Unchanged G-protein-coupled receptor kinase activity in the aging human heart
Kirsten Leineweber1, Stefan Klapproth, Anja Beilfuss
1Departments of Pathophysiology and Nephrology, University of Essen School of Medicine, Essen, Germany
Objectives:
We sought to find out whether G-protein-coupled receptor kinase (GRK) activity is also increased in the aging human heart.
Background:
In the aging and failing human heart, cardiac beta-adrenoceptors (beta-AR) are desensitized. In heart failure (HF), an increase in cardiac GRK activity considerably contributes to this beta-AR desensitization.
Methods:
We assessed GRK activity (by in vitro rhodopsin phosphorylation) in the right atria (RA) from 16 children (mean age 9 +/- 2 years) and 17 elderly patients (mean age 67 +/- 2 years) without apparent HF and in the RA from four patients with end-stage HF.Cytosolic and membranous GRK activities in the RA from children were not significantly different from those in elderly patients; in contrast, cytosolic and membranous GRK activities in the RA from patients with end-stage HF were significantly increased.
Conclusions:
In contrast to the failing human heart, in the aging human heart, GRK activity is not increased. Thus, GRK activity appears to not play an important role in beta-AR desensitization in the aging human heart.
Related Concept Videos
G-Protein Gated Ion Channels
Sensory organs,...
GPCR Desensitization
GPCRs Regulate Adenylyl Cylase Activity
Two...
Activation and Inactivation of G Proteins
Transducer Mechanism: Enzyme-Linked Receptors
Major types that are helpful drug targets include:
cAMP-dependent Protein Kinase Pathways

