| Literature DB >> 27633970 |
Mikhail Romashko1, Joseph Schragenheim1, Nader G Abraham2, John A McClung3.
Abstract
Cardiovascular disease remains the leading cause of death worldwide. Among many potential targets for pharmacological intervention, a promising strategy involves epoxyeicosatrienoic acid (EET) and soluble epoxide hydroxylase (sEH) inhibition. sEH is the enzyme that converts EET to its less potent metabolite; therefore, EET is upregulated by its inhibitor. EET has pleotropic effects that collectively reduce inflammation, while increasing vasodilation and insulin sensitivity. Recent reports indicate that EET agonists and sEH inhibitors are capable of not only reversing endothelial dysfunction and hypertension, but also of reversing cardiac remodeling, which is a hallmark of cardiomyopathy and the metabolic syndrome. EET agonists and sEH inhibitors are in development as potential therapies, and at least one drug is already in clinical trials. This review examines the activity of EET in biological systems, proposes a series of pathways to explain its mechanism of action, and discusses how these might be exploited for potential therapeutic use.Entities:
Keywords: HO-1; PGC-1α; diabetes mellitus; epoxyeicosatrienoic acid (EET); heart failure; metabolic syndrome
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Year: 2016 PMID: 27633970 DOI: 10.1016/j.tips.2016.08.001
Source DB: PubMed Journal: Trends Pharmacol Sci ISSN: 0165-6147 Impact factor: 14.819