Property Summary

NCBI Gene PubMed Count 83
PubMed Score 75.07
PubTator Score 96.50

Knowledge Summary

Patent (7,616)

Expression

  Differential Expression (24)

Disease log2 FC p
malignant mesothelioma -2.800 1.8e-08
astrocytic glioma -1.500 1.8e-02
Barrett's esophagus 1.700 4.3e-02
esophageal adenocarcinoma 1.300 4.0e-02
osteosarcoma 1.422 2.1e-04
medulloblastoma, large-cell -2.600 1.7e-05
adrenocortical adenoma -1.076 3.8e-02
adrenocortical carcinoma -1.464 2.4e-02
non-small cell lung cancer -2.342 2.1e-28
intraductal papillary-mucinous adenoma (... 1.400 8.4e-03
intraductal papillary-mucinous carcinoma... 1.400 8.5e-03
X-linked cerebral adrenoleukodystrophy -1.200 6.1e-03
lung cancer -2.600 1.1e-04
interstitial cystitis 2.100 5.9e-05
lung adenocarcinoma -2.519 2.5e-11
adult high grade glioma -1.400 8.2e-04
aldosterone-producing adenoma -1.451 3.8e-02
lung carcinoma -2.100 3.1e-18
breast carcinoma -1.200 1.9e-20
ductal carcinoma in situ -1.300 1.7e-03
invasive ductal carcinoma -1.800 4.5e-03
ulcerative colitis 2.400 2.7e-08
ovarian cancer -2.800 1.4e-10
dermatomyositis 1.200 7.9e-03

 GWAS Trait (1)

Gene RIF (58)

