Information on EC 2.7.11.15 - beta-adrenergic-receptor kinase and Organism(s) Homo sapiens and UniProt Accession P25098

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IUBMB Comments
Requires G-protein for activation and therefore belongs to the family of G-protein-dependent receptor kinases (GRKs). Acts on the agonist-occupied form of the receptor; also phosphorylates rhodopsin, but more slowly. Does not act on casein or histones. The enzyme is inhibited by Zn2+ and digitonin but is unaffected by cyclic-AMP (cf. EC 2.7.11.14, rhodopsin kinase and EC 2.7.11.16, G-protein-coupled receptor kinase).
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This record set is specific for:
Homo sapiens
UNIPROT: P25098
Word Map
The taxonomic range for the selected organisms is: Homo sapiens
The expected taxonomic range for this enzyme is: Eukaryota, Archaea, Bacteria
Synonyms
ark, bARKct, beta adrenergic receptor kinase, beta-adrenergic receptor kinase, beta-adrenergic receptor kinase 1, beta-adrenergic receptor kinase 2, beta-adrenergic receptor-specific kinase, beta-AR kinase, beta-ARK, beta-ARK 1, more
SYNONYM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
ark
265796
-
beta-adrenergic receptor kinase
beta-adrenergic receptor kinase 1
beta-adrenergic receptor kinase 2
265805
-
beta-adrenergic receptor-specific kinase
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-
-
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beta-AR kinase
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-
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beta-ARK
-
-
-
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beta-ARK 1
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-
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beta-ARK 2
-
-
-
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beta-receptor kinase
-
-
-
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betaARK
247
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betaARK1
247
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betaARK2
247
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G protein coupled receptor kinase
265796
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G protein-coupled receptor kinase
G protein-coupled receptor kinase 2
G protein-coupled receptor kinase 3
247
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G protein-coupled receptors kinase 2
265796
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G-protein coupled receptor kinase 2
247
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G-protein receptor kinase 2
265796
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G-protein-coupled receptor kinase 2
247
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GPCR kinase
247
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GRK
247
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GRK5
247
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kinase (phosphorylating), beta-adrenergic-receptor
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-
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additional information
REACTION
REACTION DIAGRAM
COMMENTARY hide
ORGANISM
UNIPROT
LITERATURE
ATP + [beta-adrenergic receptor] = ADP + phospho-[beta-adrenergic receptor]
show the reaction diagram
regulation mechanism
-
REACTION TYPE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phospho group transfer
-
-
-
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SYSTEMATIC NAME
IUBMB Comments
ATP:[beta-adrenergic receptor] phosphotransferase
Requires G-protein for activation and therefore belongs to the family of G-protein-dependent receptor kinases (GRKs). Acts on the agonist-occupied form of the receptor; also phosphorylates rhodopsin, but more slowly. Does not act on casein or histones. The enzyme is inhibited by Zn2+ and digitonin but is unaffected by cyclic-AMP (cf. EC 2.7.11.14, rhodopsin kinase and EC 2.7.11.16, G-protein-coupled receptor kinase).
CAS REGISTRY NUMBER
COMMENTARY hide
102925-39-3
-
SUBSTRATE
PRODUCT                       
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
Reversibility
r=reversible
ir=irreversible
?=not specified
ATP + alpha1D-adrenergic receptor
ADP + alpha1D-adrenergic receptor phosphate
show the reaction diagram
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
show the reaction diagram
tubulin + ATP
phosphorylated-tubulin + ADP
show the reaction diagram
-
-
-
?
ATP + Ac-DEMEFTEAESNMN-NH2
ADP + Ac-DEMEFpTEAESNMN-NH2
show the reaction diagram
-
highly specific substrate with phosphorylation sites at Thr409 and Ser413
-
-
?
ATP + Ac-DEMEFTHAESNMN-NH2
ADP + Ac-DEMEFpTHAESNMN-NH2
show the reaction diagram
-
-
-
-
?
ATP + Ac-DEMKFTEAESNMN-NH2
ADP + Ac-DEMKFpTEAESNMN-NH2
show the reaction diagram
-
-
-
-
?
