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ATP + a G protein-coupled receptor
ADP + a phosphorylated G protein-coupled receptor
ATP + activated form of G protein-coupled receptors
ADP + phosphorylated G protein-coupled receptors
-
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
ATP + alpha1-adrenergic receptor
ADP + alpha1-adrenergic receptor phosphate
GRK5 is also active with alpha1-adrenergic receptors. GRK5 activity, but not GRK2 activity, toward alpha1-adrenergic receptors can lead to transactivation of the tyrosine kinase receptor for epidermal growth factor in myocytes, cf. EC 2.7.11.15
-
-
?
ATP + ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
ATP + beta 2-adrenergic receptor
ADP + phosphorylated beta 2-adrenergic receptor
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
desensitization of the receptor by GRK4, GRK5, and GRK6
-
-
?
ATP + BLT1 receptor
ADP + phosphorylated BLT1 receptor
ATP + central M2 muscarinic receptor
ADP + phosphorylated central M2 muscarinic receptor
ATP + CXCR4 receptor
ADP + phosphorylated CXCR4 receptor
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
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 + protein
ADP + phosphoprotein
major autophosphorylation sites are Ser484 and Thr485
-
-
?
ATP + protein p105
ADP + phosphorylated protein p105
ATP + rhodopsin
ADP + phosphorylated rhodopsin
ATP + rhodopsin
ADP + rhodopsin phosphate
cf. EC 2.7.11.14, rhodopsin is also a substrate of GRK5
-
-
?
ATP + tau protein
ADP + phosphorylated tau protein
-
-
-
?
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 + 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 + ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
-
-
-
?
ATP + ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
-
-
?
ATP + beta 2-adrenergic receptor
ADP + phosphorylated beta 2-adrenergic receptor
phosphorylation in an agonist-dependent manner, phosphorylates the C-terminal tail regions of both receptor proteins
-
-
?
ATP + beta 2-adrenergic receptor
ADP + phosphorylated beta 2-adrenergic 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 + BLT1 receptor
ADP + phosphorylated BLT1 receptor
-
GRK6
-
-
?
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 + central M2 muscarinic receptor
ADP + phosphorylated central M2 muscarinic receptor
-
desensitization of the receptor by GRK5, GRK5 regulates pulmmonary responses by activation of the airway receptor, but does not regulate the peripheral cardiac muscarinic receptors
-
-
?
ATP + central M2 muscarinic receptor
ADP + phosphorylated central M2 muscarinic receptor
-
GRK5
-
-
?
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 + 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 + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
GRK4
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
GRK4
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
-
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
rapid desensitization of the receptor by GRK4 and GRK6, Na+/H+ exchanger activity of the receptor, overview
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
GRK4 and GRK6
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
dopamine D1 receptors in IEC-6 rapidly desensitize to D1-like agonist stimulation and GRK 6 isozymes A and B, but not GRK 4, appear to be involved in agonist-mediated responsiveness and desensitization
-
-
?
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
-
phosphorylation has a regulatory role
-
-
?
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
-
the GPCRs possess multiple phosphorylation sites for serine/threonine kinases
-
-
?
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 + protein p105
ADP + phosphorylated protein p105
-
-
-
-
?
ATP + protein p105
ADP + phosphorylated protein p105
-
recombinant GST-tagged p105, residues 497-968, substrate, GRK5 binds and phosphorylates p105, to which arrestin-2 is already C-terminally bound
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
GRK5 phosphorylates rhodopsin in a light-dependent manner, phosphorylates the C-terminal tail region
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
reaction only with GRK4alpha isoform, no reaction with GRK4beta, GRK4gamma, GRK4delta
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
light-activated rhodopsin, recombinant isoforms mGRK6-A, mGRK6-B, and mGRK-C, the latter showing highest activity
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
urea treated outer segments of 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
-
-
-
?
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 + [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]
-
-
-
-
?
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
?
-
-
GRK5 elevates blood pressure in vascular smooth muscle via Gi signaling involing the beta1-adrenergic receptor, mechanism overview
-
-
?
