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ATP + activated form of G protein-coupled receptors
ADP + phosphorylated G protein-coupled receptors
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
reaction only with GRK4alpha isoform, no reaction with GRK4beta, GRK4gamma, GRK4delta
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
-
-
-
?
ATP + a G protein-coupled receptor
ADP + a phosphorylated G protein-coupled receptor
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
ATP + ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
-
-
-
?
ATP + beta 2-adrenergic receptor
ADP + phosphorylated beta 2-adrenergic receptor
-
-
-
?
ATP + BLT1 receptor
ADP + phosphorylated BLT1 receptor
ATP + CXCR4 receptor
ADP + phosphorylated CXCR4 receptor
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
GRK4
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
ATP + G-protein-coupled receptor
ADP + phosphorylated G-protein-coupled receptor
ATP + histone deacetylase 6
ADP + phosphorylated histone deacetylase 6
the enzyme phosphorylates histone deacetylase 6 at Ser21 to promote its deacetylase activity
-
-
?
ATP + moesin
ADP + phosphorylated moesin
phosphorylation at Thr66
-
-
?
ATP + porcine brain tubulin
ADP + phosphorylated porcine brain tubulin
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
ATP + rhodopsin
ADP + rhodopsin phosphate
cf. EC 2.7.11.14, rhodopsin is also a substrate of GRK5
-
-
?
ATP + [alpha-synuclein]
ADP + [alpha-synuclein]phosphate
the enzyme phosphorylates alpha-synuclein at Ser129
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor]phosphate
-
GRK4-6
-
-
?
ATP + [dopamine D1 receptor]
ADP + [dopamine D1 receptor]phosphate
ATP + [follicle-stimulating hormone receptor]
ADP + [follicle-stimulating hormone receptor]phosphate
-
GRK4-6
-
-
?
ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
ATP + [luteinizing hormone/chorionic gonadotropin receptor]
ADP + [luteinizing hormone/chorionic gonadotropin receptor]phosphate
-
GRK4-6
-
-
?
ATP + [M2 muscarinic receptor]
ADP + [M2 muscarinic receptor]phosphate
-
GRK4-6
-
-
?
ATP + [M3 muscarinic acetylcholine receptor]
ADP + phospho-[M3 muscarinic acetylcholine receptor]
ATP + [rhodopsin]
ADP + [rhodopsin]phosphate
-
GRK4-6
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
nucleophosmin 1 + ATP
phosphorylated nucleophosmin 1 + ADP
-
-
-
-
?
p53 + ATP
phosphorylated-p53 + ADP
-
-
-
-
?
additional information
?
-
ATP + a G protein-coupled receptor
ADP + a phosphorylated G protein-coupled receptor
-
the GRKs are important in the cardiovascular system, the major G protein-coupled receptor regulatory pathway involves phosphorylation of activated receptors by GRKs, followed by binding of arrestin proteins, which prevent receptors from activating downstream heterotrimeric G protein pathways while allowing activation of arrestin-dependent signaling pathways, general mechanisms of GRK-arrestin regulation, overview, physiological functions and potential pathophysiological roles of GRKs and arrestins in human disorders, overview
-
-
?
ATP + a G protein-coupled receptor
ADP + a phosphorylated G protein-coupled receptor
-
cell surface localized receptors
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
-
GRK5 phosphorylates Ser-129 of alpha-synuclein at the plasma membrane and induces translocation of phosphorylated alpha-synuclein to the perikaryal area, GRK5 promotes alpha-linolenic acid-induced oligomerization of alpha-synuclein, alpha-synuclein phosphorylation by GRK5 plays a crucial role in the pathogenesis of sporadic Parkinson's disease, sPD
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
-
phosphorylation at Ser129
-
-
?
ATP + BLT1 receptor
ADP + phosphorylated BLT1 receptor
-
GRK6, ablation of GRK6 leads to augmented signaling by leukotriene B4 acting through the BLT1 receptor
-
-
?
ATP + BLT1 receptor
ADP + phosphorylated BLT1 receptor
-
GRK6
-
-
?
ATP + CXCR4 receptor
ADP + phosphorylated CXCR4 receptor
-
GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow
-
-
?
ATP + CXCR4 receptor
ADP + phosphorylated CXCR4 receptor
-
GRK6
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
-
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
regulation mechanism of GRK5, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview
-
-
?
ATP + G-protein-coupled receptor
ADP + phosphorylated G-protein-coupled receptor
-
-
-
-
?
ATP + G-protein-coupled receptor
ADP + phosphorylated G-protein-coupled receptor
-
leading to receptor endocytosis
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
GRK5 plays a distinctive role in the phosphorylation of the beta2AR
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
cf. EC 2.7.11.15, recombinant FLAG-tagged beta2-adrenergic receptor stably expressed in HEK-293 cells
-
-
?
ATP + [dopamine D1 receptor]
ADP + [dopamine D1 receptor]phosphate
-
GRK4 constitutively phosphorylates active and inactive receptor, in the latter case diminishing stimulation of the receptor by dopamine, phosphorylation reduces receptor desensitization and internalization, followed by reduced cAMP accumulation
-
-
?
ATP + [dopamine D1 receptor]
ADP + [dopamine D1 receptor]phosphate
-
GRK4 phosphorylates active and inactive receptor
-
-
?
ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
-
-
-
?
ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
-
GRK4-6
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
-
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
-
-
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
-
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
GRK5 effectively phosphorylates inactive forms of several G-protein-coupled receptors, including serotonin 5-HT2C, beta2-adrenergic and M2 muscarinic receptors and rhodopsin
-
-
?
