Property Summary

NCBI Gene PubMed Count 176
PubMed Score 411.47
PubTator Score 385.46

Knowledge Summary

Patent (12,829)

Expression

  Differential Expression (7)

Disease log2 FC p
psoriasis 2.500 1.9e-05
osteosarcoma 2.176 1.5e-10
medulloblastoma, large-cell 1.200 1.3e-05
diabetes mellitus -1.100 1.1e-03
subependymal giant cell astrocytoma -1.209 5.0e-02
COPD -1.300 5.1e-04
ovarian cancer 1.400 3.3e-13

MLP Assay (14)

AID Type Active / Inconclusive / Inactive Description
488806 screening 16 / 0 / 1977 RNA aptamer-based validation for inhibitors of GRK2
488847 screening 1924 / 0 / 326127 RNA aptamer-based HTS for inhibitors of GRK2
488855 summary 0 / 0 / 0 Summary Report: RNA aptamer-based HTS for inhibitors of GRK2
504451 screening 79 / 0 / 1911 Confirmation of RNA aptamer-based HTS for inhibitors of GRK2, Cherry Pick 1
504500 confirmatory 21 / 0 / 90 Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 1
504782 screening 8 / 0 / 354 Confirmation of RNA aptamer-based HTS for inhibitors of GRK2, Cherry Pick 2
504815 confirmatory 2 / 0 / 23 Dose Response of inhibitors of GRK2 binding with RNA aptamer, Cherry Pick 2
588428 other 1 / 0 / 10 Thermofluor assay to identify compounds that bind to GRK2 and inhibit kinase activity, Set 1
588465 other 0 / 0 / 11 Kinase assay to identify compounds that inhibit phosphorylation of rhodopsin by GRK2, Set 1
588468 other 6 / 0 / 18 Thermofluor assay to identify compounds that bind to GRK2 and inhibit kinase activity, Set 2
More...

Gene RIF (124)

PMID Text
26706289 Acute mental stress significantly increased GRK2 density in in peripheral blood mononuclear cells of young adult males.
26670611 the dual-specific GRK2 and ERK cascade inhibitor, RKIP (Raf kinase inhibitor protein), triggered dysfunctional cardiomyocyte energetics and the expression of heart failure-promoting Pparg-regulated genes.
26447102 It plays a role in progression of Vasculature which is affected by insulin resistance and type 2 diabetes expresses high levels of GRK2
26402907 Data suggest that, by targeting/repressing GRK2, microRNA-K3 of Kaposi sarcoma-associated herpesvirus (KSHV) facilitates migration and invasion of vascular endothelial cells via activation of CXCR2/AKT signaling.
26248277 Suggest a common regulatory pattern for the beta(2)-AR/GRK2 which is independent of cellular type or pathology.
26234354 It is a critical factor in diabetic endothelial dysfunction and plays a role in many physiological functions including regulation of G-protein-coupled receptors (GPCRs). (review)
26224342 Suggest role for GRK2 in the regulating cardiac hypertrophy.
26092485 Acute aerobic exercise induces a greater GRK2 expression in women than men, while increased cardiorespiratory fitness is associated with exercise-induced GRK2 expression in PBMCs
25982117 G protein beta subunits (Gb) bind to DDB1 and Gb2 targets GRK2 for ubiquitylation by the DDB1-CUL4A-ROC1 ubiquitin ligase.
25857770 Data indicate that protein kinase GRK2 silencing abolished isoproterenol-induced phosphorylation of beta2-adrenergic receptor (beta2ARs).
25316767 Results uncovered that Gaq binding to GRK2 enhances the recruitment of GRK2 to M3-ACh receptors.
25279970 Knockdown of ADRBK1 gene has detrimental effects on breast cancer cell growth.
25049229 Data indicate that residues on the G-protein coupled receptor kinase 2 (GRK2) N terminus and kinase domain extension collaborate to create a G protein-coupled receptor (GPCR) docking site.
24904059 These data demonstrate that GRK2 modulates FcinRI signaling in mast cells via at least two mechanisms.One involves GRK2-RH and modulates tyrosine phosphorylation of Syk, and the other is mediated via the phosphorylation of p38 and Akt.
24812353 This review discusses recently discovered roles of GRK2 as a biomarker in cardiomyocyte metabolism and myocardial contraction.
24702056 A thorough understanding of the functions of GRK2 in the heart is necessary in order to finalize it as a candidate for drug development.
24613411 Low levels of GRK2/GRK5 causes a slow and not complete desensitization/down-regulation of GPR17.
24465168 The gene expression levels of TREM1 in PMNs isolated from patients with bacterial infections may be used as a surrogate biomarker for determining the severity.
24169548 This study showed that, among GRK2, beta-arrestin 1, and beta-arretin 2, beta-arrestin 1 and GRK2 seem to have a role in modulating GH secretion during somatostatin analog treatment.
24135140 decreased endothelial Grk2 dosage accelerated tumor growth, along with reduced pericyte vessel coverage and enhanced macrophage infiltration, and this transformed environment promoted decreased GRK2 in breast cancer vessels
24064210 Desensitization and internalization of endothelin receptor A: impact of G protein-coupled receptor kinase 2 (GRK2)-mediated phosphorylation.
23904266 GRK2 is localized to centrosomes and plays a central role in mitogen-promoted centrosome separation.
23734232 Data indicate that CXCL12-induced phosphorylation at CXCR4 S346/347 was mediated by GRK2/3.
23705503 this study provides evidence that GRK2 mediates phosphorylation-independent mGluR5 desensitization via the interaction between the RGS domain and Galphaq in HEK 293 cells.