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
?
-
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
?
-
-
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
?
-
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
?
-
GRK5 also phosphorylates rhodopsin, cf. EC 2.7.11.14
-
-
?
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
?
-
isoform GRK5 binds DNA in vitro
-
-
?
additional information
?
-
-
G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP
-
-
?
additional information
?
-
-
no interaction of the RH domains of GRK5 and GRK6 with Galpha proteins. GRK5 contains a DNA-binding nuclear localization sequence that allows its binding to DNA and its localization in the nucleus upon GPCR activation, interaction with other oroteins, detailed overview
-
-
?
additional information
?
-
-
G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview
-
-
?
additional information
?
-
-
GRK5 defects can cause obstructive airway diseases such as asthma
-
-
?
additional information
?
-
-
GRKs are involved in diverse physiological processes and pathologies, overview
-
-
?
additional information
?
-
-
the variable C-terminal extension of GRK6 constitutes an accessorial autoregulatory domain
-
-
?
additional information
?
-
-
GRK5 performs autophosphorylation
-
-
?
additional information
?
-
-
structure-activity relationships of the enzyme C-terminus, overview
-
-
?
additional information
?
-
-
the GRKs are specific for GPCRs and arrestins, overview
-
-
?
additional information
?
-
-
arrestin-2 and GRK5, not GRK6, interact with NFkappaB1 p105 and negatively regulate lipopolysaccharide-stimulated ERK1/2 activation in macrophages, overview
-
-
?
additional information
?
-
G protein-coupled receptors and Toll-like receptors play a crucial role in the regulation of macrophage biology and innate immunity, overview
-
-
?
additional information
?
-
G protein-coupled receptors and Toll-like receptors play a crucial role in the regulation of macrophage biology and innate immunity, overview
-
-
?
additional information
?
-
G protein-coupled receptors are involved in regulating pain signaling in the context of inflammation. G protein-coupled receptor kinases modulate signaling through these receptors, GRK6 controls post-inflammatory visceral hyperalgesia, overview
-
-
?
additional information
?
-
GRK5 is important for myocardial regulation, and is up-regulated in the dysfunctional heart. But GRK5 also is a nuclear a class II histone deacetylase kinase that plays a key role in maladaptive cardiac hypertrophy apparently independent of any action directly on G protein coupled receptors, overview. Chronic Gq signaling results in the translocation of GRK5 to the nucleus, where GRK5 activity plays a role in MEF2 activation, which has implications for induction of hypertrophic gene expression. GRK5 interacts with histone deacetylase kinases in vivo
-
-
?
additional information
?
-
-
GRK6 plays a role in determining the course of inflammation and controls chronicity and severity of dextran sodium sulphate-induced colitis in mice, overview
-
-
?
additional information
?
-
G protein-coupled receptors and Toll-like receptors play a crucial role in the regulation of macrophage biology and innate immunity, overview
-
-
?
additional information
?
-
G protein-coupled receptors and Toll-like receptors play a crucial role in the regulation of macrophage biology and innate immunity, overview
-
-
?
additional information
?
-
enzyme mainly involved in homologous desensitization of the TSH receptor
-
-
?
additional information
?
-
-
the GRK4-6 family member enzymes mediate beta-adrenergic receptor desensitization, the beta-adrenergic receptor is stimulated by agonists such as isoproterenol, cholera toxin, or forskolin, and induces cAMP production
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ATP + a G protein-coupled receptor
ADP + a phosphorylated G protein-coupled receptor
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 + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
desensitization of the receptor by GRK4, GRK5, and GRK6
-
-
?
ATP + BLT1 receptor
ADP + phosphorylated BLT1 receptor
ATP + central M2 muscarinic receptor
ADP + phosphorylated central M2 muscarinic receptor
-
desensitization of the receptor by GRK5, GRK5 regulates pulmmonary responses by activation of the airway receptor, but does not regulate the peripheral cardiac muscarinic receptors
-
-
?
ATP + CXCR4 receptor
ADP + phosphorylated CXCR4 receptor
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
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 + moesin
ADP + phosphorylated moesin
phosphorylation at Thr66
-
-
?