ATP + [M3 muscarinic acetylcholine receptor]
ADP + phospho-[M3 muscarinic acetylcholine receptor]
-
-
-
-
?
ATP + [M3 muscarinic acetylcholine receptor]
ADP + phospho-[M3 muscarinic acetylcholine receptor]
-
GRK6 plays a major role in specific M3 muscarinic acetylcholine receptor regulation
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
-
GRK4-6
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
-
GRK4-6, receptor activation
-
-
?
additional information
?
-
enzyme is involved in fertilization
-
-
?
additional information
?
-
-
enzyme is involved in fertilization
-
-
?
additional information
?
-
GRK4 inhibits GalphaS-coupled GPCR signaling and lacks a PH domain, and GRK4gamma interacts with inactive GalphaS, inactive Gbeta, and inactive Galpha13, and to a lesser extent also with active GalphaS, subunits of heterotrimeric G proteins, overview
-
-
?
additional information
?
-
autophosphorylation of wild type isoform GRK4alpha is required for full kinase activity
-
-
?
additional information
?
-
-
autophosphorylation of wild type isoform GRK4alpha is required for full kinase activity
-
-
?
additional information
?
-
-
substrate specificity
-
-
?
additional information
?
-
GRK6, but not other GRKs tested, incorporated tritium after incubation with [3H]palmitate in Sf9 and in COS-7 cells overexpressing the kinase
-
-
?
additional information
?
-
-
GRK5 and especially GRK6 have selective regulatory roles in cAMP accumulation response of the secretin receptor to agonists like beta-arrestin-1 or forskolin, overview
-
-
?
additional information
?
-
-
GRKs are involved in diverse physiological processes and pathologies, overview
-
-
?
additional information
?
-
-
the enzyme is involved in GPCR signal transduction pathways and desensitization
-
-
?
additional information
?
-
-
the GRK4 isozymes are differentially regulated, overview
-
-
?
additional information
?
-
-
GRK5 performs autophosphorylation
-
-
?
additional information
?
-
-
GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview
-
-
?
additional information
?
-
-
GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling and desensitization, beta-arrestin-mediated receptor internalization, activity of GRKs and subcellular targeting is tightly regulated by interaction with receptor domains, G protein subunits, lipids, anchoring proteins and calcium-sensitive proteins
-
-
?
additional information
?
-
-
GRK4 is involved in activity of dopamine receptors in renal proximal tubules and mediates sodium reabsorption and blood pressure regulation
-
-
?
additional information
?
-
-
GRK4 is involved in activity of dopamine receptors in renal proximal tubules and mediates sodium reabsorption and blood pressure regulation
-
-
?
additional information
?
-
-
GRK6 is a key regulator of dopaminergic signaling and lymphocyte chemotaxis
-
-
?
additional information
?
-
-
GRK6 structure-function relationship determination and analysis
-
-
?
additional information
?
-
-
no binding to RH domain of G protein Galphaq and Galpha-11 by GRK4
-
-
?
additional information
?
-
GRK5 also phosphorylates rhodopsin, cf. EC 2.7.11.14
-
-
?
additional information
?
-
isoform GRK5 binds DNA in vitro
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
-
-
-
?
ATP + a G protein-coupled receptor
ADP + a phosphorylated G protein-coupled receptor
-
the GRKs are important in the cardiovascular system, the major G protein-coupled receptor regulatory pathway involves phosphorylation of activated receptors by GRKs, followed by binding of arrestin proteins, which prevent receptors from activating downstream heterotrimeric G protein pathways while allowing activation of arrestin-dependent signaling pathways, general mechanisms of GRK-arrestin regulation, overview, physiological functions and potential pathophysiological roles of GRKs and arrestins in human disorders, overview
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
-
GRK5 phosphorylates Ser-129 of alpha-synuclein at the plasma membrane and induces translocation of phosphorylated alpha-synuclein to the perikaryal area, GRK5 promotes alpha-linolenic acid-induced oligomerization of alpha-synuclein, alpha-synuclein phosphorylation by GRK5 plays a crucial role in the pathogenesis of sporadic Parkinson's disease, sPD
-
-
?
ATP + ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
-
-
-
?
ATP + BLT1 receptor
ADP + phosphorylated BLT1 receptor
-
GRK6, ablation of GRK6 leads to augmented signaling by leukotriene B4 acting through the BLT1 receptor
-
-
?
ATP + CXCR4 receptor
ADP + phosphorylated CXCR4 receptor
-
GRK6, the pathway is important in facilitating neutrophil retention in the bone marrow
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
GRK4
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
regulation mechanism of GRK5, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview
-
-
?
ATP + G-protein-coupled receptor
ADP + phosphorylated G-protein-coupled receptor
-
leading to receptor endocytosis
-
-
?
ATP + moesin
ADP + phosphorylated moesin
phosphorylation at Thr66
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
-
?
ATP + [alpha-synuclein]
ADP + [alpha-synuclein]phosphate
the enzyme phosphorylates alpha-synuclein at Ser129
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
GRK5 plays a distinctive role in the phosphorylation of the beta2AR
-
-
?
ATP + [dopamine D1 receptor]
ADP + [dopamine D1 receptor]phosphate
-
GRK4 constitutively phosphorylates active and inactive receptor, in the latter case diminishing stimulation of the receptor by dopamine, phosphorylation reduces receptor desensitization and internalization, followed by reduced cAMP accumulation
-
-
?
ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
ATP + [M3 muscarinic acetylcholine receptor]
ADP + phospho-[M3 muscarinic acetylcholine receptor]
-
GRK6 plays a major role in specific M3 muscarinic acetylcholine receptor regulation
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
-
GRK4-6, receptor activation
-
-
?
additional information
?