23689525 Changes in lymphocyte GRK2 after exercise training can strongly predict outcome in advanced heart failure.
23494575 This study identify that GRK2 as a potential molecular link between inflammation and mGluR-mediated sensitization.
23467820 Increased localization is seen in heart mitochondria from cardiac-specific GRK2 transgenic mice compared with normal littermate controls.
23460259 We further detected that reduced level of GRK2 induced a small cell cycle arrest at G2/M phase by enhancing the expression of cyclin A, B1, and E
23362259 Inhibition of G-protein-coupled receptor kinase 2 (GRK2) triggers the growth-promoting mitogen-activated protein kinase (MAPK) pathway
23312955 GRK2 takes part in the regulation of the initial inflammatory response during mycobacterial infection.
23221335 a novel role for IL-8 in inhibiting betaAR agonist-stimulated alveolar epithelial fluid transport via GRK2/PI3K-dependent mechanisms.
23208013 Gene transfer of human GRK2 inhibitory peptide preserved regional/global systolic function after acute MI without arresting progressive ventricular remodeling.
23139825 These data suggest cell type- and subcellular compartment-dependent differences in GRK/arrestin-mediated desensitization and signaling.
23082996 Data suggest that specific serine/threonine residues in DRD2 (dopamine receptor D2) are involved in regulation of DRD2 endocytosis by GRK2 and GASP1 (G protein-coupled receptor associated sorting protein 1).
23076141 GRK2 dynamically associates with and phosphorylates HDAC6 to stimulate its alpha-tubulin deacetylase activity at specific cellular localizations such as the leading edge of migrating cells, thus promoting local tubulin deacetylation and enhanced motility.
23029581 The authors found that GRK2 participates in multiple distinct steps of the flavivirus life cycle by promoting both entry and RNA synthesis.
22735336 GRK2 exerts a strong negative effect on beta-arrestin-dependent signaling through its competition with GRK5 and GRK6 for receptor phosphorylation
22731384 Persistent hyperalgesia in GRK2-deficient mice is associated with an increase in spinal cord microglia/macrophages.
22589388 GRK2-HDAC6 functional interaction may have important implications in pathological contexts related to epithelial cell migration
22375000 These data show that NPFF-induced heterologous desensitization of MOP receptor signaling is mediated by GRK2 and could involve transphosphorylation within the heteromeric receptor complex.
22196842 Increased GRK2 correlates with clinical severity using the INTERMACS scale and LV stroke volume, supporting it as a potential target in advanced heart failure.
22193721 find that a balanced, GRK2/HDAC6-mediated regulation of tubulin acetylation differentially modulates the early and late stages of cellular spreading
22089113 in preeclamptic or gestational hypertensive women, elevated GRK2 levels in the umbilical vasculature is correlated to elevated blood pressure levels, with a likely compensatory rather than causative role
21983013 The data show a novel sub-cellular localization of GRK2 in the mitochondria and an unexpected role in regulating mitochondrial biogenesis and ATP generation.
21952200 betaarr2 competes with GRK2 for interaction with the activated and GRK phosphorylated GLP-1R, suggesting a new role of betaarr2 in regulating the orchestration of GRK2 functionality
21784156 A reduced cortical concentration of GRK2 in schizophrenia (resembling that in aging) may result in altered G protein-dependent signaling, thus contributing to prefrontal deficits in schizophrenia.
21705320 GRK2 induces desensitization of H2R through a phosphorylation-independent and RGS-dependent mechanism
21473908 GRK2 is a key regulator of the transition from acute to chronic inflammatory pain. Review.
21464134 Regulation of the epithelial Na+ channel by the RH domain of G protein-coupled receptor kinase, GRK2, and Galphaq/11.
21283592 elevated levels of MIF are associated with cardiac dysfunction in diabetic patients, and the MIF effects are mediated by GRK2
21127457 An ADRBK1 SNP (rs1894111 G>A) showed a signal for association with systolic and diastolic blood pressure response to hydrochlorothiazide in Whites.
21081496 The ability of beta-arrestins to play different scaffold functions would allow coordination of both Mdm2-dependent and -independent processes aimed at the specific modulation of GRK2 turnover in different signaling contexts
20814022 Apoptosis and myocardial ischemia/reperfusion injury are found to be dependent on level of G protein-coupled receptor kinase-2.
20807772 desensitization of the dopamine D1-D2 receptor heteromer-mediated signal can occur by agonist occupancy even without activation and is dually regulated by both the catalytic and RGS domains of GRK2.
20730384 Studies seem to indicate that mild, soluble, Beta-amyloid accumulation can lead to a reduced membrane (functional) and an elevated cytosolic GRK2/5.
20696855 The RET combination analysis revealed that stimulation of the alpha(2A)-adrenergic receptor (alpha(2A)AR) leads to the recruitment of GRK2 at a receptor still associated with the Galpha(i1)beta(1)gamma(2) complex.
20684281 Elevation of lymphocyte GRK2 levels in chronic heart failure is associated with heart ejection fraction.
20628086 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
20627936 GRK2 is an important negative regulator of insulin effects, key to the etiopathogenesis of insulin resistance and obesity.
20501412 Metoprolol can inhibit the expression of GRK2 in lymphocyte of advanced elderly patients with chronic heart failure.
20493668 findings indicated that platelet GRK2 and p-Ser670 GRK2 were reduced (36-41%) in unmedicated major depressive disorder subjects, and GRK2 content correlated inversely with the severity of depression
20468064 Observational study of gene-disease association. (HuGE Navigator)
20460384 The agonist-induced internalization of GPR109A receptors is regulated by GRK2 and arrestin3 in a pertussis toxin-sensitive manner and that internalized receptor recycling is independent of endosomal acidification.
