Document Type
Article
Publication Date
9-19-2023
Publication Title
Therapeutic Advances in Cardiovascular Disease
Keywords
arrhythmias, atrial fibrillation, cardiac myocyte, cyclic AMP, G protein-coupled receptor, G proteins, heart failure, regulator of G protein signaling, signal transduction
ISSN
1753-9455
Volume
17
Abstract
G protein-coupled receptors (GPCRs) play pivotal roles in regulation of cardiac function and homeostasis. To function properly, every cell needs these receptors to be stimulated only when a specific extracellular stimulus is present, and to be silenced the moment that stimulus is removed. The regulator of G protein signaling (RGS) proteins are crucial for the latter to occur at the cell membrane, where the GPCR normally resides. Perturbations in both activation and termination of G protein signaling underlie numerous heart pathologies. Although more than 30 mammalian RGS proteins have been identified, each RGS protein seems to interact only with a specific set of G protein subunits and GPCR types/subtypes in any given tissue or cell type, and this applies to the myocardium as well. A large number of studies have provided substantial evidence for the roles various RGS proteins expressed in cardiomyocytes play in cardiac physiology and heart disease pathophysiology. This review summarizes the current understanding of the functional roles of cardiac RGS proteins and their implications for the treatment of specific heart diseases, such as heart failure and atrial fibrillation. We focus on cardiac RGS4 in particular, since this isoform appears to be selectively (among the RGS protein family) upregulated in human heart failure and is also the target of ongoing drug discovery efforts for the treatment of a variety of diseases.
Creative Commons License
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License
NSUWorks Citation
Del Calvo, Giselle; Baggio Lopez, Teresa; and Lymperopoulos, Anastasios, "The therapeutic potential of targeting cardiac RGS4." (2023). HPD Articles. 282.
https://nsuworks.nova.edu/hpd_facarticles/282
DOI
10.1177/17539447231199350
Copyright
© The Author(s), 2023
Comments
The authors disclosed receipt of the following financial support for the research, authorship, and/or publication of this article: AL is supported by a grant from the National Institutes of Health (NIH)/National Heart, Lung, and Blood Institute (NHLBI) (R01 #HL155718-01).