PMID Text
26820533 Thus, we provided new insight into the function of GRKs in agonist-unstimulated GPCR trafficking using a recombinant AM1 receptor and further determined the region of the CLR C-tail responsible for this GRK function.
26614013 We demonstrated that the SNPs and the related haplotypes of GRK5 could play a central role in predisposing Parkinson disease patients to cognitive impairment.
26515328 Specific patterns of altered heart GRK5 gene expression were found in models of cardiac hypertrophy.
26248277 Suggest a common regulatory pattern for the beta(1)-AR/GRK5 which is independent of cellular type or pathology.
26066465 ADORA2A and GRK5 gene variants may influence the etiology of malaria infection.
26032409 GRK5 is found in a partially closed state with its kinase domain C-tail forming novel interactions with nucleotide and the N-lobe.
25638254 This study sought to identify the distributed characteristics of these variant genotypes in Chinese population, and influence of GRK5 and ADRB1 polymorphisms on systolic heart failure morbidity.
25153362 These data suggest that increased GRK5 expression may contribute to the pathophysiology of schizophrenia.
25049040 G protein-coupled receptor kinase 5 gene polymorphisms may have a role in postoperative atrial fibrillation after coronary artery bypass grafting in patients receiving beta-blockers
25010510 A significant difference in the frequency of GRK5 polymorphism was found between Takotsubo cardiomyopathy patients and controls, supporting a genetic predisposition to this cardiac syndrome.
24807909 GRK5 dimerization is important for its plasma membrane localization and function.
24755472 GRK5 regulates prostate cancer cell migration and invasion. GRK5 forms a complex with moesin, phosphorylates moesin principally on T66 residue, and regulates cellular distribution of moesin.
24632620 Results demonstrate crosstalk among WIP1, CXCR4 and GRK5, which may be important for the aggressive phenotype of a subclass of medulloblastomas in children.
24613411 Low levels of GRK2/GRK5 causes a slow and not complete desensitization/down-regulation of GPR17.
24594703 GRK5 intronic (CA)n polymorphisms associated with type 2 diabetes in Chinese Hainan Island.
24178511 genetic polymorophism is associated with plasma viscosity
23794609 In the largest genotyped TC cohort in the literature, we have found no association of genetic variants in the ERalpha, beta1AR, beta2AR, or COMT genes, or with the previously implicated GRK5, with occurrence of the syndrome.
23693024 we show, for the first time, that knocking down the expression of GRK5 decreased the proliferation rate of gliioblastoma stem cells in contrast to control.
23658733 DNA-binding ability of GRK5 requires both the NLS and an N-terminal calmodulin (CaM)-binding site
23139825 These data suggest cell type- and subcellular compartment-dependent differences in GRK/arrestin-mediated desensitization and signaling.
22961080 A genome-wide association study identifies GRK5 and RASGRP1 as type 2 diabetes loci in Chinese Hans.
22467873 GRK5 phosphorylates Ser-4 in nucleophosmin and regulates the sensitivity of cells to PLK1 inhibition.
22223642 GRK5 is localized in the centrosome and regulates microtubule nucleation and normal cell cycle progression.
22196842 Increased GRK5 expression in the failing myocardium suggests a relevant role in human heart failure.
21784156 A reduced cortical concentration of GRK5 in schizophrenia (resembling that in aging) may result in altered G protein-dependent signaling, thus contributing to prefrontal deficits in schizophrenia.
21768220 GRK5 is a transcriptional modifier of a subset of Galphaq-downregulated genes, acting in opposition to the pathological effects of Galphaq and normalizing levels of these transcripts.
21728385 Hip has been identified as a novel substrate of GRK5 in vitro and in cells, and phosphorylation of Hip by GRK5 plays a role in modulating CXCR4 internalization
21575264 GRK5 mediates cell growth suppression by TIG1A. Thus, TIG1 may participate in the downregulation of G-protein coupled signaling by upregulating GRK5 expression.
21184589 GRK5 gene does not confer risk to sporadic Parkinson's disease in our sample from Southern Italy.
21127457 The GRK5 Leu41 allele protects from adverse cardiovascular outcomes in treated hypertensives.
20730384 Studies seem to indicate that mild, soluble, Beta-amyloid accumulation can lead to a reduced membrane (functional) and an elevated cytosolic GRK2/5.
20677014 Observational study of gene-disease association. (HuGE Navigator)
20628086 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
20468064 Observational study of gene-disease association. (HuGE Navigator)
20443868 This study shows for the first time that GRK5 negatively regulates VEGF signaling in human coronary artery endothelial cells.
20201926 Observational study and genome-wide association study of gene-disease association. (HuGE Navigator)
20124405 GRK5 as a novel kinase of p53, as well as a negative regulator of p53-mediated signal transduction.
20038610 This study uncovered previously unrecognized functionally important sites in the regulator of G-protein signaling homology domain of GRK5 kinase.
20023040 it has been demonstrated that the GRK5 L41 variant causes a negative inotropic effect under conditions of acute catecholamine stimulationl8AAg
20023040 Observational study of gene-disease association. (HuGE Navigator)
19913121 Observational study of gene-disease association. (HuGE Navigator)
19842931 GRK5 Gln41Leu polymorphism is not associated with sensitivity to beta(1)-adrenergic blockade in humans.
19801552 Results identify GRK5/6 as novel kinases for the single transmembrane receptor LRP6 during Wnt signaling.
19661922 beta-arrestin1 phosphorylation by GRK5 regulates G protein-independent signalling
19628119 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
19487588 Data suggest that GRK2, but not GRK5, is correlated with increasing blood pressure in black Americans
19092051 Reciprocity of regulation between platelet-derived growth factor receptor beta (PDGFRbeta) and GRK5, or their activation/deactivation cycle, mirrors other reciprocal regulatory mechanisms affecting tyrosine kinases.
19008357 GRK5 overexpression causes nuclear accumulation of IkappaB alpha, leading to the inhibition of NFkappaB transcriptional activity.
18855542 Protective effect of a GRK5 polymorphism on heart failure and its interaction with beta-adrenergic receptor antagonists is reported.
18622265 GRK5-Leu41 represents a gain-of-function polymorphism that evokes enhanced loss-of-function of beta2AR during persistent agonist exposure, and thus may contribute to beta-agonist variability in asthma treatment of African-Americans.
18425130 Observational study of gene-disease association, gene-environment interaction, and pharmacogenomic / toxicogenomic. (HuGE Navigator)
18034461 Results show that GRK5 plays a distinctive role in the phosphorylation of the beta2AR.
16849637 High expression was detected in septic neutrophils and control cells treated with cytokines plus LPS.
16385451 Observational study of gene-disease association. (HuGE Navigator)
15542828 GRK5 has a DNA-binding nuclear localization sequence
14976207 a group of hydrophobic amino acids within the membrane binding motif is critical to mediating the PM localization of GRK5
14691047 Data indicate that GRK5 does not regulate the sorting of human beta 2-adrenoceptors in the endocytic pathway.
12067742 Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro.