20443948 lymphocyte GRK2 levels are low after heart transplantation
20443852 Enhanced GRK2 expression and desensitization of betaAR vasodilatation in hypertensive patients.
20335112 Increased GRK2 gene expression may play an important role in cardiac dysfunction in diabetes.
20080565 Prevention of GRK2 phosphorylation at S670 impedes normal GRK2 down-regulation and markedly delays cell cycle progression
19913121 Observational study of gene-disease association. (HuGE Navigator)
19906838 In cells overexpressing G protein-coupled receptor kinase 2 (GRK2), the thyrotropin-releasing hormone receptor is not phosphorylated.
19846537 Data show that GRK2 stimulates the desensitization of GPR54 in HEK 293 cells and that beta-arrestin-2 mediates GPR54 activation of ERK1/2 in MDA-MB-231 cells.
19815545 G protein-coupled receptor kinase-2 constitutively regulates D2 dopamine receptor expression and signaling independently of receptor phosphorylation
19620130 GRK2 mediates adrenergic insulin resistance and inhibition of GRK2 activity leads to increased insulin sensitivity both in cells and in animal model of insulin resistance.
19487588 Data suggest that GRK2, but not GRK5, is correlated with increasing blood pressure in black Americans.
19400979 In the brain of bipolar disorder patients there were not a significant difference in the GRK2 level.
19338266 the kinase large lobe and carboxyl-terminal tail have roles in GRK2 activation by receptors
19306925 These results establish RalA and GRK2 as key regulators of LPA receptor signalling and demonstrate for the first time that LPA(1) activity facilitates the formation of a novel protein complex between these two proteins.
19292735 GRK2 immunoreactivity were found in vulnerable neurons of AD patients as well as in a two-vessel occlusion (2-VO) mammalian model of ischaemia.
19257866 Heterozygous variant of Ser49Gly of ADRBK1 can be considered as one of genetic predictors of development of how primary and secondary AF.
18976975 Knockdown of adrenergic, beta, receptor kinase 1 (ADRBK1) by siRNA inhibits the early stages of HIV-1 replication in 293T cells infected with VSV-G pseudotyped HIV-1
18854154 Knockdown of adrenergic, beta, receptor kinase 1 (ADRBK1) by siRNA inhibits the early stages of HIV-1 replication in 293T cells infected with VSV-G pseudotyped HIV-1
18511496 Histamine stimulates phospholipase C-signaling in myometrial smooth muscle cells through H(1) histamine receptors and that GRK2 recruitment is a key mechanism in the regulation of H(1) histamine receptor signaling in human uterine smooth muscle.
18463167 EGF transregulates opioid receptors through EGFR-mediated tyrosyl phosphorylation and activation of GRK2; GRK2 may be a mediator of cross-talk from RTK to GPCR signaling pathway
18451066 GRK2 reduced cell proliferation revealing a new role for this kinase in the growth of thyroid cancers.
18425130 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
18369319 Regulator of coordinated integrin and G-protein-coupled receptor-directed epithelial cell migration.
17998459 Mechanical unloading leads to complete reversal in PI3Kgamma and betaARK1-associated PI3K activation. Furthermore, displacement of active PI3K from betaARK1 restores betaAR responsiveness in failing myocytes.
17544362 GRK2 interacts not only with epithelial Na(+) channels, but also with both Nedd4 and Nedd4-2.
17482545 findings show in tissues that S-nitrosothiols (SNOs) increase beta-adrenergic receptor (beta-AR) expression and prevent agonist-stimulated receptor
17276003 Our preliminary data suggest that GRK2 is involved in GPCRs coupling dysfunction observed in AD patients.
17256744 Our data suggest that in cirrhosis-induced vasodilation, the AT1-R is desensitized by GRK-2 and beta-arrestin-2 and that changed patterns of phosphorylated Ca(2+) sensitizing proteins decrease Ca(2+) sensitivity.
17146290 Our studies indicate that GRK2 is a novel component of neuronal and glial fibrillary tau deposits with no preference in tau isoform binding. GRK2 may play a role in hyperphosphorylation of tau in tauopathies.
17102134 interaction of DREAM with GRK6 and GRK2, members of the G protein-coupled receptor kinase family of proteins, and their phosphorylation of DREAM
17055984 Phosphorylation of p38 by GRK2 at the docking groove unveils a novel mechanism for inactivating p38MAPK.
17008309 analysis of the G protein-coupled receptor kinase and beta-arrestin-mediated desensitization of the angiotensin II type 1A receptor
17006543 insulin-like growth factor-1 alters Mdm2-mediated GRK2 degradation, leading to enhanced GRK2 stability and increased kinase levels
17000469 Overexpression of GRK2 in Alzheimer disease.
16984558 Decreased expression of GRK2 is associated with obstructed bladder
16920721 clathrin has a role in phosphorylation and internalization of beta2-adrenergic receptor by GRK2
16849637 High expression was detected in septic neutrophils and control cells treated with cytokines plus LPS.
16725308 Our results suggest a feedback mechanism by which phosphorylation of GRK2 by c-Src increases both GRK2 kinase activity towards GPCRs and its specific interaction with Galphaq subunits.
16605244 The presence of the alpha(2C)AR within the heterodimer resulted in a marked reduction in the level of GRK2-mediated alpha(2A)AR phosphorylation, which was accompanied by a qualitative attenuation of beta-arrestin recruitment.