-
ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
-
-
-
?
ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
-
GRK4-6
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
-
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
-
-
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
-
-
-
?
ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
GRK5 effectively phosphorylates inactive forms of several G-protein-coupled receptors, including serotonin 5-HT2C, beta2-adrenergic and M2 muscarinic receptors and rhodopsin
-
-
?
additional information
?
-
enzyme is involved in fertilization
-
-
?
additional information
?
-
-
enzyme is involved in fertilization
-
-
?
additional information
?
-
-
GRK5 and especially GRK6 have selective regulatory roles in cAMP accumulation response of the secretin receptor to agonists like beta-arrestin-1 or forskolin, overview
-
-
?
additional information
?
-
-
GRKs are involved in diverse physiological processes and pathologies, overview
-
-
?
additional information
?
-
-
the enzyme is involved in GPCR signal transduction pathways and desensitization
-
-
?
additional information
?
-
-
the GRK4 isozymes are differentially regulated, overview
-
-
?
additional information
?
-
-
GRK activity is regulated by phosphorylation through several kinases and by interactions with several cellular proteins, e.g. calmodulin, caveolin or RKIP, GRK also interacts with PI3K, Akt, GIT or MEK, the interactions occur at the RH and PH domains, overview, the GRK interactome: role of GRKs in GPCR regulation and signaling, detailed overview
-
-
?
additional information
?
-
-
GRK-mediated receptor phosphorylation rapidly initiates profound impairment of receptor signaling and desensitization, beta-arrestin-mediated receptor internalization, activity of GRKs and subcellular targeting is tightly regulated by interaction with receptor domains, G protein subunits, lipids, anchoring proteins and calcium-sensitive proteins
-
-
?
additional information
?
-
-
GRK4 is involved in activity of dopamine receptors in renal proximal tubules and mediates sodium reabsorption and blood pressure regulation
-
-
?
additional information
?
-
-
GRK4 is involved in activity of dopamine receptors in renal proximal tubules and mediates sodium reabsorption and blood pressure regulation
-
-
?
additional information
?
-
-
GRK6 is a key regulator of dopaminergic signaling and lymphocyte chemotaxis
-
-
?
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Adenocarcinoma of Lung
Hypermethylation of the G protein-coupled receptor kinase 6 (GRK6) promoter inhibits binding of C/EBP?, and GRK6 knockdown promotes cell migration and invasion in lung adenocarcinoma cells.
Alzheimer Disease
Augmented axonal defects and synaptic degenerative changes in female GRK5 deficient mice.
Alzheimer Disease
GRK5 deficiency accelerates {beta}-amyloid accumulation in Tg2576 mice via impaired cholinergic activity.
Alzheimer Disease
GRK5 deficiency leads to reduced hippocampal acetylcholine level via impaired presynaptic M2/M4 autoreceptor desensitization.
Alzheimer Disease
GRK5 dysfunction accelerates tau hyperphosphorylation in APP (swe) mice through impaired cholinergic activity.
Aortic Coarctation
Secreted miR-27a Induced by Cyclic Stretch Modulates the Proliferation of Endothelial Cells in Hypertension via GRK6.
Arthritis
G protein-coupled receptor kinase 5 deletion suppresses synovial inflammation in a murine model of collagen antibody-induced arthritis.
Atrial Fibrillation
G protein-coupled receptor kinase 5 gene polymorphisms are associated with postoperative atrial fibrillation after coronary artery bypass grafting in patients receiving ?-blockers.
Breast Neoplasms
Expression of G protein-coupled receptor kinase 4 is associated with breast cancer tumourigenesis.
Carcinogenesis
Expression of G protein-coupled receptor kinase 4 is associated with breast cancer tumourigenesis.
Carcinoma, Hepatocellular
Expression and Significances of G-Protein-Coupled Receptor Kinase 3 in Hepatocellular Carcinoma.
Carcinoma, Hepatocellular
GRK6 expression in patients with hepatocellular carcinoma.
Cardiomegaly
Determining the Absolute Requirement of G Protein-Coupled Receptor Kinase 5 for Pathological Cardiac Hypertrophy.
Cardiomegaly
Differential Role of G Protein-Coupled Receptor Kinase 5 in Physiological Versus Pathological Cardiac Hypertrophy.
Cardiomegaly
G protein-coupled receptor kinase 5: exploring its hype in cardiac hypertrophy.
Cardiomegaly
GRK5 contributes to impaired cardiac function and immune cell recruitment in post-ischemic heart failure.
Cardiomegaly
KR-39038, a Novel GRK5 Inhibitor, Attenuates Cardiac Hypertrophy and Improves Cardiac Function in Heart Failure.
Cardiomegaly
PH domain leucine-rich repeat protein phosphatase 2 (PHLPP2) regulates G-protein-coupled receptor kinase 5 (GRK5)-induced cardiac hypertrophy in vitro.
Cardiovascular Diseases
Characterization of G protein-coupled receptor kinase 4 and measuring its constitutive activity in vivo.
Cardiovascular Diseases
Design and synthesis of novel 3-(benzo[d]oxazol-2-yl)-5-(1-(piperidin-4-yl)-1H-pyrazol-4-yl)pyridin-2-amine derivatives as selective G-protein-coupled receptor kinase-2 and -5 inhibitors.
Colitis
G protein-coupled receptor kinase 6 controls chronicity and severity of dextran sodium sulphate-induced colitis in mice.
