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G protein-coupled receptor kinase 6

GRK6, G protein-coupled receptor kinase 6
This gene encodes a member of the guanine nucleotide-binding protein (G protein)-coupled receptor kinase subfamily of the Ser/Thr protein kinase family. The protein phosphorylates the activated forms of G protein-coupled receptors thus initiating their deactivation. Several transcript variants encoding different isoforms have been described for this gene. [provided by RefSeq, Jul 2008] (from NCBI)
Top mentioned proteins: GRK2, GRK5, GRK3, IRBP, GRK4
Papers on GRK6
Aberrant GRK6 promoter methylation is associated with poor prognosis in hypopharyngeal squamous cell carcinoma.
Wang et al., Nantong, China. In Oncol Rep, Feb 2016
In the present study, we examined GRK6 expression in HSCC and also assessed the possible cause of its aberrant expression, as well as its clinical significance.
G protein-coupled receptor kinase 6/β-arrestin 2 system in a rat model of dopamine supersensitivity psychosis.
Iyo et al., Mobara, Japan. In J Psychopharmacol, Dec 2015
G protein-coupled receptor kinase 6 (GRK6) and beta-arrestin 2 (ARRB2) play important roles in the trafficking of DRD2 by phosphorylation and internalization.
Crystal Structure of G Protein-coupled Receptor Kinase 5 in Complex with a Rationally Designed Inhibitor.
Tesmer et al., Ann Arbor, United States. In J Biol Chem, Sep 2015
The overall conformation of the GRK5 kinase domain is similar to that of a previously determined structure of GRK6 in what is proposed to be its active state, but the C-terminal region of the enzyme adopts a distinct conformation.
Structure and Function of the Hypertension Variant A486V of G Protein-coupled Receptor Kinase 4.
Lumb et al., United States. In J Biol Chem, Sep 2015
In this respect, GRK4α is more similar to GRK2 than GRK6.
Neutrophil Elastase Activates Protease-activated Receptor-2 (PAR2) and Transient Receptor Potential Vanilloid 4 (TRPV4) to Cause Inflammation and Pain.
Bunnett et al., Erlangen, Germany. In J Biol Chem, Jun 2015
Although elastase did not promote recruitment of G protein-coupled receptor kinase-2 (GRK(2)) or β-arrestin to PAR(2), consistent with its inability to promote receptor endocytosis, elastase did stimulate GRK6 recruitment.
GRK6 phosphorylates IκBα at Ser(32)/Ser(36) and enhances TNF-α-induced inflammation.
Kurose et al., Fukuoka, Japan. In Biochem Biophys Res Commun, Jun 2015
However, those for GRK6 are poorly understood.
Overexpression of GRK6 rescues L-DOPA-induced signaling abnormalities in the dopamine-depleted striatum of hemiparkinsonian rats.
Gurevich et al., Nashville, United States. In Exp Neurol, Apr 2015
Overexpression of GRK6, the isoform regulating dopamine receptors, in parkinsonian rats and monkeys alleviated LID and reduced LID-associated changes in gene expression.
Functional consequences of perturbed CXCL12 signal processing: analyses of immature hematopoiesis in GRK6-deficient mice.
Bönig et al., Frankfurt am Main, Germany. In Stem Cells Dev, Apr 2015
Using, therefore, a GRK6-deficient (GRK6(-/-)) mouse, we sought to address how perturbed ligand-induced CXCR4 (in)activation affects HSPC behavior in vitro and in vivo.
A novel monoclonal antibody against human GRK6 antigen.
Li et al., Chengdu, China. In Monoclon Antib Immunodiagn Immunother, Feb 2015
G protein-coupled receptor kinase 6 (GRK6) plays a universal role in receptor desensitization, by acting as a receptor-G protein interface, thereby affecting serine/threonine kinases.
Genetic association between G protein-coupled receptor kinase 6/β-arrestin 2 and dopamine supersensitivity psychosis in schizophrenia.