ATP + protein p105
ADP + phosphorylated protein p105
-
-
-
-
?
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 + 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
-
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 + ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
-
-
-
?
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 + 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 + 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 + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
GRK4
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
rapid desensitization of the receptor by GRK4 and GRK6, Na+/H+ exchanger activity of the receptor, overview
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
-
dopamine D1 receptors in IEC-6 rapidly desensitize to D1-like agonist stimulation and GRK 6 isozymes A and B, but not GRK 4, appear to be involved in agonist-mediated responsiveness and desensitization
-
-
?
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
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ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
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phosphorylation has a regulatory role
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ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
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regulation mechanism of GRK5, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview
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ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
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ATP + [G protein-coupled receptor]
ADP + [G protein-coupled receptor]phosphate
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GRK4-6
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ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
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ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
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ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor] phosphate
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ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
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ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
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ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
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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
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ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
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ATP + [G-protein-coupled receptor]
ADP + [G-protein-coupled receptor]phosphate
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additional information
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GRK5 elevates blood pressure in vascular smooth muscle via Gi signaling involing the beta1-adrenergic receptor, mechanism overview
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additional information
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enzyme is involved in fertilization
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additional information
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enzyme is involved in fertilization
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additional information
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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
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additional information
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GRKs are involved in diverse physiological processes and pathologies, overview
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additional information
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the enzyme is involved in GPCR signal transduction pathways and desensitization
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additional information
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the GRK4 isozymes are differentially regulated, overview
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additional information
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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
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additional information
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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
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additional information
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GRK4 is involved in activity of dopamine receptors in renal proximal tubules and mediates sodium reabsorption and blood pressure regulation
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additional information
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GRK4 is involved in activity of dopamine receptors in renal proximal tubules and mediates sodium reabsorption and blood pressure regulation
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additional information
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GRK6 is a key regulator of dopaminergic signaling and lymphocyte chemotaxis
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additional information
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G protein-coupled receptor kinases and arrestins are key participants in the canonical pathways leading to phosphorylation-dependent G protein-coupled receptor, GPCR, desensitization, endocytosis, intracellular trafficking and resensitization as well as in the modulation of important intracellular signaling cascades by GPCR, structure-function relationships, overview. GRK activity is tightly modulated by mechanisms including phosphorylation by different kinases and interaction with several cellular proteins such as calmodulin, caveolin or RKIP
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additional information
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G protein-coupled receptors are involved in the regulation of diverse physiological processes, mechanisms of G protein-coupled receptor desensitization, e.g. by phosphorylation or feedback inhibition, overview
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additional information
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GRK5 defects can cause obstructive airway diseases such as asthma
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additional information
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GRKs are involved in diverse physiological processes and pathologies, overview
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additional information
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the variable C-terminal extension of GRK6 constitutes an accessorial autoregulatory domain
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additional information
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arrestin-2 and GRK5, not GRK6, interact with NFkappaB1 p105 and negatively regulate lipopolysaccharide-stimulated ERK1/2 activation in macrophages, overview
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additional information
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G protein-coupled receptors and Toll-like receptors play a crucial role in the regulation of macrophage biology and innate immunity, overview
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additional information
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G protein-coupled receptors and Toll-like receptors play a crucial role in the regulation of macrophage biology and innate immunity, overview
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additional information
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G protein-coupled receptors are involved in regulating pain signaling in the context of inflammation. G protein-coupled receptor kinases modulate signaling through these receptors, GRK6 controls post-inflammatory visceral hyperalgesia, overview
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additional information
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GRK5 is important for myocardial regulation, and is up-regulated in the dysfunctional heart. But GRK5 also is a nuclear a class II histone deacetylase kinase that plays a key role in maladaptive cardiac hypertrophy apparently independent of any action directly on G protein coupled receptors, overview. Chronic Gq signaling results in the translocation of GRK5 to the nucleus, where GRK5 activity plays a role in MEF2 activation, which has implications for induction of hypertrophic gene expression. GRK5 interacts with histone deacetylase kinases in vivo