Colonic Neoplasms
G protein-coupled receptor kinase 5 mediates Tazarotene-induced gene 1-induced growth suppression of human colon cancer cells.
Colonic Neoplasms
Tazarotene-induced gene 1 inhibits prostaglandin E2-stimulated HCT116 colon cancer cell growth.
Colorectal Neoplasms
Overexpression of GRK6 associates with the progression and prognosis of colorectal carcinoma.
Dementia
Role of G-protein coupled receptor kinase 5 gene in cognitive impairment in Parkinson's disease.
Diabetes Mellitus
A variant of GRK5 is associated with the therapeutic efficacy of repaglinide in Chinese Han patients with type 2 diabetes mellitus.
Diabetes Mellitus
GRK5 Intronic (CA)n Polymorphisms Associated with Type 2 Diabetes in Chinese Hainan Island.
Diabetes Mellitus, Type 2
A variant of GRK5 is associated with the therapeutic efficacy of repaglinide in Chinese Han patients with type 2 diabetes mellitus.
Diabetes Mellitus, Type 2
GRK5 Intronic (CA)n Polymorphisms Associated with Type 2 Diabetes in Chinese Hainan Island.
Dyskinesias
Effect of Tianqi antitremor granules on behavioral manifestations and expression of G protein-coupled receptor kinase 6 and ?-arrestin1 in levodopa-induced dyskinesia in a rat model of Parkinson's disease.
Dyskinesias
[Effects of Chinese herbal medicine Tianqi Pingchan Granule on G protein-coupled receptor kinase 6 involved in the prevention of levodopa-induced dyskinesia in rats with Parkinson disease].
Essential Hypertension
Association of G-protein-coupled receptor kinase 4 haplotypes, but not HSD3B1 or PTP1B polymorphisms, with essential hypertension.
Essential Hypertension
Association study of G protein-coupled receptor kinase 4 gene variants with essential hypertension in northern Han Chinese.
Essential Hypertension
G protein-coupled receptor kinase 4 (GRK4) regulates the phosphorylation and function of the dopamine D3 receptor.
Essential Hypertension
G protein-coupled receptor kinase 4 gene variants in human essential hypertension.
Essential Hypertension
[G protein kinase 4gammaA142V overexpression induced hypertension by downregulating D1 receptors in transgenic mice]
g-protein-coupled receptor kinase deficiency
G protein-coupled receptor kinase 6 deficiency promotes angiogenesis, tumor progression, and metastasis.
Glioma
G protein-coupled receptor kinase 6 is overexpressed in glioma and promotes glioma cell proliferation.
Heart Diseases
beta-adrenergic mechanisms in cardiac diseases: a perspective.
Heart Failure
A peptide of the N terminus of GRK5 attenuates pressure-overload hypertrophy and heart failure.
Heart Failure
G-protein-coupled receptor kinase activity in human heart failure: effects of beta-adrenoceptor blockade.
Heart Failure
KR-39038, a Novel GRK5 Inhibitor, Attenuates Cardiac Hypertrophy and Improves Cardiac Function in Heart Failure.
Heart Failure
Pharmacogenomics of beta-Adrenergic Receptors and Their Accessory Signaling Proteins in Heart Failure.
Heart Failure
Regulation of nuclear factor ?B (NF-?B) in the nucleus of cardiomyocytes by G protein-coupled receptor kinase 5 (GRK5).
Heart Failure
The analysis of heterotaxy patients reveals new loss-of-function variants of GRK5.
Heart Failure
The inotropic peptide ?ARKct improves ?AR responsiveness in normal and failing cardiomyocytes through G(??)-mediated L-type calcium current disinhibition.
Hyperalgesia
G protein-coupled receptor kinase 6 controls post-inflammatory visceral hyperalgesia.
Hyperalgesia
GRK6 acts as a critical regulator of cytokine-induced hyperalgesia by promoting PI3kinase- and inhibiting p38-signaling.
Hypertension
Autosomal genome scan for loci linked to blood pressure levels and trends since childhood: the Bogalusa Heart Study.
Hypertension
Changes in Adrenoceptors and G-Protein-Coupled Receptor Kinase 2 in L-NAME-Induced Hypertension Compared to Spontaneous Hypertension in Rats.
Hypertension
Dopamine and G protein-coupled receptor kinase 4 in the kidney: Role in blood pressure regulation.
Hypertension
Effects of decreased renal cortical expression of G protein-coupled receptor kinase 4 and angiotensin type 1 receptors in rats.
Hypertension
G protein-coupled receptor kinase 4 gene variants are not associated with preeclampsia in Northern Han Chinese.
Hypertension
G protein-coupled receptor kinase 4: role in hypertension.
Hypertension
G protein-coupled receptor kinase 4gamma interacts with inactive Galpha(s) and Galpha13.
Hypertension
G protein-coupled receptor kinase 5 in cultured vascular smooth muscle cells and rat aorta. Regulation by angiotensin II and hypertension.
Hypertension
G-protein-coupled receptor kinase 4 polymorphisms predict blood pressure response to dietary modification in Black patients with mild-to-moderate hypertension.
Hypertension
G-Protein-coupled receptor kinase activity in hypertension : increased vascular and lymphocyte G-protein receptor kinase-2 protein expression.
Hypertension
G-protein-coupled receptor kinase activity is increased in hypertension.
Hypertension
G-protein-coupled receptor kinase expression in hypertension.
Hypertension
Genetic variants of GRK4 influence circadian rhythm of blood pressure and response to candesartan in hypertensive patients.
Hypertension
Hypertension-Related Gene Polymorphisms of G-Protein-Coupled Receptor Kinase 4 Are Associated with NT-proBNP Concentration in Normotensive Healthy Adults.
