Document Detail

Epoxyeicosatrienoic acids: formation, metabolism and potential role in tissue physiology and pathophysiology.
MedLine Citation:
PMID:  19505190     Owner:  NLM     Status:  In-Process    
BACKGROUND: CYP enzymes from the CYP2C and CYP2J subfamilies metabolize arachidonic acid in a regiospecific and stereoselective manner to eight epoxyeicosatrienoic acids (EETs). Various EETs have been detected in the liver, as well as in many extrahepatic tissues, and have been implicated in numerous physiological functions from cell signaling to vasodilation and angiogenesis. OBJECTIVE: This report reviews the sites of expression and activity of arachidonic acid epoxygenase CYP isoforms, as well as the physiological role and metabolism of EETs in various extrahepatic tissues. Possible functions of EETs in tissue pathophysiology and implications as potential drug targets are also discussed. METHODS: The most recent primary research literature on EET forming enzymes and the new physiological functions of EETs in various tissues were reviewed. RESULTS/CONCLUSIONS: Epoxyeicosatrienoic acids are important in maintaining the homeostasis and in responding to stress in various extra hepatic tissues. It is not clear whether these effects are owing to EETs acting on a universal receptor or through a mechanism involving a second messenger. A better understanding of the regulation of EET levels and their mechanism of action on various receptors will accelerate research aiming at developing therapeutic agents that target EET formation or metabolism pathways.
Rüdiger Kaspera; Rheem A Totah
Publication Detail:
Type:  Journal Article; Review    
Journal Detail:
Title:  Expert opinion on drug metabolism & toxicology     Volume:  5     ISSN:  1744-7607     ISO Abbreviation:  Expert Opin Drug Metab Toxicol     Publication Date:  2009 Jul 
Date Detail:
Created Date:  2009-06-23     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  101228422     Medline TA:  Expert Opin Drug Metab Toxicol     Country:  England    
Other Details:
Languages:  eng     Pagination:  757-71     Citation Subset:  IM    
University of Washington, Department of Medicinal Chemistry, Seattle, WA 98195, USA.
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