scholarly journals Hybrid Transgenic Mice Reveal In Vivo Specificity of G Protein–Coupled Receptor Kinases in the Heart

2000 ◽  
Vol 86 (1) ◽  
pp. 43-50 ◽  
Author(s):  
Andrea D. Eckhart ◽  
Sandra J. Duncan ◽  
Raymond B. Penn ◽  
Jeffrey L. Benovic ◽  
Robert J. Lefkowitz ◽  
...  
Keyword(s):  
Transgenic Mice ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
Receptor Kinases ◽  
G Protein Coupled

scholarly journals GRK Inhibition Potentiates Glucagon-Like Peptide-1 Action

2021 ◽  
Vol 12 ◽  
Author(s):  
Seunghun P. Lee ◽  
Jenson Qi ◽  
Guozhang Xu ◽  
Matthew M. Rankin ◽  
James Littrell ◽  
...  
Keyword(s):  
G Protein ◽  
G Protein Coupled Receptor ◽  
Dipeptidyl Peptidase 4 ◽  
Receptor Kinases ◽  
Glucagon Like Peptide ◽  
Glucagon Like Peptide 1 ◽  
Receptor Interacting Proteins ◽  
G Protein Coupled

The glucagon-like peptide-1 receptor (GLP-1R) is a G-protein-coupled receptor (GPCR) whose activation results in suppression of food intake and improvement of glucose metabolism. Several receptor interacting proteins regulate the signaling of GLP-1R such as G protein-coupled receptor kinases (GRK) and β-arrestins. Here we evaluated the physiological and pharmacological impact of GRK inhibition on GLP-1R activity leveraging small molecule inhibitors of GRK2 and GRK3. We demonstrated that inhibition of GRK: i) inhibited GLP-1-mediated β-arrestin recruitment, ii) enhanced GLP-1-induced insulin secretion in isolated islets and iii) has additive effect with dipeptidyl peptidase 4 in mediating suppression of glucose excursion in mice. These findings highlight the importance of GRK to modulate GLP-1R function in vitro and in vivo. GRK inhibition is a potential therapeutic approach to enhance endogenous and pharmacologically stimulated GLP-1R signaling.

scholarly journals Receptor-specific in vivo desensitization by the G protein-coupled receptor kinase-5 in transgenic mice.

1996 ◽  
Vol 93 (18) ◽  
pp. 9954-9959 ◽  
Author(s):  
H. A. Rockman ◽  
D. J. Choi ◽  
N. U. Rahman ◽  
S. A. Akhter ◽  
R. J. Lefkowitz ◽  
...  
Keyword(s):  
Transgenic Mice ◽  
G Protein ◽  
Receptor Kinase ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals The G Protein-Coupled Receptor Kinases (GRKs) in Chemokine Receptor-Mediated Immune Cell Migration: From Molecular Cues to Physiopathology

Cells ◽  
2021 ◽  
Vol 10 (1) ◽  
pp. 75
Author(s):  
Marta Laganà ◽  
Géraldine Schlecht-Louf ◽  
Françoise Bachelerie
Keyword(s):  
G Protein ◽  
Chemokine Receptor ◽  
Immune Cell ◽  
Neutrophil Migration ◽  
G Protein Coupled Receptor ◽  
Receptor Kinases ◽  
Immune Cell Migration ◽  
And Migration ◽  
G Protein Coupled ◽  
Gpcr Desensitization

Although G protein-coupled receptor kinases (GRKs) have long been known to regulate G protein-coupled receptor (GPCR) desensitization, their more recently characterized functions as scaffolds and signalling adapters underscore that this small family of proteins governs a larger array of physiological functions than originally suspected. This review explores how GRKs contribute to the complex signalling networks involved in the migration of immune cells along chemokine gradients sensed by cell surface GPCRs. We outline emerging evidence indicating that the coordinated docking of several GRKs on an active chemokine receptor determines a specific receptor phosphorylation barcode that will translate into distinct signalling and migration outcomes. The guidance cues for neutrophil migration are emphasized based on several alterations affecting GRKs or GPCRs reported to be involved in pathological conditions.

Myocardial and Peripheral Lymphocytic Transcriptomic Dissociation of β-adrenoceptors and G Protein–coupled Receptor Kinases in Heart Transplantation

2009 ◽  
Vol 28 (11) ◽  
pp. 1166-1171 ◽  
Author(s):  
Jaime Agüero ◽  
Luis Almenar ◽  
Pilar D'Ocon ◽  
Eduardo Oliver ◽  
Fermi Montó ◽  
...  
Keyword(s):  
Heart Transplantation ◽  
G Protein ◽  
G Protein Coupled Receptor ◽  
Receptor Kinases ◽  
G Protein Coupled
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