Hypertension
Renal Dopamine Receptors and Oxidative Stress: Role in Hypertension.
Hypertension
Structure and Function of the Hypertension Variant A486V of G Protein-coupled Receptor Kinase 4.
Hypertension
The impact of alpha1-adrenoceptors up-regulation accompanied by the impairment of beta-adrenergic vasodilatation in hypertension.
Hypertension
The importance of G protein-coupled receptor kinase 4 (GRK4) in pathogenesis of salt sensitivity, salt sensitive hypertension and response to antihypertensive treatment.
Hypertension
The role of G protein-coupled receptor kinase 4 in cardiomyocyte injury after myocardial infarction.
Lung Neoplasms
GRK6 Depletion Induces HIF Activity in Lung Adenocarcinoma.
Multiple Myeloma
Design, Synthesis, and Characterization of 4-Aminoquinazolines as Potent Inhibitors of the G Protein-Coupled Receptor Kinase 6 (GRK6) for the Treatment of Multiple Myeloma.
Multiple Myeloma
Down-regulated G protein-coupled receptor kinase 6 leads to apoptosis in multiple myeloma MM1R cells.
Multiple Myeloma
Protein expression and purification of G-protein coupled receptor kinase 6 (GRK6), toward structure-based drug design and discovery for multiple myeloma.
Multiple Myeloma
[Effect of G Protein-coupled Receptor Kinase 6 on Proliferation and Apoptosis of Multiple Myeloma Cells and Its Mechanisms].
Myocardial Infarction
The role of G protein-coupled receptor kinase 4 in cardiomyocyte injury after myocardial infarction.
Neoplasm Metastasis
G protein-coupled receptor kinase 6 deficiency promotes angiogenesis, tumor progression, and metastasis.
Neoplasm Metastasis
G protein-coupled receptor kinase GRK5 phosphorylates moesin and regulates metastasis in prostate cancer.
Neoplasm Metastasis
GRK3 is essential for metastatic cells and promotes prostate tumor progression.
Neoplasms
c-Src, Insulin-Like Growth Factor I Receptor, G-Protein-Coupled Receptor Kinases and Focal Adhesion Kinase are Enriched Into Prostate Cancer Cell Exosomes.
Neoplasms
G protein-coupled receptor kinase 5 modifies cancer cell resistance to paclitaxel.
Neoplasms
G protein-coupled receptor kinase 6 deficiency promotes angiogenesis, tumor progression, and metastasis.
Neoplasms
G-protein coupled receptor kinase 5 regulates prostate tumor growth.
Neoplasms
GIT1 promotes lung cancer cell metastasis through modulating Rac1/Cdc42 activity and is associated with poor prognosis.
Neoplasms
GRK3 is essential for metastatic cells and promotes prostate tumor progression.
Neoplasms
GRK5 functions as an oncogenic factor in non-small-cell lung cancer.
Neoplasms
High expression of GRK3 is associated with favorable prognosis in pancreatic ductal adenocarcinoma.
Neoplasms
MicroRNA-760 acts as a tumor suppressor in gastric cancer development via inhibiting G-protein-coupled receptor kinase interacting protein-1 transcription.
Nephrosclerosis
G-protein-coupled receptor kinase 4 polymorphisms and blood pressure response to metoprolol among African Americans: sex-specificity and interactions.
Neuroblastoma
Endogenous G protein-coupled receptor kinase 6 Regulates M3 muscarinic acetylcholine receptor phosphorylation and desensitization in human SH-SY5Y neuroblastoma cells.
Obesity
Single Nucleotide Polymorphisms in the G-Protein Coupled Receptor Kinase 5 (GRK5) Gene are associated with Plasma LDL-Cholesterol Levels in Humans.
Osteoarthritis
GRK5 Inhibition Attenuates Cartilage Degradation via Decreased NF-?B Signaling.
Parkinson Disease
Correction: S-Nitrosylation of G protein-coupled receptor kinase 6 and Casein kinase 2 alpha modulates their kinase activity toward alpha-synuclein phosphorylation in an animal model of Parkinson's disease.
Parkinson Disease
Effect of Tianqi antitremor granules on behavioral manifestations and expression of G protein-coupled receptor kinase 6 and ?-arrestin1 in levodopa-induced dyskinesia in a rat model of Parkinson's disease.
Parkinson Disease
G protein-coupled receptor kinase 5, overexpressed in the alpha-synuclein up-regulation model of Parkinson's disease, regulates bcl-2 expression.
Parkinson Disease
Lack of association between G-protein coupled receptor kinase 5 gene and Parkinson's disease.
Parkinson Disease
Role of G-protein coupled receptor kinase 5 gene in cognitive impairment in Parkinson's disease.
Parkinson Disease
S-Nitrosylation of G protein-coupled receptor kinase 6 and Casein kinase 2 alpha modulates their kinase activity toward alpha-synuclein phosphorylation in an animal model of Parkinson's disease.
Parkinson Disease
The role of G-protein-coupled receptor kinase 5 in pathogenesis of sporadic Parkinson's disease.
Parkinson Disease
[Effects of Chinese herbal medicine Tianqi Pingchan Granule on G protein-coupled receptor kinase 6 involved in the prevention of levodopa-induced dyskinesia in rats with Parkinson disease].
Pre-Eclampsia
G protein-coupled receptor kinase 4 gene variants are not associated with preeclampsia in Northern Han Chinese.
Prostatic Neoplasms
G protein-coupled receptor kinase GRK5 phosphorylates moesin and regulates metastasis in prostate cancer.
