Faculty Articles

Title

GPCR signaling and cardiac function

ISBN or ISSN

0014-2999

Location

Netherlands

Publication Title

European Journal of Pharmacology

Volume

763

Issue

Pt B

Publication Date / Copyright Date

9-15-2015

First Page

143

Last Page

148

Publisher

Elsevier Science

Abstract

G protein-coupled receptors (GPCRs), such as β-adrenergic and angiotensin II receptors, located in the membranes of all three major cardiac cell types, i.e. myocytes, fibroblasts and endothelial cells, play crucial roles in regulating cardiac function and morphology. Their importance in cardiac physiology and disease is reflected by the fact that, collectively, they represent the direct targets of over a third of the currently approved cardiovascular drugs used in clinical practice. Over the past few decades, advances in elucidation of their structure, function and the signaling pathways they elicit, specifically in the heart, have led to identification of an increasing number of new molecular targets for heart disease therapy. Here, we review these signaling modalities employed by GPCRs known to be expressed in the cardiac myocyte membranes and to directly modulate cardiac contractility. We also highlight drugs and drug classes that directly target these GPCRs to modulate cardiac function, as well as molecules involved in cardiac GPCR signaling that have the potential of becoming novel drug targets for modulation of cardiac function in the future.

Disciplines

Medicine and Health Sciences | Pharmacy and Pharmaceutical Sciences

Keywords

Animals, Heart, Humans, Myocardial Contraction, Receptors, G-Protein-Coupled, Signal Transduction

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Peer Reviewed

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