16356165 The effect of PDE4 on the of action of PKA on GRK2 phosphorylation and transport is reported.
16121194 identification of the protein G-coupled receptor kinase 2 (GRK2), a kinase involved in the desensitization of G protein-coupled receptors (GPCR), as a downstream target and regulator of the TGFbeta-signaling cascade
16081410 GRK2-as5 has a role in membrane trafficking of the mu-opioid receptor
16077899 Overall, these data suggest that GRK2 has a regulatory role in EGF-induced ERK/MAPK activation.
15919661 the uncoupling and endocytosis of 5-HT4R require different GRK2 concentrations and involve distinct molecular events
15870073 kinase binding to an mGluR1 domain involved in G protein-coupling is essential for the phosphorylation-independent attenuation of signaling by GRK2
15843435 Ezrin is a novel substrate of GRK2
15778405 in leukocytes from patients with active relapsing-remitting multiple sclerosis (MS) or with secondary progressive MS, GRK2 levels are significantly reduced
15653687 GRK2 binding is critical not only for alpha2A-adrenergic receptor phosphorylation but also for full activity of the kinase.
15618519 beta-Arrestin 2 and GRK2 are potential mediators of signaling by activated Smoothened
15542600 role in terminating histamine H1 receptor singnaling by the kinase activity and RGS function of GRK2
15471870 analysis of the GRK2 binding site of Galphaq
15271984 GPRK2-mediated PDGFRbeta seryl phosphorylation plays an important role in desensitizing PDGFRbeta; this desensitization involves GPRK2-mediated phosphorylation of PDGFRbeta Ser(1104), with consequent dissociation of the PDGFRbeta from NHERF
15097244 The concentration of betaARK1 in lymphocytes is greater in hypertensive individuals with left ventricular hypertrophy than in those without it
14557268 GRK2 (and also GRK3, GRK5, and GRK6) is stabilized by interaction with Hsp90; GRK2 degradation induced by geldanamycin was predominantly through the proteasome pathway
12750365 GRK2 requires agonist-induced formation of opioid receptor-G protein-coupled receptor kinase (GRK)-G beta gamma complex on the membrane in order to function
12679936 The pleckstsrin homology domain of this protein binds to PKC and affects the activity of PKC kinase.
12624098 PDEG functions to link c-Src and G-protein-coupled receptor kinase 2 in a signaling unit that regulates p42/p44 mitogen-activated protein kinase by epidermal growth factor
12552191 GRK2 is potential marker for organ injury and survival after cardiopulmonary bypass
12486133 identification of the amino-terminal domain as a regulatory Gbeta gamma binding site
12456365 GRK2 plays a negative feedback regulatory role on protein kinase C(PKC)beta 1 activity in interaction between GRK2 and PKCbeta 1.
12435819 a direct correlation between the expression of GRK2 and the desensitization of natively expressed H2 receptors in U-937 cells
12379128 GRK2-phosphorylated recombinant ribosomal protein P2 reconstitutes translational activity of 60S ribosomal subunits and represents a potential novel signaling pathway responsible for P2 phosphorylation.

AA Sequence

MADLEAVLADVSYLMAMEKSKATPAARASKKILLPEPSIRSVMQKYLEDRGEVTFEKIFSQKLGYLLFRD      1 - 70
FCLNHLEEARPLVEFYEEIKKYEKLETEEERVARSREIFDSYIMKELLACSHPFSKSATEHVQGHLGKKQ     71 - 140
VPPDLFQPYIEEICQNLRGDVFQKFIESDKFTRFCQWKNVELNIHLTMNDFSVHRIIGRGGFGEVYGCRK    141 - 210
ADTGKMYAMKCLDKKRIKMKQGETLALNERIMLSLVSTGDCPFIVCMSYAFHTPDKLSFILDLMNGGDLH    211 - 280
YHLSQHGVFSEADMRFYAAEIILGLEHMHNRFVVYRDLKPANILLDEHGHVRISDLGLACDFSKKKPHAS    281 - 350
VGTHGYMAPEVLQKGVAYDSSADWFSLGCMLFKLLRGHSPFRQHKTKDKHEIDRMTLTMAVELPDSFSPE    351 - 420
LRSLLEGLLQRDVNRRLGCLGRGAQEVKESPFFRSLDWQMVFLQKYPPPLIPPRGEVNAADAFDIGSFDE    421 - 490
EDTKGIKLLDSDQELYRNFPLTISERWQQEVAETVFDTINAETDRLEARKKAKNKQLGHEEDYALGKDCI    491 - 560
MHGYMSKMGNPFLTQWQRRYFYLFPNRLEWRGEGEAPQSLLTMEEIQSVEETQIKERKCLLLKIRGGKQF    561 - 630
ILQCDSDPELVQWKKELRDAYREAQQLVQRVPKMKNKPRSPVVELSKVPLVQRGSANGL               631 - 689
//

Text Mined References (180)

PMID Year Title
26706289 2016 G protein-coupled receptor kinase-2 in peripheral blood mononuclear cells following acute mental stress.
26670611 2016 Inhibition of G-protein-coupled Receptor Kinase 2 Prevents the Dysfunctional Cardiac Substrate Metabolism in Fatty Acid Synthase Transgenic Mice.
26447102 2015 G-protein-coupled receptor kinase 2 and endothelial dysfunction: molecular insights and pathophysiological mechanisms.
26402907 2015 A KSHV microRNA Directly Targets G Protein-Coupled Receptor Kinase 2 to Promote the Migration and Invasion of Endothelial Cells by Inducing CXCR2 and Activating AKT Signaling.
26248277 2015 ?2- and ?1-Adrenoceptor Expression Exhibits a Common Regulatory Pattern With GRK2 and GRK5 in Human and Animal Models of Cardiovascular Diseases.
26234354 2015 [The Role of GRK2 and Its Potential as a New Therapeutic Target in Diabetic Vascular Complications].
26224342 2015 Integrating GRK2 and NFkappaB in the Pathophysiology of Cardiac Hypertrophy.
26092485 2015 Acute aerobic exercise mediates G protein-coupled receptor kinase 2 expression in human PBMCs.