Retinal Neovascularization
Beta-adrenoreceptor (?-AR) agonism influences retinal responses to hypoxia in a mouse model of retinopathy of prematurity.
Retinoblastoma
G-protein-coupled receptor kinase 3- and protein kinase C-mediated desensitization of the PACAP receptor type 1 in human Y-79 retinoblastoma cells.
Spinal Cord Injuries
Expression of G-protein-coupled receptor kinase 6 (GRK6) after acute spinal cord injury in adult rat.
Status Epilepticus
The expression of G protein-coupled receptor kinase 5 and its interaction with dendritic marker microtubule-associated protein-2 after status epilepticus.
Stillbirth
Enhanced Uterine Contractility and Stillbirth in Mice Lacking G Protein-Coupled Receptor Kinase 6 (GRK6): Implications for Oxytocin Receptor Desensitization.
Stomach Neoplasms
MicroRNA-760 acts as a tumor suppressor in gastric cancer development via inhibiting G-protein-coupled receptor kinase interacting protein-1 transcription.
Takotsubo Cardiomyopathy
G-protein-coupled receptor kinase 5 polymorphism and Takotsubo cardiomyopathy.
Takotsubo Cardiomyopathy
No association of G-protein-coupled receptor kinase 5 or ?-adrenergic receptor polymorphisms with Takotsubo cardiomyopathy in a large Australian cohort.
Thyroid Cancer, Papillary
Overexpression of G Protein-Coupled Receptor Kinase 6 (GRK6) Is Associated with Progression and Poor Prognosis of Papillary Thyroid Carcinoma.
Whooping Cough
Endothelin-1 activates endothelial cell nitric-oxide synthase via heterotrimeric G-protein betagamma subunit signaling to protein jinase B/Akt.
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A142V
the mutation is associated with hypertension
A486V
the mutation is associated with hypertension. There is an increased rate of autophosphorylation of a number of residues in the mutant relative to the wild type enzyme
K216M/K217M
a kinase-dead GRK4gamma mutant, that interacts with GalphaS and Galpha13 in the same way as the wild-type GRK4gamma
R65L
the mutation is associated with hypertension
A486V
-
naturally occuring functional polymorphism, the mutation leads to increased GRK4 activity and phosphorylation of dopamine receptors, phenotype
C561S/C562S/C565S
-
site-directed mutagenesis, mutation of palmitoylation sites, the mutant protein retains its ability to phosphorylate rhodopsin, albeit with a 5fold higher Km and 2fold lower Vmax compared with those of wild-type GRK6
F527D
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
G298S
the complete loss-of-function variant is identified in heterotaxy patients
I165E
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
I165E/F527D
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
I39E
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
I39E/I165E
-
site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
K216M/K217M
-
site-directed mutagenesis, kinase-dead GRK4 mutant, overexpression in HEK-293 cells leads to partially desensitization of GPCR
K220R
-
kinase-dead mutant
Q41L
the variant is identified in heterotaxy patients
R304C
the variant is identified in heterotaxy patients
R65L/A142V/A486V
-
co-expression in CHO cells with the dopamine D1 receptor causes enhanced desensitization and agonist-independent phosphorylation of the receptor
S500A
the mutant shows decreased activity compared to the wild type enzyme
T10A
the mutant shows increased activity compared to the wild type enzyme
T425M
the variant is identified in heterotaxy patients
A142V
-
expression of the GRK4gamma mutant in transgenic mice leads to development of hypertension and lack of D1 agonist-induced diuresis and natriuresis in the mice
A142V
-
naturally occuring functional polymorphism, the mutation leads to increased GRK4 activity and phosphorylation of dopamine receptors, phenotype
K215R
-
site-directed mutagenesis, dominant negative mutants of GRK5 or GRK6, overexpression of mutant GRK6 or mutant GRK5 in NG108-15 mouse neuroblastoma x rat glioma hybrid cells results in selective increase in secretin-stimulated cyclic AMP response, the dominant negative mutant of GRK5 has no effect on cAMP response
K215R
-
site-directed mutagenesis, inactive, dominant negative mutant of GRK6, 30fold overexpression in SH-SY5Y cells produces a 50% suppression of endogenous M3 muscarinic acetylcholine receptor phosphorylation and desensitization by the wild-type enzyme, GRK5 K215R mutant overexpression has no effect
K215R
-
the GRK5 mutant binds to alpha-synuclein but does not phosphorylate it
K215R
-
kinase-dead mutant of GRK5
K215R
-
a GRK5 kinase-dead mutant, fails to phosphorylate p53
K215R
-
catalytically inactive mutant is not able to rescue the phenotype of HeLa GRK5 knockdown cells
K215R
-
inactive kinase mutant is not able to rescue the phenotype of PC3 cells that stably express lentiviral small hairpin RNA and target GRK5. Over expression of kinase-inactive K215R, GRK5, or GRK5 knockdown leads to G2/M arrest in the cell cycle
R65L
-
naturally occuring functional polymorphism, the mutation leads to increased GRK4 activity and phosphorylation of dopamine receptors, phenotype
R65L
-
naturally occuring functional polymorphism, the mutation leads to increased GRK4 activity and phosphorylation of dopamine receptors, the mutation plays a role in blood pressure regulation in adolescents and young adults, phenotype
additional information
-
overexpression of wild-type GRK6 increase the endogenous M3 muscarinic acetylcholine receptor phosphorylation and desensitization level
additional information
-
transient overexpression of wild-type GRK6 in NG108-15 mouse neuroblastoma x rat glioma hybrid cells results in highly selective inhibition of secretin-stimulated cyclic AMP accumulation without afffecting the A2 adenosine receptor responsiveness to cAMP, while overexpression of wild-type GRK5 leads to a partly selective inhibition of secretin-stimulated cyclic AMP response and to inhibition of A2 adenosine receptor responsiveness
additional information
-
GRK short hairpin RNA knockdown, GRK5 knockout results in altered central and lung M2 muscarinic receptor regulation, with normal heart M2 receptor regulation, while GRK4 knockout does not result in an altered phenotype, GRK6 knockout leads to altered central dopamine receptor regulation deficient lymphocyte chemotaxis, increased acute inflammation and neutrophil chemotaxis, positive correlation between certain GRK4 polymorphisms, or haplotypes, and hypertensive disease
additional information
-
haplotypic association of the GRK5 gene with susceptibility to sporadic Parkinson's disease, the haplotype contains two functional single-nucleotide polymorphisms, m22.1 and m24, in introns of the GRK5 gene, which bind to Yin Yang-1, YY1, and cAMP response element-binding protein 1, CREB-1, respectively, and increases transcriptional activity of the reporter gene, overview
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Sallese, M.; Mariggio, S.; Collodel, G.; Moretti, E.; Piomboni, P.; Baccetti, B.; De Blasi, A.