ATP + Ac-DEMKFTHAESNMN-NH2
ADP + Ac-DEMKFpTHAESNMN-NH2
show the reaction diagram
-
-
-
-
?
ATP + Ac-DEMSFTEAESNMN-NH2
ADP + Ac-DEMSFpTEAESNMN-NH2
show the reaction diagram
-
-
-
-
?
ATP + Ac-DEMSFTHAEANMN-NH2
ADP + Ac-DEMSFpTHAEANMN-NH2
show the reaction diagram
-
-
-
-
?
ATP + Ac-EEMEFSEAEANMN-NH2
ADP + Ac-EEMEFpSEAEANMN-NH2
show the reaction diagram
-
-
-
-
?
ATP + Ac-EEMEFSEEAANMN-NH2
ADP + Ac-EEMEFpSEEAANMN-NH2
show the reaction diagram
-
-
-
-
?
ATP + Ac-EEMEFTEVEANMN-NH2
ADP + Ac-EEMEFpTEVEANMN-NH2
show the reaction diagram
-
-
-
-
?
ATP + AGDVESFLNEA
ADP + AGDVEpSFLNEA
show the reaction diagram
-
-
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
show the reaction diagram
ATP + angiotensin receptor
ADP + phosphorylated angiotensin receptor
show the reaction diagram
ATP + beta-adrenergic receptor
ADP + beta-adrenergic receptor phosphate
show the reaction diagram
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
show the reaction diagram
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
show the reaction diagram
ATP + beta-synuclein
ADP + phosphorylated beta-synuclein
show the reaction diagram
-
-
-
-
?
ATP + beta2-adrenergic receptor
ADP + beta2-adrenergic receptor phosphate
show the reaction diagram
ATP + beta2-adrenergic receptor
ADP + phosphorylated beta2-adrenergic receptor
show the reaction diagram
-
-
-
-
?
ATP + calcium-sensing receptor
ADP + calcium-sensing receptor phosphate
show the reaction diagram
ATP + DEKKEESEESDDDMG
ADP + DEKKEEpSEESDDDMG
show the reaction diagram
-
-
-
-
?
ATP + DEMEFTEAESNMN
ADP + Ac-EEMEFpTEVEANMN-NH2
show the reaction diagram
-
best substrate
-
-
?
ATP + DEMEFTEAESNMN
ADP + DEMEFpTEAESNMN
show the reaction diagram
-
-
-
-
?
ATP + DEMEFTEAESNMNDLVSEYQ
ADP + DEMEFpTEAESNMNDLVSEYQ
show the reaction diagram
-
-
-
-
?
ATP + dephospho-beta-tubulin
ADP + phosphorylated beta-tubulin
show the reaction diagram
ATP + DREAM
ADP + phosphorylated DREAM
show the reaction diagram
ATP + EAYEMPSEEGYQD
ADP + EAYEMPpSEEGYQD
show the reaction diagram
-
-
-
-
?
ATP + EEMEFSEAEANMN
ADP + EEMEFpSEAEANMN
show the reaction diagram
-
-
-
-
?
ATP + epidermal growth factor receptor
ADP + phosphorylated epidermal growth factor receptor
show the reaction diagram
-
-
-
-
?
ATP + epithelial Na+ channel
ADP + phosphorylated epithelial Na+ channel
show the reaction diagram
ATP + ezrin
ADP + phosphorylated ezrin
show the reaction diagram
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
show the reaction diagram
ATP + GEGMDEMEFTEAESNMN
ADP + GEGMDEMEFpTEAESNMN
show the reaction diagram
-
-
-
-
?
ATP + GMEGLGTDITVI
ADP + GMEGLGpTDITVI
show the reaction diagram
-
-
-
-
?
ATP + GPEPWETISEEMNM
ADP + GPEPWEpTISEEMNM
show the reaction diagram
-
-
-
-
?
ATP + GRDKYKTLRQIRQG
ADP + GRDKYKpTLRQIRQG
show the reaction diagram
-
-
-
-
?
ATP + histone deacetylase 6
ADP + phosphorylated histone deacetylase 6
show the reaction diagram
-
phosphorylation at Ser-670
-
-
?