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additional information
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GRK6 plays a role in determining the course of inflammation and controls chronicity and severity of dextran sodium sulphate-induced colitis in mice, overview
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additional information
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G protein-coupled receptors and Toll-like receptors play a crucial role in the regulation of macrophage biology and innate immunity, overview
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additional information
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G protein-coupled receptors and Toll-like receptors play a crucial role in the regulation of macrophage biology and innate immunity, overview
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additional information
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enzyme mainly involved in homologous desensitization of the TSH receptor
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additional information
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the GRK4-6 family member enzymes mediate beta-adrenergic receptor desensitization, the beta-adrenergic receptor is stimulated by agonists such as isoproterenol, cholera toxin, or forskolin, and induces cAMP production
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C561S/C562S/C565S
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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
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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
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site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
I165E/F527D
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site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
I39E
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site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
I39E/I165E
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site-directed mutagenesis, mutant structure in comparison to the wild-type enzyme
K220R
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kinase-dead mutant
Q41L
the variant is identified in heterotaxy patients
R304C
the variant is identified in heterotaxy patients
R65L/A142V/A486V
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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
K215R
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inactive dominant negative mutants of GRK5 or GRK6, overexpression of the GRK5 mutant in myometrial cells does not influence beta-adrenergic receptor sensitivity, while overexpression of GRK6 mutant leads to a 70% increase in isoproterenol-stimulated beta-adrenergic signaling via the beta-adrenergic receptor
A142V
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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
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naturally occuring functional polymorphism, the mutation leads to increased GRK4 activity and phosphorylation of dopamine receptors, phenotype
A142V
the mutation is associated with hypertension
A486V
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naturally occuring functional polymorphism, the mutation leads to increased GRK4 activity and phosphorylation of dopamine receptors, phenotype
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
K215R
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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
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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
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the GRK5 mutant binds to alpha-synuclein but does not phosphorylate it
K215R
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kinase-dead mutant of GRK5
K215R
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a GRK5 kinase-dead mutant, fails to phosphorylate p53
K215R
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catalytically inactive mutant is not able to rescue the phenotype of HeLa GRK5 knockdown cells
K215R
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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
K216M/K217M
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site-directed mutagenesis, kinase-dead GRK4 mutant, overexpression in HEK-293 cells leads to partially desensitization of GPCR
K216M/K217M
a kinase-dead GRK4gamma mutant, that interacts with GalphaS and Galpha13 in the same way as the wild-type GRK4gamma
R65L
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naturally occuring functional polymorphism, the mutation leads to increased GRK4 activity and phosphorylation of dopamine receptors, phenotype
R65L
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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
R65L
the mutation is associated with hypertension
additional information
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construction of transgenic mice overexpressing GRK5 2fold in vascular smooth muscle leading to hypertension in the mutant mice with a 25-35% increase in blood pressure, which segregates with sex, male show higher blood pressure than female mice, and is dependent on Gi-mediated signaling, inhibition of the latter by pertussis toxin or inhibition of beta1-adrenergic receptor activity restore blood pressure to normal level
additional information
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overexpression of wild-type GRK6 increase the endogenous M3 muscarinic acetylcholine receptor phosphorylation and desensitization level
additional information
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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
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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
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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
additional information
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construction of GRK5 deletion mutant mice
additional information
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construction of isozymes mGRK6-A, mGRK6-B, mGRK-C, and mGRK-D by alternative splicing, recombinant isoforms mGRK6-A, mGRK6-B, and mGRK-C are membrane-associated, recombinant isoform mGRK6-D is inactive and located in the nucleus, structure-activity relationships of the enzyme C-terminus, overview
additional information
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construction of transgenic tissue specific or knockout mice
additional information
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phenotypes of several GRK and arrestin knockout mice mutants and of transgenic mice overexpressing GRK4 or GRK5, overview
additional information
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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, knockout mice phenotypes, detailed overview
additional information
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GRK5 knockdown results in enhanced IkappaB kinase-mediated p105 phosphorylation and degradation, and correlates well with an enhanced LPS-stimulated ERK1/2 phosphorylation
additional information
capsaicin-induced referred hyperalgesia post-colitis is increased in GRK6-deficient mice compared to wild-type mice. However, referred hyperalgesia post-colitis is not affected by ablation of GRK6. GRK6 overexpression inhibits the in vitro sensitization of the capsaicin receptor TRPVI by interleukin 1beta, overview
additional information
cardiac GRK5 overexpression augments hypertrophy in vivo, pressure overload causes GRK5 nuclear accumulation in vivo, overview
additional information
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severity of colitis is increased in GRK6-deficient and GRK6+/- mice and is accompanied by increased keratinocyte-derived chemokine levels and increased granulocyte infiltration, the chemotactic response of GRK6-/- granulocytes to supernatants of colon cultures is enhanced, phenotype, 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
