scholarly journals Role of Helix 8 of the Thyrotropin-Releasing Hormone Receptor in Phosphorylation by G Protein-Coupled Receptor Kinase

2009 ◽  
Vol 77 (2) ◽  
pp. 288-297 ◽  
Author(s):  
Austin U. Gehret ◽  
Brian W. Jones ◽  
Phuong N. Tran ◽  
Laurie B. Cook ◽  
Emileigh K. Greuber ◽  
...  
Keyword(s):  
G Protein ◽  
Hormone Receptor ◽  
Thyrotropin Releasing Hormone ◽  
Receptor Kinase ◽  
G Protein Coupled Receptor ◽  
Releasing Hormone ◽  
G Protein Coupled

scholarly journals Role of G protein-coupled receptor kinase 2 in tumoral angiogenesis

2014 ◽  
Vol 1 (4) ◽  
pp. e969166 ◽  
Author(s):  
Verónica Rivas ◽  
Laura Nogués ◽  
Clara Reglero ◽  
Federico Mayor ◽  
Petronila Penela
Keyword(s):  
G Protein ◽  
Receptor Kinase ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

scholarly journals Regulation of cellular oxidative stress and apoptosis by G protein-coupled receptor kinase-2; The role of NADPH oxidase 4

2016 ◽  
Vol 28 (3) ◽  
pp. 190-203 ◽  
Author(s):  
Tiju Theccanat ◽  
Jennifer L. Philip ◽  
Abdur M. Razzaque ◽  
Nicholas Ludmer ◽  
Jinju Li ◽  
...  
Keyword(s):  
Oxidative Stress ◽  
Nadph Oxidase ◽  
G Protein ◽  
Receptor Kinase ◽  
G Protein Coupled Receptor ◽  
Nadph Oxidase 4 ◽  
G Protein Coupled

scholarly journals Role of Endothelial G Protein-Coupled Receptor Kinase 2 in Angioedema

Hypertension ◽  
2020 ◽  
Vol 76 (5) ◽  
pp. 1625-1636 ◽  
Author(s):  
Jessica Gambardella ◽  
Daniela Sorriento ◽  
Maria Bova ◽  
Mariarosaria Rusciano ◽  
Stefania Loffredo ◽  
...  
Keyword(s):  
Vascular Permeability ◽  
G Protein ◽  
Molecular Mechanisms ◽  
No Production ◽  
Receptor Kinase ◽  
Severe Phenotype ◽  
G Protein Coupled Receptor ◽  
G Protein Coupled

Excessive BK (bradykinin) stimulation is responsible for the exaggerated permeabilization of the endothelium in angioedema. However, the molecular mechanisms underlying these responses have not been investigated. BK receptors are Gq-protein-coupled receptors phosphorylated by GRK2 (G protein-coupled receptor kinase 2) with a hitherto unknown biological and pathophysiological significance. In the present study, we sought to identify the functional role of GRK2 in angioedema through the regulation of BK signaling. We found that the accumulation of cytosolic Ca 2+ in endothelial cells induced by BK was sensitive to GRK2 activity, as it was significantly augmented by inhibiting the kinase. Accordingly, permeabilization and NO production induced by BK were enhanced, as well. In vivo, mice with reduced GRK2 levels in the endothelium (Tie2-CRE/GRK2 fl+/fl − ) exhibited an increased response to BK in terms of vascular permeability and extravasation. Finally, patients with reduced GRK2 levels displayed a severe phenotype of angioedema. Taken together, these findings establish GRK2 as a novel pivotal regulator of BK signaling with an essential role in the pathophysiology of vascular permeability and angioedema.

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