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Current and future G protein-coupled receptor signaling targets for heart failure therapy

Authors Siryk-Bathgate A, Dabul S, Lymperopoulos A

Received 30 August 2013

Accepted for publication 11 September 2013

Published 11 October 2013 Volume 2013:7 Pages 1209—1222

DOI https://doi.org/10.2147/DDDT.S35905

Checked for plagiarism Yes

Review by Single-blind

Peer reviewer comments 3


Ashley Siryk-Bathgate, Samalia Dabul, Anastasios Lymperopoulos

Laboratory for the Study of Neurohormonal Control of the Circulation, Department of Pharmaceutical Sciences, Nova Southeastern University College of Pharmacy, Fort Lauderdale, FL, USA

Abstract: Although there have been significant advances in the therapy of heart failure in recent decades, such as the introduction of β-blockers and antagonists of the renin–angiotensin–aldosterone system, this devastating disease still carries tremendous morbidity and mortality in the western world. G protein-coupled receptors, such as β -adrenergic and angiotensin II receptors, located in the membranes of all three major cardiac cell types, ie, myocytes, fibroblasts, and endothelial cells, play crucial roles in regulation of cardiac function in health and disease. Their importance is reflected by the fact that, collectively, they represent the direct targets of over one-third of the currently approved cardiovascular drugs used in clinical practice. Over the past few decades, advances in elucidation of the signaling pathways they elicit, specifically in the heart, have led to identification of an increasing number of new molecular targets for heart failure therapy. Here, we review these possible targets for heart failure therapy that have emerged from studies of cardiac G protein-coupled receptor signaling in health and disease, with a particular focus on the main cardiac G protein-coupled receptor types, ie, the β -adrenergic and the angiotensin II type 1 receptors. We also highlight key issues that need to be addressed to improve the chances of success of novel therapies directed against these targets.

Keywords: heart failure, G protein-coupled receptor, signaling, cardiac, therapeutic target

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