25982117 2015 A Non-Canonical Function of G? as a Subunit of E3 Ligase in Targeting GRK2 Ubiquitylation.
25857770 2015 Membrane-permeable tastants amplify ?2-adrenergic receptor signaling and delay receptor desensitization via intracellular inhibition of GRK2's kinase activity.
25316767 2015 Influence of g?q on the dynamics of m3-acetylcholine receptor-g-protein-coupled receptor kinase 2 interaction.
25279970 2014 si-RNA-Mediated Silencing of ADRBK1 Gene Attenuates Breast Cancer Cell Proliferation.
25049229 2014 Mapping the putative G protein-coupled receptor (GPCR) docking site on GPCR kinase 2: insights from intact cell phosphorylation and recruitment assays.
24904059 2014 Regulation of Fc?RI signaling in mast cells by G protein-coupled receptor kinase 2 and its RH domain.
24812353 2014 G protein-coupled receptor kinase 2: a link between myocardial contractile function and cardiac metabolism.
24702056 2014 GRK2 in the heart: a GPCR kinase and beyond.
24613411 2014 Does GRK-? arrestin machinery work as a "switch on" for GPR17-mediated activation of intracellular signaling pathways?
24465168 2014 Gene expression analysis of TREM1 and GRK2 in polymorphonuclear leukocytes as the surrogate biomarkers of acute bacterial infections.
24169548 2013 ?-Arrestin 1 and 2 and G protein-coupled receptor kinase 2 expression in pituitary adenomas: role in the regulation of response to somatostatin analogue treatment in patients with acromegaly.
24135140 2013 Developmental and tumoral vascularization is regulated by G protein-coupled receptor kinase 2.
24064210 2013 Desensitization and internalization of endothelin receptor A: impact of G protein-coupled receptor kinase 2 (GRK2)-mediated phosphorylation.
23904266 2013 G protein-coupled receptor kinase 2 (GRK2) is localized to centrosomes and mediates epidermal growth factor-promoted centrosomal separation.
23734232 2013 Hierarchical organization of multi-site phosphorylation at the CXCR4 C terminus.
23705503 [Phosphorylation-independent desensitization of metabotropic glutamate receptor 5 by G protein-coupled receptor kinase 2 in HEK 293 cells].
23689525 2014 Reduction of lymphocyte G protein-coupled receptor kinase-2 (GRK2) after exercise training predicts survival in patients with heart failure.
23494575 2013 G protein-coupled receptor kinase 2 and group I metabotropic glutamate receptors mediate inflammation-induced sensitization to excitotoxic neurodegeneration.
23467820 2013 Prodeath signaling of G protein-coupled receptor kinase 2 in cardiac myocytes after ischemic stress occurs via extracellular signal-regulated kinase-dependent heat shock protein 90-mediated mitochondrial targeting.
23460259 2013 GRK2 negatively regulates IGF-1R signaling pathway and cyclins' expression in HepG2 cells.
23362259 2013 Inhibition of G-protein-coupled receptor kinase 2 (GRK2) triggers the growth-promoting mitogen-activated protein kinase (MAPK) pathway.
23312955 2013 Epithelial G protein-coupled receptor kinases regulate the initial inflammatory response during mycobacterial infection.
23221335 2013 IL-8 inhibits cAMP-stimulated alveolar epithelial fluid transport via a GRK2/PI3K-dependent mechanism.
23208013 2013 MCARD-mediated gene transfer of GRK2 inhibitor in ovine model of acute myocardial infarction.
23186163 2013 Toward a comprehensive characterization of a human cancer cell phosphoproteome.
23139825 2012 Distinct cellular and subcellular distributions of G protein-coupled receptor kinase and arrestin isoforms in the striatum.
23082996 2013 ARF6 and GASP-1 are post-endocytic sorting proteins selectively involved in the intracellular trafficking of dopamine D? receptors mediated by GRK and PKC in transfected cells.
23076141 The interplay between G protein-coupled receptor kinase 2 (GRK2) and histone deacetylase 6 (HDAC6) at the crossroads of epithelial cell motility.
23029581 2012 G protein-coupled receptor kinase 2 promotes flaviviridae entry and replication.
22735336 2012 Competing G protein-coupled receptor kinases balance G protein and ?-arrestin signaling.
22731384 2012 MicroRNA-124 as a novel treatment for persistent hyperalgesia.
22589388 2012 Roles of GRK2 in cell signaling beyond GPCR desensitization: GRK2-HDAC6 interaction modulates cell spreading and motility.
22447027 2012 Bidirectional regulation of neutrophil migration by mitogen-activated protein kinases.
22375000 2012 GRK2 protein-mediated transphosphorylation contributes to loss of function of ?-opioid receptors induced by neuropeptide FF (NPFF2) receptors.
22196842 2012 Myocardial G protein receptor-coupled kinase expression correlates with functional parameters and clinical severity in advanced heart failure.
22193721 2012 A novel GRK2/HDAC6 interaction modulates cell spreading and motility.
22089113 2012 GRK2 levels in umbilical arteries of pregnancies complicated by gestational hypertension and preeclampsia.
21983013 2012 Mitochondrial localization unveils a novel role for GRK2 in organelle biogenesis.
21952200 2011 Beta-arrestin2 as a competitor for GRK2 interaction with the GLP-1 receptor upon receptor activation.
21784156 2011 Reduced expression of G protein-coupled receptor kinases in schizophrenia but not in schizoaffective disorder.
21705320 2011 Roles of phosphorylation-dependent and -independent mechanisms in the regulation of histamine H2 receptor by G protein-coupled receptor kinase 2.
21473908 2011 Microglial GRK2: a novel regulator of transition from acute to chronic pain.
