Structural Manipulation of Eicosanoid Receptors and Cellular Signaling

Eicosanoids are lipid mediators derived from the metabolism of arachidonic acid. These agents are locally released and activate different cell membrane receptors, and the latter are part of the G-protein coupled receptor family. While activation of eicosanoid receptors is associated with a wide vari...

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Main Author: Charles Brink
Format: Article
Language:English
Published: Wiley 2007-01-01
Series:The Scientific World Journal
Online Access:http://dx.doi.org/10.1100/tsw.2007.163
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author Charles Brink
author_facet Charles Brink
author_sort Charles Brink
collection DOAJ
description Eicosanoids are lipid mediators derived from the metabolism of arachidonic acid. These agents are locally released and activate different cell membrane receptors, and the latter are part of the G-protein coupled receptor family. While activation of eicosanoid receptors is associated with a wide variety of actions, there is limited information concerning the structural components of the eicosanoid receptors. To date, our understanding of the eicosanoid ligand-receptor binding interaction has been based on the rhodopsin template model. While receptors in the same family do share a common architecture, there are amino acid residues in the membrane binding pocket that play a key role in ligand recognition as well as the diversity observed in the cellular signaling. In order to understand the eicosanoid receptor binding interaction, attention must be focused on both the nature of the endogenous ligands as well as the template G-protein model that has been proposed. The data derived from chemical alterations in the endogenous ligands, together with the mutagenesis studies involving the structural modifications of the eicosanoid receptors, have suggested a working model of the eicosanoid receptors. However, the data also document various nuances in the receptor structure associated with ligand binding as well as a number of differences that will require further investigation.
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spelling doaj-art-e7948c77466f48559eb98708b4aa4a7a2025-08-20T02:21:10ZengWileyThe Scientific World Journal1537-744X2007-01-0171285130610.1100/tsw.2007.163Structural Manipulation of Eicosanoid Receptors and Cellular SignalingCharles Brink0INSERM U698, Haemostasis, Bio-Engineering and Cardiovascular Remodelling, CHU Xavier Bichat Secteur Claude Bernard, 46 rue Henri Huchard, 75877 Paris Cedex 18, FranceEicosanoids are lipid mediators derived from the metabolism of arachidonic acid. These agents are locally released and activate different cell membrane receptors, and the latter are part of the G-protein coupled receptor family. While activation of eicosanoid receptors is associated with a wide variety of actions, there is limited information concerning the structural components of the eicosanoid receptors. To date, our understanding of the eicosanoid ligand-receptor binding interaction has been based on the rhodopsin template model. While receptors in the same family do share a common architecture, there are amino acid residues in the membrane binding pocket that play a key role in ligand recognition as well as the diversity observed in the cellular signaling. In order to understand the eicosanoid receptor binding interaction, attention must be focused on both the nature of the endogenous ligands as well as the template G-protein model that has been proposed. The data derived from chemical alterations in the endogenous ligands, together with the mutagenesis studies involving the structural modifications of the eicosanoid receptors, have suggested a working model of the eicosanoid receptors. However, the data also document various nuances in the receptor structure associated with ligand binding as well as a number of differences that will require further investigation.http://dx.doi.org/10.1100/tsw.2007.163
spellingShingle Charles Brink
Structural Manipulation of Eicosanoid Receptors and Cellular Signaling
The Scientific World Journal
title Structural Manipulation of Eicosanoid Receptors and Cellular Signaling
title_full Structural Manipulation of Eicosanoid Receptors and Cellular Signaling
title_fullStr Structural Manipulation of Eicosanoid Receptors and Cellular Signaling
title_full_unstemmed Structural Manipulation of Eicosanoid Receptors and Cellular Signaling
title_short Structural Manipulation of Eicosanoid Receptors and Cellular Signaling
title_sort structural manipulation of eicosanoid receptors and cellular signaling
url http://dx.doi.org/10.1100/tsw.2007.163
work_keys_str_mv AT charlesbrink structuralmanipulationofeicosanoidreceptorsandcellularsignaling