Related Experiment Video
Updated: May 17, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
G protein-coupled receptor kinases in cardiovascular disease: why "where" matters
Fadia A Kamal1, Joshua G Travers, Burns C Blaxall
1The Heart Institute, Molecular Cardiovascular Biology, Cincinnati Children's Hospital Medical Center, Cincinnati, OH 45229, USA.
Abstract:
Cardiac function is mainly controlled by β-adrenergic receptors (β-ARs), members of the G protein-coupled receptor (GPCR) family. GPCR signaling and expression are tightly controlled by G protein-coupled receptor kinases (GRKs), which induce GPCR internalization and signal termination through phosphorylation. Reduced β-AR density and activity associated with elevated cardiac GRK expression and activity have been described in various cardiovascular diseases. Moreover, alterations in extracardiac GRKs have been observed in blood vessels, adrenal glands, kidneys, and fat cells. The broad tissue distribution of GPCRs and GRKs suggests that a keen appreciation of integrative physiology may drive future therapeutic development. In this review, we provide a brief summary of GRK isoforms, subcellular localization, and interacting partners that impinge directly or indirectly on the cardiovascular system. We also discuss GRK/GPCR interactions and their implications in cardiovascular pathophysiology.
More Related Videos
07:41A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
09:21BRET-based G Protein Biosensors for Measuring G Protein-Coupled Receptor Activity in Live Cells
Published on: November 7, 2025
Related Concept Videos
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G Protein-coupled Receptors
GPCRs are also called heptahelical, 7TM, or serpentine receptors, and consist of seven (H1-H7) transmembrane alpha-helices that span the bilayer to form a cylindrical core. The transmembrane helices are connected by three extracellular loops and three...
G-Protein Gated Ion Channels
Sensory organs,...
G-protein Coupled Receptors
G-protein Coupled Receptors