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2q7r
From Proteopedia
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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.]] | ||
| - | [[Category: | + | [[Category: Flap]] |
| - | [[Category: | + | [[Category: Lipid transport]] |
| - | [[Category: | + | [[Category: Mapeg]] |
| - | [[Category: | + | [[Category: Membrane protein]] |
| - | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 14:29:41 2008'' | |
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on | + | |
Revision as of 11:29, 4 May 2008
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
