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G protein-coupled receptor kinase 2 (GRK2): mechanisms of regulation and physiological functions [PDF]

FEBS Letters, 1998
G protein‐coupled receptor kinase 2 (GRK2) plays a key role in determining the rate and extent of G protein‐coupled receptor (GPCR) desensitization and resensitization. Recent data indicate that GRK2 activity, subcellular distribution and expression are tightly regulated.
Anna Aragay, Federico Mayor Menendez, P Penela   +2 more
exaly   +3 more sources

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G-Protein-Coupled Receptor Kinase 2 and Hypertension

High Blood Pressure & Cardiovascular Prevention, 2013
Numerous factors partake in the fine-tuning of arterial blood pressure. The heptahelical G-protein-coupled receptors (GPCRs) represent one of the largest classes of cell-surface receptors. Further, ligands directed at GPCRs account for nearly 30 % of current clinical pharmaceutical agents available.
SANTULLI, GAETANO, TRIMARCO, BRUNO, Iaccarino G.   +2 more
openaire   +4 more sources

G protein-coupled receptor kinase 2 (GRK2) in migration and inflammation

Archives of Physiology and Biochemistry, 2008
G protein-coupled receptor kinase 2 (GRK2) is a key modulator of G protein-coupled receptors and other plasma membrane receptors stimulated by chemotactic messengers. On top of that, GRK2 has been reported to interact with a variety of signal transduction proteins related to cell migration such as MEK, Akt, PI3Kgamma or GIT.
Petronila, Penela, Cristina, Murga, Catalina, Ribas, Alicia, Salcedo, María, Jurado-Pueyo, Veronica, Rivas, Ivette, Aymerich, Federico, Mayor   +7 more
openaire   +2 more sources

A role for G protein‐coupled receptor kinase 2 in mechanical allodynia

European Journal of Neuroscience, 2007
AbstractInflammation and nerve injury can both induce mechanical allodynia via mechanisms involving the production of pro‐inflammatory cytokines and increased neuronal activity. Many neurotransmitters involved in pain signal via G protein‐coupled receptors (GPCRs).
Wendy, Kleibeuker, Annemarie, Ledeboer, Niels, Eijkelkamp, Linda R, Watkins, Steven F, Maier, Jitske, Zijlstra, Cobi J, Heijnen, Annemieke, Kavelaars   +7 more
openaire   +2 more sources

Agonist-dependent modulation of G protein-coupled receptor kinase 2 by mitogen-activated protein kinases.

Molecular Pharmacology, 2000
A variety of G protein-coupled receptors (GPCRs) are phosphorylated by G protein-coupled receptor kinase 2 (GRK2). This event promotes the binding of regulatory proteins termed beta-arrestins to GPCRs, leading to uncoupling from G proteins and receptor ...
Ana Elorza, Susana Sarnago, Federico Mayor   +2 more
semanticscholar   +1 more source

Vascular-targeted overexpression of G protein-coupled receptor kinase-2 in transgenic mice attenuates beta-adrenergic receptor signaling and increases resting blood pressure.

Molecular Pharmacology, 2002
Cardiovascular regulation is tightly controlled by signaling through G protein-coupled receptors (GPCRs). beta-Adrenergic receptors (ARs) are GPCRs that regulate inotropy and chronotropy in the heart and mediate vasodilation, which critically influences ...
A. Eckhart, T. Ozaki, H. Tevaearai, H. Rockman, W. Koch   +4 more
semanticscholar   +1 more source

G Protein-Coupled Receptor Kinase 2 in Patients With Acute Myocardial Infarction

The American Journal of Cardiology, 2011
Lymphocyte G protein-coupled receptor kinase 2 (GRK2) levels are increased in patients with chronic heart failure, and in this condition, they correlate with cardiac function. The aim of this study was to assess the prognostic role of GRK2 during acute cardiac dysfunction in humans.
SANTULLI, GAETANO, Campanile A, SPINELLI, LETIZIA, ASSANTE DI PANZILLO, EMILIANO, CICCARELLI, MICHELE, TRIMARCO, BRUNO, Iaccarino G.   +6 more
openaire   +4 more sources

MAP kinase protects G protein-coupled receptor kinase 2 from proteasomal degradation

Biochemical and Biophysical Research Communications, 2005
The G protein-coupled receptor kinase 2 (GRK2) phosphorylates and shuts down signaling from 7-transmembrane receptors (7TMs). Although, receptor activity controls GRK2 expression levels, the underlying molecular mechanisms are poorly understood. We have previously shown that extracellular signal-regulated kinase (ERK1/2) activation increases GRK2 ...
Juliane, Theilade, Jakob L, Hansen, Stig, Haunsø, Søren P, Sheikh   +3 more
openaire   +2 more sources

Role of G Protein–Coupled Receptor Kinase 2 and Arrestins in β-Adrenergic Receptor Internalization

Trends in Cardiovascular Medicine, 1998
G protein-coupled receptors (GPCRs) mediate the action of messengers that are key modulators of the function, growth, and differentiation of cardiac and vascular cells. A general feature of GPCRs is the existence of complex regulatory mechanisms that modulate receptor responsiveness and underlie important physiologic phenomena such as signal ...
F, Mayor, P, Penela, A, Ruiz-Gómez
openaire   +2 more sources

Nerve growth factor stimulation of p42/p44 mitogen-activated protein kinase in PC12 cells: role of G(i/o), G protein-coupled receptor kinase 2, beta-arrestin I, and endocytic processing.

Molecular Pharmacology, 2001
In this study, we have shown that nerve growth factor (NGF)-dependent activation of the p42/p44 mitogen-activated protein kinase (p42/p44 MAPK) pathway in PC12 cells can be partially blocked by pertussis toxin (which inactivates the G proteins G(i/o ...
S. Rakhit, S. Pyne, N. J. Pyne
semanticscholar   +1 more source