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Showing 1 to 13 of 13 for “"GRK2"”.
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NOVEL ROLES FOR GRK2 IN METABOLIC HOMEOSTASIS AND SKELETAL MUSCLE PHYSIOLOGY
… of G protein-coupled receptor kinase 2 (GRK2) in the physiology and pathophysiology of the heart. Adrenergic receptors are the primary target for GRK2 activity in the heart; phosphorylation by GRK2 leads to desensitization of these receptors. As such, levels of GRK2 activity in the heart …
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ROLES OF MAST CELL G PROTEIN-COUPLED RECEPTOR KINASE 2 (GRK2) IN ALLERGY AND INFLAMMATION
… to promote their desensitization. MCs express GRK2 but its role on the regulation of MRGPRX2/B2 and FcRI function has not been studied in detail. For the present study, we generated mice with MC-specific deletion of GRK2 and utilized GRK2 inhibitors to determine if it differentially regulates …
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Regulation G-Protein-gekoppelter Rezeptorkinasen
GRK2 wird an Serin29 durch PKC phosphoryliert. Die Phosphorylierung verhindert die Inhibition der GRK2 durch Calmodulin. Die Inhibition der GRK2 durch Calmodulin wird durch den N-Terminus der GRK2 vermittelt und ist auf eine gestörte Aktivierbarkeit der GRK2 durch G-Protein …
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Development of a Microplate-Based Calcium Assay for Studying Desensitization of the P2Y2 Nucleotide Receptor
… kinase (GRK) family and the β-arrestins. As GRK2 and β-arrestin-1 have been demonstrated to mediate P2Y2R desensitization in rat arterial smooth muscle cells, it was hypothesized that the human homologs would mediate P2Y2R desensitization in human 1321N1 cells. To test this hypothesis, a …
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Identification of the Role of P-Rex1 and its Adaptor Functions in Neutrophils
… to exert this effect. Instead, P-Rex1 binds GRK2, both in vitro and in cells, but does not appear to regulate GRK2 activity. Moreover, P-Rex1 binds GRK2 directly in vitro through its DEP domains, independently of its GEF activity, and the catalytic domain of GRK2 is not essential for this …
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Signal Transduction Mechanisms Mediating the Regulation of Vascular G Protein-Coupled Receptors
… and re-sensitization. GPCR kinase 2 (GRK2) modulates multiple cellular responses through GPCR desensitization and alterations in GRK2 activity are considered to play an important role in the development of hypertension. The main premise of our study was to test whether the inhibition …
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RAF-1 kinase inhibitor protein-mediated cholecystokinin-2 receptor desensitization and extracellular signal-regulated kinase activation
… RKIP association from Raf-1 to GPCR kinase-2 (GRK2) for inhibiting GRK2-mediated G-protein-coupled receptor (GPCR) desensitization. As a member of the GPCR superfamily, Cholecystokinin-2 receptor (CCK2R) is a physiological receptor for gastrin (G17) and activates extracellular signal-regulated …
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Characterization of a Novel Signaling Motif in the CD3 ε Subunit of the T Cell Receptor
… kinase, G protein-coupled receptor kinase 2 (GRK2). Interactions between the BRS and GRK2 contribute to the ability of the TCR to cross talk with G protein-coupled receptors, such as CXCR4. The BRS was also capable of mediating interactions with certain charged phospholipids. To address the …
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Discovery and characterisation of the novel, pathological GNB3 mutation (D153del/ Gβ<sub>3D</sub>), in the retinopathy globe enlarged (rge) chicken
… 255, 255);">3D </sub>protein, the cAMP induced GRK2 phosphorylation activity is significantly altered. Moreover MAPK1 (ERK2) phosphorylation is significantly decreased compared to normal tissues. In contrast human 825TT cell lines expressing the Gβ<sub style="background-color: rgb(255, 255, …
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Phosphorylation Bar Codes Induce Distinct Conformations and Functionalities of beta-Arrestin
… and decreased 50% in one (S246). Depletion of GRK2 or 6 by siRNA indicates that S355, 356 are GRK6 sites whereas the remainder are GRK2 sites. Phosphorylation of GRK2 sites inhibits that of GRK6 sites. Carvedilol, a beta-arrestin biased agonist, promotes phosphorylation of only the GRK6 sites …
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Rhodopsin kinase structure: different nucleotide-binding states and implications for mechanism of activation of a G protein coupled receptor kinase
… kinase C-terminal extension were not resolved in GRK2 and GRK6 structures. The long-term goal of this project was to address this question by structural analysis of rhodopsin kinase (also known as GRK1), which represents a model system for studying phosphorylation-dependent desensitization of …
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Pharmacological insights into C-‐C motif chemokine receptor 5 mediated chemotaxis
… required for CCL3 stimulated monocyte migration. GRK2 and PKC inhibition along with internalisation blockade showed antagonistic effects on the ability of cells to migrate, suggesting arrestin dependent signalling was involved in chemotaxis. Inhibition of dynamin, Grb2 and non-‐receptor tyrosine …
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Identification of A Conserved Cluster In The Rh Domain of Grk Critical For Activation By Gpcrs
… evidence from studies of rhodopsin kinase and GRK2 suggests there is an allosteric docking site for the receptor distinct from the GRK catalytic site. While the agonist-activated GPCR appears crucial for GRK activation, the molecular details of this interaction remain unclear. Recent studies …