G protein-coupled receptor kinase 2 (GRK2) as a multifunctional signaling hub. [PDF]
Cell Mol Life Sci, 2019 Accumulating evidence indicates that G protein-coupled receptor kinase 2 (GRK2) is a versatile protein that acts as a signaling hub by modulating G protein-coupled receptor (GPCR) signaling and also via phosphorylation or scaffolding interactions with an extensive number of non-GPCR cellular partners. GRK2 multifunctionality arises from its multidomain
Penela P +3 more
europepmc +7 more sources
Mitochondrial accumulation of GRK2 as a protective mechanism against hypoxia-induced endothelial dysfunction [PDF]
Cell Death DiscoveryHypoxia, a condition characterized by a temporary lack of oxygen, causes mitochondrial damage, which in turn leads to endothelial dysfunction. G-protein-coupled receptor kinase 2 (GRK2) plays a key role in vascular homeostasis and remodeling, influencing
Cristina Gatto +17 more
doaj +2 more sources
G Protein-Coupled Receptor Kinase 5 (GRK5) Modulates Nociceptin/Orphanin FQ Opioid (NOP) Receptor Desensitization in Rat Sympathetic Neurons. [PDF]
J Neurosci ResABSTRACT Stimulation of nociceptin/orphanin FQ peptide (NOP) opioid receptors by the endogenous ligand nociceptin (Noc) leads to voltage‐gated Ca2+ channel inhibition or G protein inwardly rectifying K+ channel activation. One mechanism of G protein‐coupled receptor (GPCR) desensitization occurs when G protein‐coupled receptor kinases (GRK ...
Farrag M +6 more
europepmc +2 more sources
G Protein-Coupled Receptor Kinase 2 (GRK2) and 5 (GRK5) Exhibit Selective Phosphorylation of the Neurotensin Receptor in Vitro. [PDF]
Biochemistry, 2015 G protein-coupled receptor kinases (GRKs) play an important role in the desensitization of G protein-mediated signaling of G protein-coupled receptors (GPCRs). The level of interest in mapping their phosphorylation sites has increased because recent studies suggest that the differential pattern of receptor phosphorylation has distinct biological ...
Inagaki S +7 more
europepmc +4 more sources
G protein-coupled receptor kinase 2 (GRK2) modulation and cell cycle progression. [PDF]
Proc Natl Acad Sci U S A, 2010 Cell cycle progression requires changes in the activity or levels of a variety of key signaling proteins. G protein–coupled receptor kinase 2 (GRK2) plays a central role in G protein–coupled receptor regulation. Recent research is uncovering its involvement in additional cellular functions, but the potential role of GRK2 in the cell cycle has not been ...
Penela P, Rivas V, Salcedo A, Mayor F.
europepmc +4 more sources
Overlapping and opposing functions of G protein-coupled receptor kinase 2 (GRK2) and GRK5 during heart development. [PDF]
J Biol Chem, 2014 G protein-coupled receptor kinases 2 (GRK2) and 5 (GRK5) are fundamental regulators of cardiac performance in adults but are less well characterized for their function in the hearts of embryos. GRK2 and -5 belong to different subfamilies and function as competitors in the control of certain receptors and signaling pathways.
Philipp M, Berger IM, Just S, Caron MG.
europepmc +4 more sources
The RAF Kinase Inhibitor Protein (RKIP): Good as Tumour Suppressor, Bad for the Heart
Cells, 2022 The RAF kinase inhibitor protein, RKIP, is a dual inhibitor of the RAF1 kinase and the G protein-coupled receptor kinase 2, GRK2. By inhibition of the RAF1-MAPK (mitogen-activated protein kinase) pathway, RKIP acts as a beneficial tumour suppressor.
Joshua Abd Alla, Ursula Quitterer
doaj +1 more source
eLife, 2021 G protein-coupled receptors (GPCRs) transmit extracellular signals to the inside by activation of intracellular effector proteins. Different agonists can promote differential receptor-induced signaling responses – termed bias – potentially by eliciting ...
Anja Flöser +6 more
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Desensitization and internalization of endothelin receptor A: impact of G protein-coupled receptor kinase 2 (GRK2)-mediated phosphorylation. [PDF]
J Biol Chem, 2013 Endothelin receptor A (ETA), a G protein-coupled receptor, mediates endothelin signaling, which is regulated by GRK2. Three Ser and seven Thr residues recently proven to be phosphoacceptor sites are located in the C-terminal extremity (CTE) of the receptor following its palmitoylation site. We created various phosphorylation-deficient ETA mutants.
Gärtner F +4 more
europepmc +4 more sources
The β-blocker Nebivolol Is a GRK/β-arrestin Biased Agonist [PDF]
, 2013 Nebivolol, a third generation β-adrenoceptor (β-AR) antagonist (β-blocker), causes vasodilation by inducing nitric oxide (NO) production. The mechanism via which nebivolol induces NO production remains unknown, resulting in the genesis of much of the ...
Andresen, Bradley T. +9 more
core +16 more sources