Epoxyeicosatrienoic acid analogs and vascular function

Sudhahar Varadarajan, S. Shaw, J. D. Imig

Research output: Contribution to journalReview article

67 Citations (Scopus)

Abstract

Arachidonic acid metabolites, eicosanoids, are key contributors to vascular function and improper eicosanoid regulation contributes to the progression of cardiovascular diseases. Epoxyeicosatrienoic acids (EETs) are synthesized from arachidonic acid by epoxygenase enzymes to four regioisomers, 5,6-EET, 8,9-EET, 11,12-EET, and 14,15-EET. These EETs have interesting beneficial effects like vasodilation, anti-inflammation, and anti-platelet aggregation that could combat cardiovascular diseases. There is mounting evidence that each regioisomeric EET may have unique vascular effects and that the contribution of individual EETs to vascular function differs from organ to organ. Over the past decade EET analogs and antagonists have been synthesized to determine EET structure function relationships and define the contribution of each regioisomeric EET. A number of studies have demonstrated that EET analogs induce vasodilation, lower blood pressure and decrease inflammation. EET antagonists have also been used to demonstrate that endogenous EETs contribute importantly to cardiovascular function. This review will discuss EET synthesis, regulation and physiological roles in the cardiovascular system. Next we will focus on the development of EET analogs and what has been learned about their contribution to vascular function. Finally, the development of EET antagonists and how these have been utilized to determine the cardiovascular actions of endogenous epoxides will be discussed. Overall, this review will highlight the important knowledge garnered by the development of EET analogs and their possible value in the treatment of cardiovascular diseases.

Original languageEnglish (US)
Pages (from-to)1181-1190
Number of pages10
JournalCurrent Medicinal Chemistry
Volume17
Issue number12
DOIs
StatePublished - Jan 1 2010

Fingerprint

Blood Vessels
Acids
Cardiovascular Diseases
Eicosanoids
Vasodilation
Inflammation
Epoxy Compounds
Cardiovascular System
Cardiovascular system
Platelet Aggregation
Arachidonic Acid
Blood pressure
Metabolites
Platelets
Mountings
Blood Pressure
Agglomeration
Enzymes
11,12-epoxy-5,8,14-eicosatrienoic acid

Keywords

  • Agonist and antagonist
  • Analogs
  • Cardiovascular
  • Endothelium derived hyperpolarizing factor
  • Epoxyeicosatrienoic acids
  • Inflammation

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

Cite this

Epoxyeicosatrienoic acid analogs and vascular function. / Varadarajan, Sudhahar; Shaw, S.; Imig, J. D.

In: Current Medicinal Chemistry, Vol. 17, No. 12, 01.01.2010, p. 1181-1190.

Research output: Contribution to journalReview article

Varadarajan, Sudhahar ; Shaw, S. ; Imig, J. D. / Epoxyeicosatrienoic acid analogs and vascular function. In: Current Medicinal Chemistry. 2010 ; Vol. 17, No. 12. pp. 1181-1190.
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