with as ligand. 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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