G-protein-coupled receptor kinases in cardiovascular conditions: focus on G-protein-coupled receptor kinase 2, a gain in translational medicine

Abstract

With increasing knowledge of the regulatory mechanisms of G-protein-coupled receptor signaling in heart physiology, many studies have focused on the role of this system in cardiovascular disease. In recent years, scientists have moved their attention from the receptors to their regulatory proteins: the G-protein-coupled receptor kinases. This class of protein is indispensable for terminating signaling of G-protein-coupled receptors through receptor desensitization and downregulation. This article attempts to assemble the currently available information regarding G-protein-coupled receptor kinases and their role in cardiovascular disease and, in particular, the potential employment of G-protein-coupled receptor kinase 2 as biomarker of cardiac dysfunction.

KEYWORDS::

• βARKct
• chronic adrenergic activation
• GPCR desensitization
• GPCR downregulation
• G-protein-coupled receptor kinases
• GRK2 ablation
• GRK2 upregulation
• lymphocyte β-adrenergic signaling

Financial & competing interests disclosure

Guido Iaccarino holds a US patent for the use of GRK2 as a biomarker for heart falilure, The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

No writing assistance was utilized in the production of this manuscript.

Additional information

Funding

Guido Iaccarino holds a US patent for the use of GRK2 as a biomarker for heart falilure, The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.