G protein-coupled receptor kinase GRK4. Molecular analysis of the four isoforms and ultrastructural localization in spermatozoa and germinal cells
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Ambrose, C.; James, M.; Barnes, G.; Lin, C.; Bates, G.; Altherr, M.; Duyao, M.; Groot, N.; Church, D.; Wasmuth, J.J.; et al.
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Cloning and expression of GRK5: a member of the G protein-coupled receptor kinase family
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Homo sapiens (P34947)
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Stoffel, R.H.; Randall, R.R.; Premont, R.T.; Lefkowitz, R.J.; Inglese, J.
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Ghadessy, R.S.; Willets, J.M.; Kelly, E.
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Mechanisms of regulation of the expression and function of G protein-coupled receptor kinases
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Homo sapiens, Mus musculus
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Oyama, N.; Urasawa, K.; Kaneta, S.; Sakai, H.; Saito, T.; Takagi, C.; Yoshida, I.; Kitabatake, A.; Tsutsui, H.
Chronic beta-adrenergic receptor stimulation enhances the expression of G-protein coupled receptor kinases, GRK2 and GRK5, in both the heart and peripheral lymphocytes
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Homo sapiens, Rattus norvegicus
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Decreased expression of G-protein coupled receptor kinase 2 in cold thyroid nodules
Exp. Clin. Endocrinol. Diabetes
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Homo sapiens
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Picascia, A.; Capobianco, L.; Iacovelli, L.; De Blasi, A.
Analysis of differential modulatory activities of GRK2 and GRK4 on Galphaq-coupled receptor signaling
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Homo sapiens
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Willets, J.M.; Mistry, R.; Nahorski, S.R.; Challiss, R.A.
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Novel features of G protein-coupled receptor kinase 4
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The G protein-coupled receptor kinase 4 gene affects blood pressure in young normotensive twins
Am. J. Hypertens.
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2006
Homo sapiens
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Wang, Y.; Li, B.; Zhao, W.; Liu, P.; Zhao, Q.; Chen, S.; Li, H.; Gu, D.
Association study of G protein-coupled receptor kinase 4 gene variants with essential hypertension in northern Han Chinese
Ann. Hum. Genet.
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Homo sapiens
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Premont, R.T.; Gainetdinov, R.R.
Physiological roles of G protein-coupled receptor kinases and arrestins
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2007
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Ribas, C.; Penela, P.; Murga, C.; Salcedo, A.; Garcia-Hoz, C.; Jurado-Pueyo, M.; Aymerich, I.; Mayor, F.
The G protein-coupled receptor kinase (GRK) interactome: Role of GRKs in GPCR regulation and signaling
Biochim. Biophys. Acta
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Homo sapiens, Mammalia
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Lodowski, D.T.; Tesmer, V.M.; Benovic, J.L.; Tesmer, J.J.
The structure of G protein-coupled receptor kinase (GRK)-6 defines a second lineage of GRKs
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rawaka, S.; Wada, M.; Goto, S.; Karube, H.; Sakamoto, M.; Ren, C.H.; Koyama, S.; Nagasawa, H.; Kimura, H.; Kawanami, T.; Kurita, K.; Tajima, K.; Daimon, M.; Baba, M.; Kido, T.; Saino, S.; Goto, K.; Asao, H.; Kitanaka, C.; Takashita, E.; Hongo, S.; Nakamura, T.; Kayama, T.; Suzuki, Y.; Kobayashi, K.; Kat, K.a.t.a.
The role of G-protein-coupled receptor kinase 5 in pathogenesis of sporadic Parkinsons disease
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Yang, W.; Xia, S.
Mechanisms of regulation and function of G-protein-coupled receptor kinases
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Homo sapiens
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Keever, L.B.; Jones, J.E.; Andresen, B.T.
G protein-coupled receptor kinase 4gamma interacts with inactive GalphaS and Galpha13
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Tran, T.M.; Jorgensen, R.; Clark, R.B.
Phosphorylation of the beta2-adrenergic receptor in plasma membranes by intrinsic GRK5
Biochemistry
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Homo sapiens (P34947)
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Mayer, G.; Wulffen, B.; Huber, C.; Brockmann, J.; Flicke, B.; Neumann, L.; Hafenbradl, D.; Klebl, B.M.; Lohse, M.J.; Krasel, C.; Blind, M.