J. Biol. Chem.
272
10188-10195
1997
Homo sapiens (P32298), Homo sapiens
brenda
Sallese, M.; Lombardi, M.S.; De Blasi, A.
Two isoforms of G protein-coupled receptor kinase 4 identified by molecular cloning
Biochem. Biophys. Res. Commun.
199
848-854
1994
Homo sapiens (P32298)
brenda
Ambrose, C.; James, M.; Barnes, G.; Lin, C.; Bates, G.; Altherr, M.; Duyao, M.; Groot, N.; Church, D.; Wasmuth, J.J.; et al.
A novel G protein-coupled receptor kinase gene cloned from 4p16.3
Hum. Mol. Genet.
1
697-703
1992
Homo sapiens (P32298)
brenda
Kunapuli, P.; Benovic, J.L.
Cloning and expression of GRK5: a member of the G protein-coupled receptor kinase family
Proc. Natl. Acad. Sci. USA
90
5588-5592
1993
Homo sapiens (P34947)
brenda
Premont, R.T.; Koch, W.J.; Inglese, J.; Lefkowitz, R.J.
Identification, purification, and characterization of GRK5, a member of the family of G protein-coupled receptor kinases
J. Biol. Chem.
269
6832-6841
1994
Bos taurus (P43249)
brenda
Stoffel, R.H.; Randall, R.R.; Premont, R.T.; Lefkowitz, R.J.; Inglese, J.
Palmitoylation of G protein-coupled receptor kinase, GRK6. Lipid modification diversity in the GRK family
J. Biol. Chem.
269
27791-27794
1994
Homo sapiens (P43250)
brenda
Benovic, J.L.; Gomez, J.
Molecular cloning and expression of GRK6. A new member of the G protein-coupled receptor kinase family
J. Biol. Chem.
268
19521-19527
1993
Homo sapiens (P43250)
brenda
Fehr, C.; Fickova, M.; Hiemke, C.; Reuss, S.; Dahmen, N.
Molecular cloning of rat G-protein-coupled receptor kinase 6 (GRK6) from brain tissue, and its mRNA expression in different brain regions and peripheral tissues
Brain Res. Mol. Brain Res.
49
278-282
1997
Rattus norvegicus (P97711)
brenda
Nagayama, Y.; Tanaka, K.; Hara, T.; Namba, H.; Yamashita, S.; Taniyama, K.; Niwa, M.
Involvement of G protein-coupled receptor kinase 5 in homologous desensitization of the thyrotropin receptor
J. Biol. Chem.
271
10143-10148
1996
Rattus norvegicus (Q62833)
brenda
Walker, J.K.; Gainetdinov, R.R.; Feldman, D.S.; McFawn, P.K.; Caron, M.G.; Lefkowitz, R.J.; Premont, R.T.; Fisher, J.T.
G protein-coupled receptor kinase 5 regulates airway responses induced by muscarinic receptor activation
Am. J. Physiol.
286
L312-319
2004
Mus musculus
brenda
Fraga, S.; Jose, P.A.; Soares-da-Silva, P.
Involvement of G protein-coupled receptor kinase 4 and 6 in rapid desensitization of dopamine D1 receptor in rat IEC-6 intestinal epithelial cells
Am. J. Physiol.
