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.
journal_name
Trends Pharmacol Scijournal_title
Trends in pharmacological sciencesauthors
Romashko M,Schragenheim J,Abraham NG,McClung JAdoi
10.1016/j.tips.2016.08.001subject
Has Abstractpub_date
2016-11-01 00:00:00pages
945-962issue
11eissn
0165-6147issn
1873-3735pii
S0165-6147(16)30105-5journal_volume
37pub_type
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