An RNA molecule that specifically inhibits G-protein-coupled receptor kinase 2 in vitro
RNA
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Homo sapiens (P34947)
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Wang, L.; Gesty-Palmer, D.; Fields, T.A.; Spurney, R.F.
Inhibition of WNT signaling by G protein-coupled receptor (GPCR) kinase 2 (GRK2)
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Homo sapiens
brenda
Sorriento, D.; Ciccarelli, M.; Santulli, G.; Campanile, A.; Altobelli, G.G.; Cimini, V.; Galasso, G.; Astone, D.; Piscione, F.; Pastore, L.; Trimarco, B.; Iaccarino, G.
The G-protein-coupled receptor kinase 5 inhibits NFkappaB transcriptional activity by inducing nuclear accumulation of IkappaB alpha
Proc. Natl. Acad. Sci. USA
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Homo sapiens
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Chen, X.; Zhu, H.; Yuan, M.; Fu, J.; Zhou, Y.; Ma, L.
G-protein-coupled receptor kinase 5 phosphorylates p53 and inhibits DNA damage-induced apoptosis
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Homo sapiens
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So, C.H.; Michal, A.M.; Mashayekhi, R.; Benovic, J.L.
G protein-coupled receptor kinase 5 phosphorylates nucleophosmin and regulates cell sensitivity to polo-like kinase 1 inhibition
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Michal, A.M.; So, C.H.; Beeharry, N.; Shankar, H.; Mashayekhi, R.; Yen, T.J.; Benovic, J.L.
G Protein-coupled receptor kinase 5 is localized to centrosomes and regulates cell cycle progression
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G-protein coupled receptor kinase 5 regulates prostate tumor growth
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Regulation of C3a receptor signaling in human mast cells by G protein coupled receptor kinases
PLoS ONE
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Homo sapiens
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Chakraborty, P.K.; Zhang, Y.; Coomes, A.S.; Kim, W.J.; Stupay, R.; Lynch, L.D.; Atkinson, T.; Kim, J.I.; Nie, Z.; Daaka, Y.
G protein-coupled receptor kinase GRK5 phosphorylates moesin and regulates metastasis in prostate cancer
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Homo sapiens (P34947), Homo sapiens
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Li, L.; Homan, K.T.; Vishnivetskiy, S.A.; Manglik, A.; Tesmer, J.J.; Gurevich, V.V.; Gurevich, E.V.
G protein-coupled receptor kinases of the GRK4 protein subfamily phosphorylate inactive G protein-coupled receptors (GPCRs)
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Homo sapiens (P34947)
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Allen, S.J.; Parthasarathy, G.; Darke, P.L.; Diehl, R.E.; Ford, R.E.; Hall, D.L.; Johnson, S.A.; Reid, J.C.; Rickert, K.W.; Shipman, J.M.; Soisson, S.M.; Zuck, P.; Munshi, S.K.; Lumb, K.J.
Structure and function of the hypertension variant A486V of G protein-coupled receptor kinase 4
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Homo sapiens (P32298), Homo sapiens
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Johnson, L.R.; Robinson, J.D.; Lester, K.N.; Pitcher, J.A.
Distinct structural features of G protein-coupled receptor kinase 5 (GRK5) regulate its nuclear localization and DNA-binding ability
PLoS ONE
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Homo sapiens (P34947)
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Rowlands, R.A.; Cato, M.C.; Waldschmidt, H.V.; Bouley, R.A.; Chen, Q.; Avramova, L.; Larsen, S.D.; Tesmer, J.J.G.; White, A.D.
Structure-based design of selective, covalent G protein-coupled receptor kinase 5 inhibitors
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Homo sapiens (P34947)
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Yao, S.; Wu, D.; Chen, J.; Wang, P.; Lv, X.; Huang, J.
Hypermethylation of the G protein-coupled receptor kinase 6 (GRK6) promoter inhibits binding of C/EBPalpha, and GRK6 knockdown promotes cell migration and invasion in lung adenocarcinoma cells
FEBS Open Bio
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Homo sapiens (P43250)
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Lagman, J.; Sayegh, P.; Lee, C.S.; Sulon, S.M.; Jacinto, A.Z.; Sok, V.; Peng, N.; Alp, D.; Benovic, J.L.; So, C.H.
G protein-coupled receptor kinase 5 modifies cancer cell resistance to paclitaxel
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Homo sapiens (P34947)
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Wu, W.; Sung, C.C.; Yu, P.; Li, J.; Chung, K.K.K.
S-nitrosylation of G protein-coupled receptor kinase 6 and casein kinase 2 alpha modulates their kinase activity toward alpha-synuclein phosphorylation in an animal model of Parkinsons disease
PLoS ONE
15
e0232019
2020
Homo sapiens (P43250)
brenda
Beyett, T.; Chen, Q.; Labudde, E.; Krampen, J.; Sharma, P.; Tesmer, J.
Characterization of a hyperphosphorylated variant of G protein-coupled receptor kinase 5 expressed in E. coli
Protein Expr. Purif.
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2020
Homo sapiens (P34947), Homo sapiens
brenda
Lessel, D.; Muhammad, T.; Casar Tena, T.; Moepps, B.; Burkhalter, M.D.; Hitz, M.P.; Toka, O.; Rentzsch, A.; Schubert, S.; Schalinski, A.; Bauer, U.M.; Kubisch, C.; Ware, S.M.; Philipp, M.
The analysis of heterotaxy patients reveals new loss-of-function variants of GRK5
Sci. Rep.
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Homo sapiens (P34947), Homo sapiens
brenda