2q7r
From Proteopedia
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Crystal structure of human FLAP with an iodinated analog of MK-591
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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 with 3CS 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
Page seeded by OCA on Mon Nov 12 23:30:47 2007
