Apelin-13 in blood pressure regulation and cardiovascular disease.
Despite extensive pharmacological treatment, hypertension and heart failure still pose as high health and economic burden. Thus, novel therapeutic approaches are needed to promote more effective treatment of hypertension and cardiovascular disease. In this review we summarized recent evidence supporting the therapeutic potential of apelin-13, a recently discovered endogenous ligand for the G-protein coupled receptor APJ.



Systemic administration of apelin-13 or its posttranslationally modified form, pyroglutamate apelin-13, exert vasodilatory and antihypertensive effects. Yet, central application of apelin increases blood pressure and its systemic effects may be compromised in the presence of endothelial dysfunction. In addition, positive inotropic effects by exogenous apelin in the normal and failing heart, as well as cardioprotective effects after myocardial infarction, strongly suggest its therapeutic potential in preventing and treating heart failure and consequences of myocardial ischemia. However, therapeutic use of apelin is limited primarily by its short half-life and parenteral administration, and significant effort has been directed to the development of novel agonists, delivery methods, and improving the efficacy of agonists at APJ.



The apelin/APJ axis may represent a new target for the development of novel therapeutic approaches for the treatment of hypertension and cardiovascular disease.
aHypertension and Vascular Research Center bDepartment of Surgery cDepartment of Physiology and Pharmacology dDepartment of Obstetrics and Gynecology, Wake Forest School of Medicine, Winston-Salem, North Carolina, USA.
Liliya M
LM
Yamaleyeva
Hossam A
HA
Shaltout
Jasmina
J
Varagic
D000959:Antihypertensive Agents / Q000494:pharmacology* / Q000627:therapeutic use; D001794:Blood Pressure / Q000187:drug effects*; D006333:Heart Failure / Q000188:drug therapy; D006801:Humans; D036341:Intercellular Signaling Peptides and Proteins / Q000494:pharmacology* / Q000627:therapeutic use; D017202:Myocardial Ischemia / Q000188:drug therapy
D000959:Antihypertensive Agents; D036341:Intercellular Signaling Peptides and Proteins; C495199:apelin-13 peptide