ATP + insulin receptor substrate-1
ADP + phosphorylated insulin receptor substrate-1
show the reaction diagram
-
phosphorylation at Ser-307
-
-
?
ATP + KKELQSLYRGFK
ADP + KKELQpSLYRGFK
show the reaction diagram
-
-
-
-
?
ATP + LDTMESDSEVEAI
ADP + LDTMESDpSEVEAI
show the reaction diagram
-
-
-
-
?
ATP + MEPEGESYEDPPQ
ADP + MEPEGEpSYEDPPQ
show the reaction diagram
-
-
-
-
?
ATP + MNDLVSEYQQYQ
ADP + MNDLVpSEYQQYQ
show the reaction diagram
-
-
-
-
?
ATP + Mst2 protein
ADP + phosphorylated Mst2 protein
show the reaction diagram
-
-
-
-
?
ATP + Nedd4 protein
ADP + phosphorylated Nedd4 protein
show the reaction diagram
-
-
-
-
?
ATP + Nedd4-2 protein
ADP + phosphorylated Nedd4-2 protein
show the reaction diagram
-
-
-
-
?
ATP + p38 mitogen-activated protein kinase
ADP + phosphorylated p38 mitogen-activated protein kinase
show the reaction diagram
-
-
-
-
?
ATP + PDEgamma
ADP + phosphorylated PDEgamma
show the reaction diagram
ATP + PDGFRbeta
ADP + phosphorylated PDGFRbeta
show the reaction diagram
-
-
-
-
?
ATP + PGWEERTHTDGRVF
ADP + PGWEERpTHTDGRVF
show the reaction diagram
-
-
-
-
?
ATP + phosducin
ADP + phosphorylated phosducin
show the reaction diagram
ATP + phosphodiesterase gamma
ADP + phosphorylated phosphodiesterase gamma
show the reaction diagram
-
-
-
-
?
ATP + platelet-activating factor receptor
ADP + phospho-platelet-activating factor receptor
show the reaction diagram
PAF receptor acts as substrate
-
-
?
ATP + platelet-derived growth factor receptor-beta protein
ADP + phosphorylated platelet-derived growth factor receptor
show the reaction diagram
-
-
-
-
?
ATP + PPLDDYTHSIPEN
ADP + PPLDDYpTHSIPEN
show the reaction diagram
-
-
-
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?
ATP + PRAEAEDSFL
ADP + PRAEAEDpSFL
show the reaction diagram
-
-
-
-
?
ATP + R-smad
ADP + phosphorylated R-smad
show the reaction diagram
-
GRK2
-
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
show the reaction diagram
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
-
-
-
-
?
ATP + rhodopsin
ADP + rhodopsin phosphate
show the reaction diagram
-
cf. EC 2.7.11.14, rhodopsin is also a substrate of GRK2
-
-
?
ATP + ribosomal protein P2
ADP + phosphorylated ribosomal protein P2
show the reaction diagram
ATP + RRREEEEESAAA
?
show the reaction diagram
-
-
-
-
?
ATP + RRREEEEESAAA
ADP + RRREEEEEpSAAA
show the reaction diagram
-
-
-
-
?
ATP + Smad2 protein
ADP + phosphorylated Smad2 protein
show the reaction diagram
-
-
-
-
?
ATP + synuclein
ADP + phosphorylated synuclein
show the reaction diagram
ATP + tubulin
ADP + phosphorylated tubulin
show the reaction diagram
ATP + VKCQKLTDDHVQF
ADP + VKCQKLpTDDHVQF
show the reaction diagram
-
-
-
-
?
ATP + VPSDNIDSQGRNC
ADP + VPSDNIDpSQGRNC
show the reaction diagram
-
-
-
-
?
ATP + VSKTETSQVAPA
ADP + VSKTETpSQVAPA
show the reaction diagram
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
show the reaction diagram
-
-
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
show the reaction diagram
ATP + [neurotensin receptor]
ADP + phospho-[neurotensin receptor]
show the reaction diagram
-
the enzyme phosphorylates only the C-terminal serine residues
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
show the reaction diagram
ezrin + ATP
phosphorylated ezrin + ADP
show the reaction diagram
-
-
-
-
?
moesin + ATP
phosphorylated moesin + ADP
show the reaction diagram
-
-
-
-
?
radixin + ATP
phosphorylated radixin + ADP
show the reaction diagram
-
-
-
-
?
additional information
?