287
R772-779
2004
Rattus norvegicus
brenda
Ghadessy, R.S.; Willets, J.M.; Kelly, E.
G protein-coupled receptor kinase 6 (GRK6) selectively regulates endogenous secretin receptor responsiveness in NG108-15 cells
Br. J. Pharmacol.
138
660-670
2003
Homo sapiens
brenda
Penela, P.; Ribas, C.; Mayor, F.
Mechanisms of regulation of the expression and function of G protein-coupled receptor kinases
Cell. Signal.
15
973-981
2003
Homo sapiens, Mus musculus
brenda
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
Circ. J.
69
987-990
2005
Homo sapiens, Rattus norvegicus
brenda
Keys, J.R.; Zhou, R.H.; Harris, D.M.; Druckman, C.A.; Eckhart, A.D.
Vascular smooth muscle overexpression of G protein-coupled receptor kinase 5 elevates blood pressure, which segregates with sex and is dependent on Gi-mediated signaling
Circulation
112
1145-1153
2005
Bos taurus
brenda
Simon, V.; Robin, M.T.; Legrand, C.; Cohen-Tannoudji, J.
Endogenous G protein-coupled receptor kinase 6 triggers homologous beta-adrenergic receptor desensitization in primary uterine smooth muscle cells
Endocrinology
144
3058-3066
2003
Rattus norvegicus
brenda
Voigt, C.; Holzapfel, H.P.; Paschke, R.
Decreased expression of G-protein coupled receptor kinase 2 in cold thyroid nodules
Exp. Clin. Endocrinol. Diabetes
113
102-106
2005
Homo sapiens
brenda
Vatter, P.; Stoesser, C.; Samel, I.; Gierschik, P.; Moepps, B.
The variable C-terminal extension of G-protein-coupled receptor kinase 6 constitutes an accessorial autoregulatory domain
FEBS J.
272
6039-6051
2005
Mus musculus
brenda
Picascia, A.; Capobianco, L.; Iacovelli, L.; De Blasi, A.
Analysis of differential modulatory activities of GRK2 and GRK4 on Galphaq-coupled receptor signaling
Methods Enzymol.
390
337-353
2004
Homo sapiens
brenda
Kohout, T.A.; Lefkowitz, R.J.
Regulation of G protein-coupled receptor kinases and arrestins during receptor desensitization
Mol. Pharmacol.
63
9-18
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Mus musculus
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Willets, J.M.; Mistry, R.; Nahorski, S.R.; Challiss, R.A.
Specificity of G protein-coupled receptor kinase 6-mediated phosphorylation and regulation of single-cell M3 muscarinic acetylcholine receptor signaling
Mol. Pharmacol.
64
1059-1068
2003
Homo sapiens
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Neve, K.A.
Novel features of G protein-coupled receptor kinase 4
Mol. Pharmacol.
69
673-676
2006
Homo sapiens
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Zhu, H.; Lu, Y.; Wang, X.; Treiber, F.A.; Harshfield, G.A.; Snieder, H.; Dong, Y.
The G protein-coupled receptor kinase 4 gene affects blood pressure in young normotensive twins
Am. J. Hypertens.
19
61-66
2006
Homo sapiens
brenda
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.
70
778-783
2006
Homo sapiens
brenda
Premont, R.T.; Gainetdinov, R.R.
Physiological roles of G protein-coupled receptor kinases and arrestins
Annu. Rev. Physiol.
69
511-534
2007
Homo sapiens, Mus musculus
brenda
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
1768
913-922
2007
Homo sapiens, Mammalia
brenda
Fraga, S.; Luo, Y.; Jose, P.; Zandi-Nejad, K.; Mount, D.B.; Soares-da-Silva, P.
Dopamine D1-like receptor-mediated inhibition of Cl/HCO3- exchanger activity in rat intestinal epithelial IEC-6 cells is regulated by G protein-coupled receptor kinase 6 (GRK 6)
Cell. Physiol. Biochem.