AA Sequence

MELENIVANTVLLKAREGGGGKRKGKSKKWKEILKFPHISQCEDLRRTIDRDYCSLCDKQPIGRLLFRQF      1 - 70
CETRPGLECYIQFLDSVAEYEVTPDEKLGEKGKEIMTKYLTPKSPVFIAQVGQDLVSQTEEKLLQKPCKE     71 - 140
LFSACAQSVHEYLRGEPFHEYLDSMFFDRFLQWKWLERQPVTKNTFRQYRVLGKGGFGEVCACQVRATGK    141 - 210
MYACKRLEKKRIKKRKGESMALNEKQILEKVNSQFVVNLAYAYETKDALCLVLTIMNGGDLKFHIYNMGN    211 - 280
PGFEEERALFYAAEILCGLEDLHRENTVYRDLKPENILLDDYGHIRISDLGLAVKIPEGDLIRGRVGTVG    281 - 350
YMAPEVLNNQRYGLSPDYWGLGCLIYEMIEGQSPFRGRKEKVKREEVDRRVLETEEVYSHKFSEEAKSIC    351 - 420
KMLLTKDAKQRLGCQEEGAAEVKRHPFFRNMNFKRLEAGMLDPPFVPDPRAVYCKDVLDIEQFSTVKGVN    421 - 490
LDHTDDDFYSKFSTGSVSIPWQNEMIETECFKELNVFGPNGTLPPDLNRNHPPEPPKKGLLQRLFKRQHQ    491 - 560
NNSKSSPSSKTSFNHHINSNHVSSNSTGSS                                            561 - 590
//

Text Mined References (88)