-
NATURAL SUBSTRATE
NATURAL PRODUCT
REACTION DIAGRAM
ORGANISM
UNIPROT
COMMENTARY
(Substrate) hide
LITERATURE
(Substrate)
COMMENTARY
(Product) hide
LITERATURE
(Product)
REVERSIBILITY
r=reversible
ir=irreversible
?=not specified
ATP + alpha1D-adrenergic receptor
ADP + alpha1D-adrenergic receptor phosphate
show the reaction diagram
inhibition of vascular smooth muscle G protein-coupled receptor kinase 2 enhances alpha1D-adrenergic receptor constriction and signalling, overview
-
-
?
ATP + protein
ADP + phosphoprotein
show the reaction diagram
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
show the reaction diagram
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
show the reaction diagram
-
colocalization of GRK2, GRK5, alpha-synuclein, and tau in neurodegenerative disorders characterized by fibrillary tau inclusions and/or alpha-synuclein-enriched Lewy bodies, overview
-
-
?
ATP + angiotensin receptor
ADP + phosphorylated angiotensin receptor
show the reaction diagram
-
phosphorylation by GRK2 preceeds the binding of arrestins, which inhibits the seven-transmembrane receptor, but initiates internalization, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + beta-adrenergic receptor phosphate
show the reaction diagram
-
the mechanism of myocardial beta-adrenergic receptor desensitization during cardiac surgery involves GRK2, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
show the reaction diagram
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
show the reaction diagram
ATP + beta2-adrenergic receptor
ADP + beta2-adrenergic receptor phosphate
show the reaction diagram
-
role of GRK activity in the regulation of beta2 adrenergic signaling, feedback mechanism, overview
-
-
?
ATP + beta2-adrenergic receptor
ADP + phosphorylated beta2-adrenergic receptor
show the reaction diagram
-
-
-
-
?
ATP + calcium-sensing receptor
ADP + calcium-sensing receptor phosphate
show the reaction diagram
homologous desensitization of G protein-coupled receptors is generally mediated by GRKs through phosphorylation-dependent and independent mechanisms, GRK2 can phosphorylate calcium-sensing receptor and, along with beta-arrestins, can attenuate calcium-sensing receptor-mediated signaling, mechanism, overview
-
-
?
ATP + DREAM
ADP + phosphorylated DREAM
show the reaction diagram
-
i.e. downstream regulatory element antagonist modulator protein, GRK2 mediates phosphorylation of DREAM/potassium channel interacting protein KChIP3, a multifunctional protein of the neuronal calcium sensor subfamily of Ca2+-binding proteins with specific roles in different cell compartments, regulating membrane trafficking of Kv4.2 potassium channel, phosphorylation of Ser95 affects cell surface localization, but not Kv4 channel tetramerization, overview
-
-
?
ATP + epithelial Na+ channel
ADP + phosphorylated epithelial Na+ channel
show the reaction diagram
-
channel inactivation
-
-
?
ATP + ezrin
ADP + phosphorylated ezrin
show the reaction diagram
-
phosphorylation of ezrin affects the 7TM receptor mediated cytoskeletal reorganization
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
show the reaction diagram
ATP + PDEgamma
ADP + phosphorylated PDEgamma
show the reaction diagram
-
phosphorylation of PDEgamma possibly stimulates EGFR-mediated ERK activation
-
-
?
ATP + PDGFRbeta
ADP + phosphorylated PDGFRbeta
show the reaction diagram
-
-
-
-
?
ATP + phosducin
ADP + phosphorylated phosducin
show the reaction diagram
-
phosducin is activated to inhibit Gbetagamma protein
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
show the reaction diagram
-
-
-
-
?
ATP + ribosomal protein P2
ADP + phosphorylated ribosomal protein P2
show the reaction diagram
-
activation of P2
-
-
?
ATP + synuclein
ADP + phosphorylated synuclein
show the reaction diagram
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
show the reaction diagram
-
-
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
show the reaction diagram
-
-
-
-
?
