2q7r
From Proteopedia
| |||||||
| , 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
Page seeded by OCA on Thu Mar 20 18:22:47 2008
