Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
11019353 | Pharmacology & Therapeutics | 2018 | 56 Pages |
Abstract
Apelin is a vasoactive peptide and is an endogenous ligand for APJ receptors, which are widely expressed in blood vessels, heart, and cardiovascular regulatory regions of the brain. A growing body of evidence now demonstrates a regulatory role for the apelin/APJ receptor system in cardiovascular physiology and pathophysiology, thus making it a potential target for cardiovascular drug discovery and development. Indeed, ongoing studies are investigating the potential benefits of apelin and apelin-mimetics for disorders such as heart failure and pulmonary arterial hypertension. Apelin causes relaxation of isolated arteries, and systemic administration of apelin typically results in a reduction in systolic and diastolic blood pressure and an increase in blood flow. Nonetheless, vasopressor responses and contraction of vascular smooth muscle in response to apelin have also been observed under certain conditions. The goal of the current review is to summarize major findings regarding the apelin/APJ receptor system in blood vessels, with an emphasis on regulation of vascular tone, and to identify areas of investigation that may provide guidance for the development of novel therapeutic agents that target this system.
Keywords
ElabelaPKCAT-1MLCHIF-1αAPJN(G)-nitro-l-arginine methyl esterERKcGMPACE-2PI3KvasoconstrictionBKCacAMPl-NAMECyclic adenosine monophosphatevasodilationcoronary artery diseaseApelinmyosin light chainCADphosphoinositide 3-kinasecyclic guanosine monophosphateNitric oxideKORProtein kinase Cextracellular signal-regulated kinaseapelin receptorκ-opioid receptors
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Authors
Amreen Mughal, Stephen T. O'Rourke,