Myocardial G protein-coupled receptor kinases: Implications for heart failure therapy

摘要: The beta-adrenergic signaling cascade is an important regulator of myocardial function. Significant alterations this pathway are associated with several cardiovascular diseases, including congestive heart failure (CHF). Included in these increased activity and expression G protein-coupled receptor kinases (GRKs), such as the kinase (beta ARK1), which phosphorylate desensitize receptors ARs). A body evidence accumulating that suggests GRKs, particular beta ARK1, critical determinants cardiac function under normal conditions disease states. Transgenic mice myocardial-targeted GRK have shown profound changes vivo functional performance heart. studies compelling finding inhibition ARK1 or significantly enhances potentiates AR failing cardiomyocytes. This article summarizes advances made study addresses its potential a novel therapeutic target for CHF.