ATP + [neurotensin receptor]
ADP + phospho-[neurotensin receptor]
show the reaction diagram
-
the enzyme phosphorylates only the C-terminal serine residues
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
show the reaction diagram
-
GRK2 and GRK3, receptor activation
-
-
?
ezrin + ATP
phosphorylated ezrin + ADP
show the reaction diagram
-
-
-
-
?
moesin + ATP
phosphorylated moesin + ADP
show the reaction diagram
-
-
-
-
?
radixin + ATP
phosphorylated radixin + ADP
show the reaction diagram
-
-
-
-
?
additional information
?
-
METALS and IONS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
Ca2+
-
inhibits GRK2
additional information
-
no activation by Ca2+
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
(6R)-6-([[(1S)-1-(5-fluoro-2-methoxyphenyl)ethyl]amino]methyl)-4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine-3-carboxamide
-
1-[(3R)-1-benzylpyrrolidin-3-yl]-3-[(3,5-dimethyl-1,2-oxazol-4-yl)methyl]urea
-
2-(3-methoxybenzyl)-7-(1H-pyrazol-4-yl)phthalazin-1(2H)-one
-
2-[(2-amino-2-oxoethyl)(propan-2-yl)amino]-N-[(1S)-1-(naphthalen-2-yl)ethyl]acetamide
-
2-[(3S)-3-[(phenylsulfanyl)methyl]pyrrolidin-1-yl]-N-(pyridin-3-ylmethyl)acetamide
-
3-(3-fluoro-4-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-(3-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-(4-fluoro-3-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-benzyl-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-benzyl-6-(1H-pyrazol-5-yl)quinazolin-4(3H)-one
-
3-benzyl-6-(pyridin-4-yl)quinazolin-4(3H)-one
-
3-benzyl-6-(pyrimidin-5-yl)quinazolin-4(3H)-one
-
3-benzyl-7-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-benzyl-7-fluoro-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-benzyl-8-fluoro-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-cyano-N-[[(3R)-1-(thiophen-2-ylmethyl)piperidin-3-yl]methyl]benzamide
-
3-[(1R)-1-(3-methoxyphenyl)ethyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-[(1S)-1-(3-methoxyphenyl)ethyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-[1-(3-methoxyphenyl)-3-(methylamino)propyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-[3-(4-fluorophenoxy)benzyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
3-[3-(difluoromethoxy)benzyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
-
4-acetyl-N-[(2S)-2-(dimethylamino)-2-(4-methoxyphenyl)ethyl]-1H-pyrrole-2-carboxamide
-
4-acetyl-N-[2-(3,4-dihydroisoquinolin-2(1H)-yl)-2-methylpropyl]-1H-pyrrole-2-carboxamide
-
4-acetyl-N-[[(3R)-1-benzylpiperidin-3-yl]methyl]-1H-pyrrole-2-carboxamide
-
5-(4-fluorophenyl)-N-[[(3S,5R,8aR)-hexahydro-1H-pyrrolo[2,1-c][1,4]oxazin-3-yl]methyl]-5-oxopentanamide
-
5-fluoro-N-(imidazo[1,2-a]pyridin-2-ylmethyl)-2-methoxybenzamide
-
balanol
CCG-224406
-
CCG224406
-
CCG258208
-
-
GRK2ct
C-terminal portion of GRK2
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N-(4-acetylphenyl)-N2-[(3-chlorophenyl)methyl]-N2-methyl-L-alaninamide
-
N-(4-cyanophenyl)-3-[4-(4-hydroxyphenyl)-3,6-dihydropyridin-1(2H)-yl]propanamide
-
N-(4-fluorophenyl)-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
-
N-[(2,6-difluorocyclohexa-1,5-dien-1-yl)methyl]-4-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
-
N-[(2,6-difluorophenyl)methyl]-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
-
N-[(2R)-2-(3,4-dihydroisoquinolin-2(1H)-yl)butyl]-N'-(1-ethyl-1H-pyrazol-4-yl)urea
-
N-[(2R)-2-(3,4-dihydroisoquinolin-2(1H)-yl)propyl]-N'-[(2S)-1-(1H-pyrrol-1-yl)propan-2-yl]urea
-
N-[(4-fluorophenyl)methyl]-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
-
N-[1-[benzyl(methyl)amino]-2-methylpropan-2-yl]-6-methyl-4-oxo-1,4-dihydropyridine-3-carboxamide
-
N2-methyl-N2-[[4-(methylsulfanyl)phenyl]methyl]-N-(1,3,5-trimethyl-1H-pyrazol-4-yl)-L-alaninamide