Iyo et al., Chiba, Japan. In Neuropsychiatr Dis Treat, 2014
The present study explored the potential roles of G protein-coupled receptor kinase 6 (GRK6) and β-arrestin 2 (ARRB2) that are involved in the trafficking of DRD2 in patients with DSP.
[Research on Molecular Mechanisms of Engulfment of Apoptotic Cells].
Nakaya, In Yakugaku Zasshi, 2014
We further determined that G protein-coupled receptor kinase 6 (GRK6), originally identified as a kinase responsible for the desensitization and downregulation of G-protein-coupled receptors, activates Rac1 independent of the two known intracellular engulfment pathways in phagocytes.
Mapping the putative G protein-coupled receptor (GPCR) docking site on GPCR kinase 2: insights from intact cell phosphorylation and recruitment assays.
Sterne-Marr et al., Montréal, Canada. In J Biol Chem, 2014
Taken together with data on GRK1 and GRK6, our data suggest that all three GRK subfamilies make conserved interactions with G protein-coupled receptors, but there may be unique interactions that influence selectivity.
The H50Q mutation enhances α-synuclein aggregation, secretion, and toxicity.
Lashuel et al., Lausanne, Switzerland. In J Biol Chem, 2014
In cell-based models, H50Q mutation did not affect α-Syn subcellular localization or its ability to be phosphorylated by PLK2 and GRK6.
Reduced expression of G protein-coupled receptor kinases in schizophrenia but not in schizoaffective disorder.
Gurevich et al., Nashville, United States. In Neurobiol Dis, 2011
A reduced cortical concentration of GRK6 in schizophrenia (resembling that in aging) may result in altered G protein-dependent signaling, thus contributing to prefrontal deficits in schizophrenia.
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.
Clark et al., Houston, United States. In Mol Pharmacol, 2010
A number of double mutations of GRK6 kinase within helices 3, 9, and 10 reduced phosphorylation of the beta2 adrenergic receptor and rhodopsin compared to wild-type GRK6 kinase.
Kinome-wide RNAi studies in human multiple myeloma identify vulnerable kinase targets, including a lymphoid-restricted kinase, GRK6.
Stewart et al., Scottsdale, United States. In Blood, 2010
inhibition of GRK6 represents a uniquely targeted novel therapeutic strategy in human multiple myeloma.
G Protein-coupled receptor kinases phosphorylate LRP6 in the Wnt pathway.
Chen et al., Durham, United States. In J Biol Chem, 2010
Results identify GRK5/6 as novel kinases for the single transmembrane receptor LRP6 during Wnt signaling.
Impaired recruitment of Grk6 and beta-Arrestin 2 causes delayed internalization and desensitization of a WHIM syndrome-associated CXCR4 mutant receptor.
Tosato et al., Bethesda, United States. In Plos One, 2008
Recruitment of beta-Arrestin 2, but not beta-Arrestin 1, to the active WHIM-mutant receptor is delayed compared to the WT CXCR4 receptor and Grk6 fails to associate with the WHIM-mutant receptor.
The G protein-coupled receptor kinase (GRK) interactome: role of GRKs in GPCR regulation and signaling.
Mayor et al., Madrid, Spain. In Biochim Biophys Acta, 2007
Novel studies have revealed a phosphorylation-independent desensitization mechanism operating through their RGS-homology (RH) domain and the recent determination of the crystal structures of GRK2 and GRK6 has uncovered interesting details on the structure-function relationships of these kinases.
Non-visual GRKs: are we seeing the whole picture?
Nahorski et al., Leicester, United Kingdom. In Trends Pharmacol Sci, 2003
However, recent work has indicated roles for the other, non-visual GRKs (GRK4, GRK5 and GRK6) and has revealed potential phosphorylation-independent regulation of GPCRs by GRK2 and GRK3.
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