21464134 2011 Regulation of the epithelial Na+ channel by the RH domain of G protein-coupled receptor kinase, GRK2, and Galphaq/11.
21283592 2011 Hyperglycemic myocardial damage is mediated by proinflammatory cytokine: macrophage migration inhibitory factor.
21269460 2011 Initial characterization of the human central proteome.
21127457 2011 Polymorphisms in genes coding for GRK2 and GRK5 and response differences in antihypertensive-treated patients.
21081496 2011 Multiple scaffolding functions of {beta}-arrestins in the degradation of G protein-coupled receptor kinase 2.
20814022 2010 Level of G protein-coupled receptor kinase-2 determines myocardial ischemia/reperfusion injury via pro- and anti-apoptotic mechanisms.
20807772 2010 Dopamine D1-D2 receptor Heteromer-mediated calcium release is desensitized by D1 receptor occupancy with or without signal activation: dual functional regulation by G protein-coupled receptor kinase 2.
20730384 2010 Dysfunction of G protein-coupled receptor kinases in Alzheimer's disease.
20696855 2010 Combining resonance energy transfer methods reveals a complex between the alpha2A-adrenergic receptor, Galphai1beta1gamma2, and GRK2.
20684281 2010 [Lymphocyte GRK2 expression of the very elderly with chronic heart failure].
20628086 2010 Variation at the NFATC2 locus increases the risk of thiazolidinedione-induced edema in the Diabetes REduction Assessment with ramipril and rosiglitazone Medication (DREAM) study.
20627936 2010 G protein-coupled receptor kinase 2 plays a relevant role in insulin resistance and obesity.
20501412 2010 [Effect of metoprolol on the expression of GRK2 in lymphocyte of advanced elderly patients with chronic heart failure].
20493668 2010 Reduced platelet G protein-coupled receptor kinase 2 in major depressive disorder: antidepressant treatment-induced upregulation of GRK2 protein discriminates between responder and non-responder patients.
20468064 2010 Association study of 182 candidate genes in anorexia nervosa.
20460384 2010 Internalization of the human nicotinic acid receptor GPR109A is regulated by G(i), GRK2, and arrestin3.
20443948 2010 Dynamic changes in lymphocyte GRK2 levels in cardiac transplant patients: a biomarker for left ventricular function.
20443852 2008 Enhanced GRK2 expression and desensitization of betaAR vasodilatation in hypertensive patients.
20335112 2010 [High glucose up-regulates GRK2 gene expression in H9C2 cardiomyoblasts in vitro].
20080565 2010 G protein-coupled receptor kinase 2 (GRK2) modulation and cell cycle progression.
20074556 2010 Function of the cytoplasmic tail of human calcitonin receptor-like receptor in complex with receptor activity-modifying protein 2.
19946888 2010 Defining the membrane proteome of NK cells.
19913121 2009 Gene-centric association signals for lipids and apolipoproteins identified via the HumanCVD BeadChip.
19906838 2010 Role of helix 8 of the thyrotropin-releasing hormone receptor in phosphorylation by G protein-coupled receptor kinase.
19846537 2009 Regulation of GPR54 signaling by GRK2 and {beta}-arrestin.
19815545 2009 G protein-coupled receptor kinase-2 constitutively regulates D2 dopamine receptor expression and signaling independently of receptor phosphorylation.
19620130 2009 The G protein coupled receptor kinase 2 plays an essential role in beta-adrenergic receptor-induced insulin resistance.
19487588 2009 G protein-coupled receptor kinase 2 expression and activity are associated with blood pressure in black Americans.
19400979 2009 Decreased GRK3 but not GRK2 expression in frontal cortex from bipolar disorder patients.
19338266 2009 GRK2 activation by receptors: role of the kinase large lobe and carboxyl-terminal tail.
19306925 2009 Dual regulation of lysophosphatidic acid (LPA1) receptor signalling by Ral and GRK.
19292735 2009 Insights into cerebrovascular complications and Alzheimer disease through the selective loss of GRK2 regulation.
19257866 2009 [Genetics of atrial fibrillation].
18511496 2008 Selective regulation of H1 histamine receptor signaling by G protein-coupled receptor kinase 2 in uterine smooth muscle cells.
18463167 2008 EGF transregulates opioid receptors through EGFR-mediated GRK2 phosphorylation and activation.
18451066 2008 Immunohistochemical detection, regulation and antiproliferative function of G-protein-coupled receptor kinase 2 in thyroid carcinomas.
18425130 2008 A GRK5 polymorphism that inhibits beta-adrenergic receptor signaling is protective in heart failure.
18369319 2008 G protein-coupled receptor kinase 2 positively regulates epithelial cell migration.
18088087 2008 Phosphoproteome of resting human platelets.
17998459 2007 Dynamic regulation of phosphoinositide 3-kinase-gamma activity and beta-adrenergic receptor trafficking in end-stage human heart failure.
17986524 2008 Characterization of G-protein coupled receptor kinase interaction with the neurokinin-1 receptor using bioluminescence resonance energy transfer.
17544362 2007 GRK2 interacts with and phosphorylates Nedd4 and Nedd4-2.
17482545 2007 Regulation of beta-adrenergic receptor signaling by S-nitrosylation of G-protein-coupled receptor kinase 2.
17344846 2007 Patterns of somatic mutation in human cancer genomes.
17276003 2007 Lymphocyte G-protein-coupled receptor kinase-2 is upregulated in patients with Alzheimer's disease.
17256744 2007 Vascular dysfunction in human and rat cirrhosis: role of receptor-desensitizing and calcium-sensitizing proteins.
17146290 2006 Identification of G-protein coupled receptor kinase 2 in paired helical filaments and neurofibrillary tangles.