18
347-360
2006
Rattus norvegicus
brenda
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
J. Biol. Chem.
281
16785-16793
2006
Homo sapiens
brenda
Parameswaran, N.; Pao, C.S.; Leonhard, K.S.; Kang, D.S.; Kratz, M.; Ley, S.C.; Benovic, J.L.
Arrestin-2 and G protein-coupled receptor kinase 5 interact with NFkappaB1 p105 and negatively regulate lipopolysaccharide-stimulated ERK1/2 activation in macrophages
J. Biol. Chem.
281
34159-34170
2006
Mus musculus
brenda
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
J. Neurosci.
26
9227-9238
2006
Homo sapiens
brenda
Yang, W.; Xia, S.
Mechanisms of regulation and function of G-protein-coupled receptor kinases
World J. Gastroenterol.
12
7753-7757
2006
Homo sapiens
brenda
Cohn, H.I.; Harris, D.M.; Pesant, S.; Pfeiffer, M.; Zhou, R.H.; Koch, W.J.; Dorn, G.W.; Eckhart, A.D.
Inhibition of vascular smooth muscle G protein-coupled receptor kinase 2 enhances alpha1D-adrenergic receptor constriction
Am. J. Physiol. Heart Circ. Physiol.
295
H1695-H1704
2008
Mus musculus, Mus musculus (Q99MK8)
brenda
Keever, L.B.; Jones, J.E.; Andresen, B.T.
G protein-coupled receptor kinase 4gamma interacts with inactive GalphaS and Galpha13
Biochem. Biophys. Res. Commun.
367
649-655
2008
Homo sapiens (P32298)
brenda
Tran, T.M.; Jorgensen, R.; Clark, R.B.
Phosphorylation of the beta2-adrenergic receptor in plasma membranes by intrinsic GRK5
Biochemistry
46
14438-14449
2007
Homo sapiens (P34947)
brenda
Eijkelkamp, N.; Heijnen, C.J.; Elsenbruch, S.; Holtmann, G.; Schedlowski, M.; Kavelaars, A.
G protein-coupled receptor kinase 6 controls post-inflammatory visceral hyperalgesia
Brain Behav. Immun.
23
18-26
2008
Mus musculus (O70293)
brenda
Eijkelkamp, N.; Heijnen, C.J.; Lucas, A.; Premont, R.T.; Elsenbruch, S.; Schedlowski, M.; Kavelaars, A.
G protein-coupled receptor kinase 6 controls chronicity and severity of dextran sodium sulphate-induced colitis in mice
Gut
56
847-854
2007
Mus musculus
brenda
Loniewski, K.; Shi, Y.; Pestka, J.; Parameswaran, N.
Toll-like receptors differentially regulate GPCR kinases and arrestins in primary macrophages
Mol. Immunol.
45
2312-2322
2008
Mus musculus (O70293), Mus musculus (Q8VEB1), Mus musculus C57BL/6 (O70293), Mus musculus C57BL/6 (Q8VEB1)
brenda
Martini, J.S.; Raake, P.; Vinge, L.E.; DeGeorge, B.; Chuprun, J.K.; Harris, D.M.; Gao, E.; Eckhart, A.D.; Pitcher, J.A.; Koch, W.J.
Uncovering G protein-coupled receptor kinase-5 as a histone deacetylase kinase in the nucleus of cardiomyocytes
Proc. Natl. Acad. Sci. USA
105
12457-12462
2008
Mus musculus (Q8VEB1)
brenda
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
14
524-534
2008
Homo sapiens (P34947)
brenda
Wang, L.; Gesty-Palmer, D.; Fields, T.A.; Spurney, R.F.
Inhibition of WNT signaling by G protein-coupled receptor (GPCR) kinase 2 (GRK2)
Mol. Endocrinol.
23
1455-1465
2009
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
105
17818-17823
2008
Homo sapiens
brenda
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
J. Biol. Chem.
285
12823-12830
2010
Homo sapiens
brenda
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
J. Biol. Chem.
287
17088-17099
2012
Homo sapiens
brenda
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
J. Biol. Chem.
287
6928-6940
2012
Homo sapiens
brenda
Kim, J.I.; Chakraborty, P.; Wang, Z.; Daaka, Y.