-
N3-[(6-fluoroquinolin-8-yl)methyl]-N-[(pyridin-3-yl)methyl]-beta-alaninamide
-
paroxetine
Takeda 103A
-
Takeda CMPD 101
-
-
Takeda CMPD 103A
-
-
59-74E
-
-
actin
-
-
actinin
-
inhibits GRK2
-
alpha-actinin
-
-
balanol
-
-
betaARKct
-
the isolated C-terminal sequence of the enzyme acts as a peptide inhibitor
-
Calmodulin
calveolin
-
-
-
caveolin
-
CCG215022
-
-
CCG224061
-
-
-
CCG224406
-
-
CCG258748
-
-
-
CMPD101
-
CMPD103A
-
-
-
GRK2ct
-
GRK2 inhibitor GRK2ct corresponding to the carboxyl-terminal 194 amino acids of GRK2 is expressed in failing cardiac fibroblasts using an adenoviral-mediated approach driven by the CMV promoter. Inhibition restores beta-agonist stimulated inhibition of collagen synthesis and decreases collagen synthesis in response to TGF beta stimulation
-
GSK180736A
-
-
heparin
nitric oxide
-
inhibits GRK2 by S-nitrosylation at Cys340, regulatory function of S-nitrosylation
paroxetine
-
-
Protein kinase C inhibitor H7
weak
-
RKIP
-
-
RNA aptamer C13
-
development and synthesis of a highly specific RNA aptamer C13 that potently inhibits GRK2 by binding to it kinase domain, binding kinetics, inhibitor secondary structure, overview
-
S-nitrosothiols
-
inhibit GRK2 by S-nitrosylation at Cys340, regulatory function of S-nitrosylation
-
additional information
-
ACTIVATING COMPOUND
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
beta-arrestin
-
required for phosphorylation activity and receptor substrate endocytosis
-
G protein
-
G protein betagamma-subunit
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from brain, stimulates the phosphorylation of rhodopsin, but not of the peptide RRREEEEESAAA, an intact N-terminus of the gamma subunit is required for stimulation, but not for kinase binding, endoprotease Lys-C blocks stimulation, Gbetagamma binds to the C-terminal region of beta-ARK containing the pleckstrin homology domain, role of the G protein gamma-subunit
-
G protein Gbetagamma subunits
-
required for activity, 20fold stimulation with substrate rhodopsin, 2 regulatory Gbetagamma binding sites: one N-terminal domain of GRK2, and one C-terminal within the pleckstrin homology domain, both sites are functionally different, overview
-
isoproterenol
requirement, beta-agonist, beta-adrenergic receptor as substrate
phosphatidylinositol 4,5-bisphosphate
-
binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity
phosphatidylserine
-
binding of GRK2 and GRK3 via their pleckstrin homology domains, activate the phosphorylation activity
PIP2
-
activates GRK2 through binding to its PH domain
platelet activating factor
requirement, agonist, beta-adrenergic receptor as substrate
additional information
-
KM VALUE [mM]
SUBSTRATE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.0339
DEMEFTEAESNMN
0.0324
DEMEFTEAESNMNDLVSEYQ
-
0.054
EEMEFSEAEANMN
-
pH and temperature not specified in the publication
-
0.1
GEGMDEMEFTEAESNMN
-
additional information
additional information
-
kinetics
-
IC50 VALUE [mM]
INHIBITOR
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
IMAGE
0.000019
2-(3-methoxybenzyl)-7-(1H-pyrazol-4-yl)phthalazin-1(2H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00275
3-(3-fluoro-4-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000006
3-(3-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000018
3-(4-fluoro-3-methoxybenzyl)-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000095
3-benzyl-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.1
3-benzyl-6-(1H-pyrazol-5-yl)quinazolin-4(3H)-one
Homo sapiens
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.025
3-benzyl-6-(pyridin-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.1
3-benzyl-6-(pyrimidin-5-yl)quinazolin-4(3H)-one