PMID Year Title
26820533 2016 Inhibitory effects of two G protein-coupled receptor kinases on the cell surface expression and signaling of the human adrenomedullin receptor.
26614013 2015 Role of G-protein coupled receptor kinase 5 gene in cognitive impairment in Parkinson's disease.
26515328 2015 Differential Role of G Protein-Coupled Receptor Kinase 5 in Physiological Versus Pathological Cardiac Hypertrophy.
26248277 2015 ?2- and ?1-Adrenoceptor Expression Exhibits a Common Regulatory Pattern With GRK2 and GRK5 in Human and Animal Models of Cardiovascular Diseases.
26066465 2015 Categorical complexities of Plasmodium falciparum malaria in individuals is associated with genetic variations in ADORA2A and GRK5 genes.
26032409 2015 Atomic Structure of GRK5 Reveals Distinct Structural Features Novel for G Protein-coupled Receptor Kinases.
25638254 2015 Effects of GRK5 and ADRB1 polymorphisms influence on systolic heart failure.
25153362 2014 Increased G protein-coupled receptor kinase (GRK) expression in the anterior cingulate cortex in schizophrenia.
25049040 2014 G protein-coupled receptor kinase 5 gene polymorphisms are associated with postoperative atrial fibrillation after coronary artery bypass grafting in patients receiving ?-blockers.
25010510 2015 G-protein-coupled receptor kinase 5 polymorphism and Takotsubo cardiomyopathy.
24807909 2014 The regulator of G protein signaling (RGS) domain of G protein-coupled receptor kinase 5 (GRK5) regulates plasma membrane localization and function.
24755472 2014 G protein-coupled receptor kinase GRK5 phosphorylates moesin and regulates metastasis in prostate cancer.
24632620 2015 The WIP1 oncogene promotes progression and invasion of aggressive medulloblastoma variants.
24613411 2014 Does GRK-? arrestin machinery work as a "switch on" for GPR17-mediated activation of intracellular signaling pathways?
24594703 2014 GRK5 intronic (CA)n polymorphisms associated with type 2 diabetes in Chinese Hainan Island.
24178511 2013 Gene-centric association signals for haemostasis and thrombosis traits identified with the HumanCVD BeadChip.
23794609 2013 No association of G-protein-coupled receptor kinase 5 or ?-adrenergic receptor polymorphisms with Takotsubo cardiomyopathy in a large Australian cohort.
23693024 2013 G-protein coupled receptor kinase (GRK)-5 regulates proliferation of glioblastoma-derived stem cells.
23658733 2013 Distinct structural features of G protein-coupled receptor kinase 5 (GRK5) regulate its nuclear localization and DNA-binding ability.
23251661 2012 Novel genetic loci identified for the pathophysiology of childhood obesity in the Hispanic population.
23139825 2012 Distinct cellular and subcellular distributions of G protein-coupled receptor kinase and arrestin isoforms in the striatum.
22961080 2013 A genome-wide association study identifies GRK5 and RASGRP1 as type 2 diabetes loci in Chinese Hans.
22467873 2012 G protein-coupled receptor kinase 5 phosphorylates nucleophosmin and regulates cell sensitivity to polo-like kinase 1 inhibition.
22223642 2012 G Protein-coupled receptor kinase 5 is localized to centrosomes and regulates cell cycle progression.
22196842 2012 Myocardial G protein receptor-coupled kinase expression correlates with functional parameters and clinical severity in advanced heart failure.
22099983 2012 G-protein coupled receptor kinase 5 regulates prostate tumor growth.
21784156 2011 Reduced expression of G protein-coupled receptor kinases in schizophrenia but not in schizoaffective disorder.
21768220 2011 Nuclear effects of G-protein receptor kinase 5 on histone deacetylase 5-regulated gene transcription in heart failure.
21728385 2011 G protein-coupled receptor kinase 5 phosphorylation of hip regulates internalization of the chemokine receptor CXCR4.
21575264 2011 G protein-coupled receptor kinase 5 mediates Tazarotene-induced gene 1-induced growth suppression of human colon cancer cells.
21184589 2011 Lack of association between G-protein coupled receptor kinase 5 gene and Parkinson's disease.
21127457 2011 Polymorphisms in genes coding for GRK2 and GRK5 and response differences in antihypertensive-treated patients.
20730384 2010 Dysfunction of G protein-coupled receptor kinases in Alzheimer's disease.
20677014 2010 An approach based on a genome-wide association study reveals candidate loci for narcolepsy.
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.
20468064 2010 Association study of 182 candidate genes in anorexia nervosa.
20443868 2009 Negative regulation of VEGF signaling in human coronary artery endothelial cells by G protein-coupled receptor kinase 5.
20201926 2010 Human variation in alcohol response is influenced by variation in neuronal signaling genes.
20124405 2010 G-protein-coupled receptor kinase 5 phosphorylates p53 and inhibits DNA damage-induced apoptosis.
20038610 2010 Role for the regulator of G-protein signaling homology domain of G protein-coupled receptor kinases 5 and 6 in beta 2-adrenergic receptor and rhodopsin phosphorylation.
20023040 2010 L41Q polymorphism of the G protein coupled receptor kinase 5 is associated with left ventricular apical ballooning syndrome.
19913121 2009 Gene-centric association signals for lipids and apolipoproteins identified via the HumanCVD BeadChip.