17102134 2007 G protein-coupled receptor kinase 2-mediated phosphorylation of downstream regulatory element antagonist modulator regulates membrane trafficking of Kv4.2 potassium channel.
17055984 2006 Phosphorylation of p38 by GRK2 at the docking groove unveils a novel mechanism for inactivating p38MAPK.
17008309 2006 G protein-coupled receptor kinase and beta-arrestin-mediated desensitization of the angiotensin II type 1A receptor elucidated by diacylglycerol dynamics.
17006543 2006 Mdm2 is involved in the ubiquitination and degradation of G-protein-coupled receptor kinase 2.
17000469 2006 Overexpression of GRK2 in Alzheimer disease and in a chronic hypoperfusion rat model is an early marker of brain mitochondrial lesions.
16984558 2006 Decreased expression of G protein-coupled receptor kinases in the detrusor smooth muscle of human urinary bladder with outlet obstruction.
16920721 2006 Clathrin required for phosphorylation and internalization of beta2-adrenergic receptor by G protein-coupled receptor kinase 2 (GRK2).
16849637 2006 Impaired neutrophil chemotaxis in sepsis associates with GRK expression and inhibition of actin assembly and tyrosine phosphorylation.
16725308 2006 Tyrosine phosphorylation of G-protein-coupled-receptor kinase 2 (GRK2) by c-Src modulates its interaction with Galphaq.
16605244 2006 Alpha2A- and alpha2C-adrenergic receptors form homo- and heterodimers: the heterodimeric state impairs agonist-promoted GRK phosphorylation and beta-arrestin recruitment.
16356165 2006 Phosphodiesterase-4 influences the PKA phosphorylation status and membrane translocation of G-protein receptor kinase 2 (GRK2) in HEK-293beta2 cells and cardiac myocytes.
16121194 2005 The G protein-coupled receptor kinase-2 is a TGFbeta-inducible antagonist of TGFbeta signal transduction.
16081410 2005 Chemical genetic engineering of G protein-coupled receptor kinase 2.
16077899 2005 Regulation of EGF-induced ERK/MAPK activation and EGFR internalization by G protein-coupled receptor kinase 2.
15919661 2005 Uncoupling and endocytosis of 5-hydroxytryptamine 4 receptors. Distinct molecular events with different GRK2 requirements.
15870073 2005 Phosphorylation-independent regulation of metabotropic glutamate receptor 1 signaling requires g protein-coupled receptor kinase 2 binding to the second intracellular loop.
15843435 2005 G protein-coupled receptor kinase 2-mediated phosphorylation of ezrin is required for G protein-coupled receptor-dependent reorganization of the actin cytoskeleton.
15778405 2005 G protein-coupled receptor kinase 2 in multiple sclerosis and experimental autoimmune encephalomyelitis.
15653687 2005 Structure/function analysis of alpha2A-adrenergic receptor interaction with G protein-coupled receptor kinase 2.
15620700 2005 Activation of tyrosine kinase of EGFR induces Gbetagamma-dependent GRK-EGFR complex formation.
15618519 2004 Activity-dependent internalization of smoothened mediated by beta-arrestin 2 and GRK2.
15569306 2004 D1 dopamine receptor signaling involves caveolin-2 in HEK-293 cells.
15542600 2005 Bimodal regulation of the human H1 histamine receptor by G protein-coupled receptor kinase 2.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
15471870 2004 Characterization of the GRK2 binding site of Galphaq.
15271984 2004 Phosphorylation of the platelet-derived growth factor receptor-beta by G protein-coupled receptor kinase-2 reduces receptor signaling and interaction with the Na(+)/H(+) exchanger regulatory factor.
15097244 2004 Hypertensive left ventricular hypertrophy: relation to beta-adrenergic receptor kinase-1 (betaARK1) in peripheral lymphocytes.
15051637 2004 Targeted beta-adrenergic receptor kinase (betaARK1) inhibition by gene transfer in failing human hearts.
14997482 2004 Identification and characterization of phosphorylated proteins in the human pituitary.
14729942 2004 Identification of phosphoproteins and their phosphorylation sites in the WEHI-231 B lymphoma cell line.
14654844 2003 Protein kinase C switches the Raf kinase inhibitor from Raf-1 to GRK-2.
14557268 2003 G protein-coupled receptor kinase interaction with Hsp90 mediates kinase maturation.
12885252 2003 Differential interaction of GRK2 with members of the G alpha q family.
12750365 2003 Agonist-induced formation of opioid receptor-G protein-coupled receptor kinase (GRK)-G beta gamma complex on membrane is required for GRK2 function in vivo.
12679936 2003 Pleckstrin homology domain of G protein-coupled receptor kinase-2 binds to PKC and affects the activity of PKC kinase.
12639913 2003 Regulation of melanocortin-4 receptor signaling: agonist-mediated desensitization and internalization.
12624098 2003 The inhibitory gamma subunit of the type 6 retinal cGMP phosphodiesterase functions to link c-Src and G-protein-coupled receptor kinase 2 in a signaling unit that regulates p42/p44 mitogen-activated protein kinase by epidermal growth factor.
12552191 2003 Cardiopulmonary bypass decreases G protein-coupled receptor kinase activity and expression in human peripheral blood mononuclear cells.
12507501 2003 Aberrantly expressed recoverin is functionally associated with G-protein-coupled receptor kinases in cancer cell lines.
12486133 2003 The amino-terminal domain of G-protein-coupled receptor kinase 2 is a regulatory Gbeta gamma binding site.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12456365 2003 PH domain of G protein-coupled receptor kinase-2 binds to protein kinase C (PKC) and negatively regulates activity of PKC kinase.
