2q7m: Difference between revisions

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New page: left|200px<br /> <applet load="2q7m" size="450" color="white" frame="true" align="right" spinBox="true" caption="2q7m, resolution 4.25Å" /> '''Crystal structure o...
 
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[[Image:2q7m.gif|left|200px]]<br />
[[Image:2q7m.jpg|left|200px]]<br /><applet load="2q7m" size="350" color="white" frame="true" align="right" spinBox="true"  
<applet load="2q7m" size="450" color="white" frame="true" align="right" spinBox="true"  
caption="2q7m, resolution 4.25&Aring;" />
caption="2q7m, resolution 4.25&Aring;" />
'''Crystal structure of human FLAP with MK-591'''<br />
'''Crystal structure of human FLAP with 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.
==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==
2Q7M 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 2CS as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://ispc.weizmann.ac.il/oca-bin/ocashort?id=2Q7M OCA].  
2Q7M 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=2CS:'>2CS</scene> as [http://en.wikipedia.org/wiki/ligand ligand]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=2Q7M OCA].  


==Reference==
==Reference==
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[[Category: membrane protein]]
[[Category: membrane protein]]


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