G-protein coupled receptor kinase 5 regulates prostate tumor growth
J. Urol.
187
322-329
2012
Homo sapiens
brenda
Guo, Q.; Subramanian, H.; Gupta, K.; Ali, H.
Regulation of C3a receptor signaling in human mast cells by G protein coupled receptor kinases
PLoS ONE
6
e22559
2011
Homo sapiens
brenda
Bychkov, E.; Zurkovsky, L.; Garret, M.B.; Ahmed, M.R.; Gurevich, E.V.
Distinct cellular and subcellular distributions of G protein-coupled receptor kinase and arrestin isoforms in the striatum
PLoS ONE
7
e48912
2012
Rattus norvegicus
brenda
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
Cancer Res.
74
3489-3500
2014
Homo sapiens (P34947), Homo sapiens
brenda
Packiriswamy, N.; Steury, M.; McCabe, I.C.; Fitzgerald, S.D.; Parameswaran, N.
Bacterial dose-dependent role of G protein-coupled receptor kinase 5 in Escherichia coli-induced pneumonia
Infect. Immun.
84
1633-1641
2016
Mus musculus (Q8VEB1)
brenda
Franklin, J.M.; Carrasco, G.A.
G-protein receptor kinase 5 regulates the cannabinoid receptor 2-induced up-regulation of serotonin 2A receptors
J. Biol. Chem.
288
15712-15724
2013
Rattus norvegicus (Q62833)
brenda
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)
J. Biol. Chem.
290
10775-10790
2015
Homo sapiens (P34947)
brenda
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
J. Biol. Chem.
290
20360-20373
2015
Homo sapiens (P32298), Homo sapiens
brenda
Homan, K.T.; Waldschmidt, H.V.; Glukhova, A.; Cannavo, A.; Song, J.; Cheung, J.Y.; Koch, W.J.; Larsen, S.D.; Tesmer, J.J.
Crystal structure of G protein-coupled receptor kinase 5 in complex with a rationally designed inhibitor
J. Biol. Chem.
290
20649-20659
2015
Bos taurus (P43249)
brenda
Park, C.H.; Lee, J.H.; Lee, M.Y.; Lee, J.H.; Lee, B.H.; Oh, K.S.
A novel role of G protein-coupled receptor kinase 5 in urotensin II-stimulated cellular hypertrophy in H9c2UT cells
Mol. Cell. Biochem.
422
151-160
2016
Rattus norvegicus (Q62833)
brenda
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
8
e62508
2013
Homo sapiens (P34947)
brenda
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
ACS Med. Chem. Lett.
10
1628-1634
2019
Homo sapiens (P34947)
brenda
Zeng, X.; Chen, S.; Gao, Q.; Zong, W.; Jiang, D.; Zeng, G.; Zhou, L.; Chen, L.; Luo, W.; Xiao, J.; Xiao, B.; Ouyang, D.; Hu, K.
The expression of G protein-coupled receptor kinase 5 and its interaction with dendritic marker microtubule-associated protein-2 after status epilepticus
Epilepsy Res.
138
62-70
2017
Rattus norvegicus (Q62833)
brenda
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
9
605-617
2019
Homo sapiens (P43250)
brenda
Zhao, J.; Li, X.; Chen, X.; Cai, Y.; Wang, Y.; Sun, W.; Mai, H.; Yang, J.; Fan, W.; Tang, P.; Ou, M.; Zhang, Y.; Huang, X.; Zhao, B.; Cui, L.
GRK5 influences the phosphorylation of tau via GSK3beta and contributes to Alzheimer's disease
J. Cell. Physiol.
234
10411-10420
2019
Mus musculus (Q8VEB1), Mus musculus
brenda
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
Mol. Cell. Biochem.
461
103-118
2019
Homo sapiens (P34947)
brenda
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.
168
105547
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.
6
33231
2016
Homo sapiens (P34947), Homo sapiens
brenda