12435819 2002 Reduction of G protein-coupled receptor kinase 2 expression in U-937 cells attenuates H2 histamine receptor desensitization and induces cell maturation.
12379128 2002 Beta 2-adrenergic receptor stimulated, G protein-coupled receptor kinase 2 mediated, phosphorylation of ribosomal protein P2.
12351722 2002 Interaction with neuronal calcium sensor NCS-1 mediates desensitization of the D2 dopamine receptor.
12163475 2002 Phosphoinositide 3-kinase regulates beta2-adrenergic receptor endocytosis by AP-2 recruitment to the receptor/beta-arrestin complex.
12130708 2002 Orphanin FQ/nociceptin-mediated desensitization of opioid receptor-like 1 receptor and mu opioid receptors involves protein kinase C: a molecular mechanism for heterologous cross-talk.
12130691 2002 Oxidative stress decreases G protein-coupled receptor kinase 2 in lymphocytes via a calpain-dependent mechanism.
12123746 2002 Identification of two C-terminal amino acids, Ser(355) and Thr(357), required for short-term homologous desensitization of mu-opioid receptors.
12107237 2002 Expression and activity of g protein-coupled receptor kinases in differentiated thyroid carcinoma.
11762794 2001 G-protein coupled receptor kinase 2 and 3 expression in human detrusor cultured smooth muscle cells.
11517230 2001 Determination of bradykinin B2 receptor in vivo phosphorylation sites and their role in receptor function.
11309381 2001 The scaffold protein gravin (cAMP-dependent protein kinase-anchoring protein 250) binds the beta 2-adrenergic receptor via the receptor cytoplasmic Arg-329 to Leu-413 domain and provides a mobile scaffold during desensitization.
11278469 2001 Regulation of membrane targeting of the G protein-coupled receptor kinase 2 by protein kinase A and its anchoring protein AKAP79.
11042191 2001 Phosphorylation of GRK2 by protein kinase C abolishes its inhibition by calmodulin.
11040053 2000 Identification of G protein-coupled receptor kinase 2 phosphorylation sites responsible for agonist-stimulated delta-opioid receptor phosphorylation.
10896954 2000 The GIT family of ADP-ribosylation factor GTPase-activating proteins. Functional diversity of GIT2 through alternative splicing.
10884381 2000 Phosphorylation of phosducin and phosducin-like protein by G protein-coupled receptor kinase 2.
10861009 2000 G protein-coupled receptor kinase-5 regulates thrombin-activated signaling in endothelial cells.
10858453 2000 Gravin-mediated formation of signaling complexes in beta 2-adrenergic receptor desensitization and resensitization.
10852916 2000 Synucleins are a novel class of substrates for G protein-coupled receptor kinases.
10754297 2000 Human NK cells express CC chemokine receptors 4 and 8 and respond to thymus and activation-regulated chemokine, macrophage-derived chemokine, and I-309.
10744734 2000 Mutational analysis of Gbetagamma and phospholipid interaction with G protein-coupled receptor kinase 2.
10727525 2000 Agonist-dependent modulation of G protein-coupled receptor kinase 2 by mitogen-activated protein kinases.
10722682 2000 Interaction between the conserved region in the C-terminal domain of GRK2 and rhodopsin is necessary for GRK2 to catalyze receptor phosphorylation.
10617630 2000 Constitutive phosphorylation of the Parkinson's disease associated alpha-synuclein.
10574913 1999 Feedback inhibition of G protein-coupled receptor kinase 2 (GRK2) activity by extracellular signal-regulated kinases.
10467231 1999 Expression of G-protein-coupled receptor kinases in pregnant term and non-pregnant human myometrium.
10379886 1999 Role of G protein-coupled receptor kinases on the agonist-induced phosphorylation and internalization of the follitropin receptor.
10091590 1999 Sequestration of dopamine D2 receptors depends on coexpression of G-protein-coupled receptor kinases 2 or 5.
10085131 1999 Differential effects of CC chemokines on CC chemokine receptor 5 (CCR5) phosphorylation and identification of phosphorylation sites on the CCR5 carboxyl terminus.
10085129 1999 Regulation of G protein-coupled receptor kinases by caveolin.
9826657 1998 beta2-Adrenergic receptor regulation by GIT1, a G protein-coupled receptor kinase-associated ADP ribosylation factor GTPase-activating protein.
9618528 1998 Expression of a beta-adrenergic receptor kinase 1 inhibitor prevents the development of myocardial failure in gene-targeted mice.
9501202 1998 Monocyte chemoattractant protein-1-induced CCR2B receptor desensitization mediated by the G protein-coupled receptor kinase 2.
9446593 1998 The solution structure and dynamics of the pleckstrin homology domain of G protein-coupled receptor kinase 2 (beta-adrenergic receptor kinase 1). A binding partner of Gbetagamma subunits.
8885248 1996 GRK2 and beta-arrestin 1 as negative regulators of thyrotropin receptor-stimulated response.
8662816 1996 Phosphorylation of the type 1A angiotensin II receptor by G protein-coupled receptor kinases and protein kinase C.
8195124 1994 Structure of the human gene encoding the beta-adrenergic receptor kinase.
7876239 1995 Four consecutive serines in the third intracellular loop are the sites for beta-adrenergic receptor kinase-mediated phosphorylation and desensitization of the alpha 2A-adrenergic receptor.
7836371 1995 Phosphorylation of the N-formyl peptide receptor carboxyl terminus by the G protein-coupled receptor kinase, GRK2.
2037065 1991 cDNA cloning and chromosomal localization of the human beta-adrenergic receptor kinase.
1339451 1992 High expression of beta-adrenergic receptor kinase in human peripheral blood leukocytes. Isoproterenol and platelet activating factor can induce kinase translocation.