Related Experiment Video
Updated: Jun 25, 2026

Measuring G-protein-coupled Receptor Signaling via Radio-labeled GTP Binding
Published on: June 9, 2017
GRK mythology: G-protein receptor kinases in cardiovascular disease
1Center for Pharmacogenomics, Washington University, 660 S. Euclid Ave., Campus Box 8086, St. Louis, MO 63110, USA. gdorn@dom.wustl.edu
Abstract:
G-protein receptor kinases (GRKs) are indispensable for terminating signaling of G-protein coupled receptors (GPCR) through receptor desensitization and downregulation. Increased neurohormone levels in heart failure and the adverse consequences of constant neurohormonal stimulation suggest an important protective role for mechanisms that desensitize neurohormone receptor responses. For that reason, GRK2, the first GRK identified in the heart, has been extensively studied in heart failure, cardiac hypertrophy, and myocardial infarction. However, our understanding of the roles of GRKs in general, and the differential effects of cardiac receptor phosphorylation by individual cardiac-expressed GRKs, have evolved considerably in the last few years. Here, recent developments are reviewed, with an emphasis on novel GRK functions and signaling pathways.
More Related Videos
Related Concept Videos
G-Protein Gated Ion Channels
Sensory organs,...
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
GPCR Desensitization
GPCRs Regulate Adenylyl Cylase Activity
Two...
Transducer Mechanism: G Protein–Coupled Receptors
GPCRs are also called heptahelical, 7TM, or...
Activation and Inactivation of G Proteins

