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Apelin-13 in blood pressure regulation and cardiovascular disease
Liliya M Yamaleyeva1, Hossam A Shaltout, Jasmina Varagic
1aHypertension 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.
Insights
Apelin-13 shows therapeutic potential for hypertension and heart failure, offering novel treatment strategies. Research focuses on overcoming its short half-life and improving delivery for cardiovascular disease management.
Area of Science:
- Cardiovascular Pharmacology
- Endocrinology
- G-protein coupled receptor signaling
Background:
- Hypertension and heart failure represent significant global health and economic burdens.
- Current pharmacological treatments for cardiovascular diseases necessitate novel therapeutic approaches.
- Apelin-13, an endogenous ligand for the APJ receptor, has emerged as a potential therapeutic agent.
Purpose of the Study:
- To review recent evidence on the therapeutic potential of apelin-13 for cardiovascular diseases.
- To explore the role of the apelin/APJ axis in managing hypertension and heart failure.
Main Methods:
- Review of existing scientific literature on apelin-13 and its effects.
- Analysis of studies investigating systemic and central administration of apelin-13.
- Examination of research on apelin's inotropic and cardioprotective effects.
Main Results:
- Systemic apelin-13 demonstrates vasodilatory and antihypertensive effects.
- Central apelin administration can increase blood pressure; endothelial dysfunction may impair systemic effects.
- Apelin exhibits positive inotropic and cardioprotective effects in cardiac models, suggesting utility in heart failure and ischemia.
Conclusions:
- The apelin/APJ axis presents a promising new target for developing novel therapeutics for hypertension and cardiovascular disease.
- Challenges in apelin therapy include its short half-life and parenteral administration, driving research into improved agonists and delivery methods.
Purpose Of Review:
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.
Recent Findings:
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.
Summary:
The apelin/APJ axis may represent a new target for the development of novel therapeutic approaches for the treatment of hypertension and cardiovascular disease.
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