Homo sapiens
IC50 above 0.1 mM, pH and temperature not specified in the publication
0.0041
3-benzyl-7-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000278
3-benzyl-7-fluoro-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000472
3-benzyl-8-fluoro-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000013
3-[(1R)-1-(3-methoxyphenyl)ethyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00211
3-[(1S)-1-(3-methoxyphenyl)ethyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000012
3-[1-(3-methoxyphenyl)-3-(methylamino)propyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000078
3-[3-(4-fluorophenoxy)benzyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.000206
3-[3-(difluoromethoxy)benzyl]-6-(1H-pyrazol-4-yl)quinazolin-4(3H)-one
Homo sapiens
pH and temperature not specified in the publication
0.00005
balanol
Homo sapiens
pH 7.4, 20°C
0.000009
N-(4-fluorophenyl)-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.02
N-[(2,6-difluorocyclohexa-1,5-dien-1-yl)methyl]-4-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
Homo sapiens
pH and temperature not specified in the publication
0.00001
N-[(2,6-difluorophenyl)methyl]-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
Homo sapiens
IC50 below 0.00001 mM, pH and temperature not specified in the publication
0.00001
N-[(4-fluorophenyl)methyl]-3-[[4-oxo-6-(1H-pyrazol-4-yl)quinazolin-3(4H)-yl]methyl]benzamide
Homo sapiens
IC50 below 0.00001 mM, pH and temperature not specified in the publication
0.0000041
RNA aptamer C13
Homo sapiens
-
inhibition of GRK2, kinetics, overview
-
SPECIFIC ACTIVITY [µmol/min/mg]
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
additional information
pH OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
7.4
assay at
7
-
assay at
7.5
-
assay at
TEMPERATURE OPTIMUM
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
20
assay at
20
-
assay at
22
-
assay at room temperature
25
-
assay at
37
-
assay at
ORGANISM
COMMENTARY hide
LITERATURE
UNIPROT
SEQUENCE DB
SOURCE
SOURCE TISSUE
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
SOURCE
peripheral blood leukocytes
Manually annotated by BRENDA team
GRK2 is increased in hypertension
Manually annotated by BRENDA team
GRK2 is increased in hypertension
Manually annotated by BRENDA team
-
40-50% co-localization of GRK2 with neurofibrillary tangles in Alzheimer's disease
Manually annotated by BRENDA team
myeloid and lymphoid leukemia cell lines, high expression of beta-ARK 1
Manually annotated by BRENDA team
moderate expression of beta-ARK 2
Manually annotated by BRENDA team
high expression of beta-ARK 1
Manually annotated by BRENDA team
-
primary isolated from hearts of patients in the end-stage of heart failure undergoing heart transplantation
Manually annotated by BRENDA team
-
colocalization of GRK2 and tau in intracellular neurofibrillary tangles and isolated paired helical filaments
Manually annotated by BRENDA team
-
neuroblastoma cell line
Manually annotated by BRENDA team
-
increased expression of GRK3 in hyperfunctioning thyroid nodule
Manually annotated by BRENDA team
-
prepared without lymphocytic infiltrations in the tumor, GRKs expression patterns, low expression of GRK2, and high expression level of GRK3
Manually annotated by BRENDA team
high expression of beta-ARK 1
Manually annotated by BRENDA team
-
an osteosarcoma cell line
Manually annotated by BRENDA team
additional information
LOCALIZATION
ORGANISM
UNIPROT
COMMENTARY hide
GeneOntology No.
LITERATURE
SOURCE
GENERAL INFORMATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
malfunction
physiological function
UNIPROT
ENTRY NAME
ORGANISM
NO. OF AA
NO. OF TRANSM. HELICES
MOLECULAR WEIGHT[Da]
SOURCE
SEQUENCE
LOCALIZATION PREDICTION?