19842931 2009 GRK5 Gln41Leu polymorphism is not associated with sensitivity to beta(1)-adrenergic blockade in humans.
19801552 2009 G Protein-coupled receptor kinases phosphorylate LRP6 in the Wnt pathway.
19661922 2009 Beta-arrestin1 phosphorylation by GRK5 regulates G protein-independent 5-HT4 receptor signalling.
19628119 2009 Clinical and genetic modifiers of long-term survival in heart failure.
19487588 2009 G protein-coupled receptor kinase 2 expression and activity are associated with blood pressure in black Americans.
19092051 2009 Reciprocal regulation of the platelet-derived growth factor receptor-beta and G protein-coupled receptor kinase 5 by cross-phosphorylation: effects on catalysis.
19008357 2008 The G-protein-coupled receptor kinase 5 inhibits NFkappaB transcriptional activity by inducing nuclear accumulation of IkappaB alpha.
18855542 2008 Protective effect of a GRK5 polymorphism on heart failure and its interaction with beta-adrenergic receptor antagonists.
18669648 2008 A quantitative atlas of mitotic phosphorylation.
18622265 2008 A polymorphism of G-protein coupled receptor kinase5 alters agonist-promoted desensitization of beta2-adrenergic receptors.
18425130 2008 A GRK5 polymorphism that inhibits beta-adrenergic receptor signaling is protective in heart failure.
18034461 2007 Phosphorylation of the beta2-adrenergic receptor in plasma membranes by intrinsic GRK5.
17986524 2008 Characterization of G-protein coupled receptor kinase interaction with the neurokinin-1 receptor using bioluminescence resonance energy transfer.
17344846 2007 Patterns of somatic mutation in human cancer genomes.
16849637 2006 Impaired neutrophil chemotaxis in sepsis associates with GRK expression and inhibition of actin assembly and tyrosine phosphorylation.
16385451 2006 A scan of chromosome 10 identifies a novel locus showing strong association with late-onset Alzheimer disease.
15542828 2004 G protein-coupled receptor kinase 5 contains a DNA-binding nuclear localization sequence.
15489334 2004 The status, quality, and expansion of the NIH full-length cDNA project: the Mammalian Gene Collection (MGC).
15164054 2004 The DNA sequence and comparative analysis of human chromosome 10.
15146197 2004 Transcriptome characterization elucidates signaling networks that control human ES cell growth and differentiation.
14976207 2004 A predicted amphipathic helix mediates plasma membrane localization of GRK5.
14702039 2004 Complete sequencing and characterization of 21,243 full-length human cDNAs.
14691047 2004 Endosome sorting of beta 2-adrenoceptors is GRK5 independent.
12507501 2003 Aberrantly expressed recoverin is functionally associated with G-protein-coupled receptor kinases in cancer cell lines.
12477932 2002 Generation and initial analysis of more than 15,000 full-length human and mouse cDNA sequences.
12067742 2002 Human substance P receptor undergoes agonist-dependent phosphorylation by G protein-coupled receptor kinase 5 in vitro.
11700307 2002 G protein-coupled receptor kinase 5 regulates beta 1-adrenergic receptor association with PSD-95.
11517230 2001 Determination of bradykinin B2 receptor in vivo phosphorylation sites and their role in receptor function.
11504827 2001 Phosphorylation and desensitization of the human thromboxane receptor-alpha by G protein-coupled receptor kinases.
10858434 2000 Dynamic interaction of human vasopressin/oxytocin receptor subtypes with G protein-coupled receptor kinases and protein kinase C after agonist stimulation.
10852916 2000 Synucleins are a novel class of substrates for G protein-coupled receptor kinases.
10617630 2000 Constitutive phosphorylation of the Parkinson's disease associated alpha-synuclein.
10467231 1999 Expression of G-protein-coupled receptor kinases in pregnant term and non-pregnant human myometrium.
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.
9813065 1998 Structure-function analysis of G protein-coupled receptor kinase-5. Role of the carboxyl terminus in kinase regulation.
9218466 1997 Regulation of G protein-coupled receptor kinases by calmodulin and localization of the calmodulin binding domain.
8889548 1996 Normalization and subtraction: two approaches to facilitate gene discovery.
8662852 1996 Identification of the G protein-coupled receptor kinase phosphorylation sites in the human beta2-adrenergic receptor.
8662816 1996 Phosphorylation of the type 1A angiotensin II receptor by G protein-coupled receptor kinases and protein kinase C.
8626574 1996 Involvement of G protein-coupled receptor kinase 5 in homologous desensitization of the thyrotropin receptor.
8381058 1993 Altered expression of beta-adrenergic receptor kinase and beta 1-adrenergic receptors in the failing human heart.
8288567 1994 Expression, purification, and characterization of the G protein-coupled receptor kinase GRK5.
8144599 1994 Phospholipid-stimulated autophosphorylation activates the G protein-coupled receptor kinase GRK5.
7789183 1995 Chromosomal mapping of the genes GPRK5 and GPRK6 encoding G protein-coupled receptor kinases GRK5 and GRK6.
7685906 1993 Cloning and expression of GRK5: a member of the G protein-coupled receptor kinase family.