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2q7m

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Revision as of 16:22, 20 March 2008 by OCA (Talk | contribs)
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Image:2q7m.jpg


PDB ID 2q7m

Drag the structure with the mouse to rotate
, resolution 4.25Å
Ligands:
Gene: ALOX5AP, FLAP (Homo sapiens)
Coordinates: save as pdb, mmCIF, xml



Crystal structure of human FLAP with 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

2Q7M 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 18:22:43 2008

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