ARBK1_HUMAN
689
0
79574
Swiss-Prot
other Location (Reliability: 2)
MOLECULAR WEIGHT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
80000
-
x * 80000, GRK2, SDS-PAGE
additional information
SUBUNIT
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
?
-
x * 80000, GRK2, SDS-PAGE
additional information
POSTTRANSLATIONAL MODIFICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
phosphoprotein
additional information
-
mechanisms of regulation of GRK protein stability and degradation, e.g. via ubiquitination or protease cleavage, overview
CRYSTALLIZATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
crystal structures of human GRK2 in complex with Gbetagamma in the presence and absence of the AGC (protein kinase A, kinase G, and kinase C subfamily) kinase inhibitor balanol is determined. Balanol stabilizes the kinase domain of GRK2 in a slightly more closed conformation distinct from that of the protein kinase A balanol complex
PROTEIN VARIANTS
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
D110A
the Galphaq binding site mutant of GRK 2 inhibits the inositol phosphate signal significantly less than wild-type GRK2, the mutant GRK 2 D110A still inhibitS inositol phosphate formation by 22.35
D110A/K220R
the mutant inhibits the inositol phosphate signal significantly less than wild-type GRK2, but does not differ significantly from wild-type GRK2 in its ability to inhibit calcium-sensing receptor signaling
K220R
S670A
additional information
GENERAL STABILITY
ORGANISM
UNIPROT
LITERATURE
glycerol stabilizes
-
PURIFICATION (Commentary)
ORGANISM
UNIPROT
LITERATURE
recombinant beta-ARK 1, expressed in Sf9 cells
-
recombinant GRK2 from insect Sf9 cells by ammonium sulfate fractionation, hydrophobic interaction and heparin affinity chromatography
-
recombinant GST-tagged GRK2 and GRK2 C-terminal or N-terminal domains from insect Sf9 cells by ion exchange and heparin affinity chromatography
-
recombinant GST-tagged wild-type and truncation mutant GRK2s from Escherichia coli by glutathione affinity chromatography, recombinant wild-type GRK2 from Sf9 insect cells by heparin affinity chromatography and gel filtration
-
CLONED (Commentary)
ORGANISM
UNIPROT
LITERATURE
beta ARK locus segregated with the long arm of chromosome 11, centromeric to 11q13
cloning and sequencing
expressed in HEK-293 cells
expressed in Sf9 clls using the baculovirus expression system
expression of GRK2, with or without inhibitor GRK2ct, in vascular smooth emuscle of transgenic mice, phenotypes, overview
adenovirus-mediated gene transfer and expression of inhibitor betaARKct in primary myocytes isolated from hearts of patients in the end-stage of heart failure undergoing heart transplantation, betaARK1 activity is inhibited but beta-adrenergic signaling and contractile function are improved
-
beta-ARK 1 is cloned and expressed in SF9 cells using the baculovirus expression system
-
cDNA encoding beta-ARK 1 is cloned and sequenced, very similar sequences of bovine and human kinases
cDNA encoding beta-ARK 2 is cloned, expressed in COS-7 cells and sequenced
co-expression of rat thyrotropin receptor with GRK2 and GRK3 in HEK-293 cells, receptor phosphorylation occurs with both enzymes
-
DNAs encoding the C-terminal domains Gly556-Ser670 and Pro466-Leu689 are cloned and expressed in Escherichia coli
-
expressed in NG-108-15 cells
-
expression in COS7 cells
expression of GRK2 in Spodoptera frugiperda Sf9 cells
-
expression of GST-tagged GRK2 and GRK2 C-terminal or N-terminal domains in Spodoptera frugiperda Sf9 cells using the baculovirus transfection method
-
expression of GST-tagged wild-type and truncation mutant GRK2s in Escherichia coli, expression of wild-type GRK2 in Spodoptera frugiperda Sf9 cells using the baculovirus infection system, expression of wild-type and truncation mutant GRK2s in HEK-293 cells
-
expression of kinase-dead GRK2 mutant and of the N-terminal region of GRK2, residues Ala2-Thr187, in HEK-293 cells
-
expression of wild-type and mutant GRK2
overexpression of the C-terminus of betaARK in ventricular cardiomyocytes and in the myocardium of rabbits suffering heart failure by adenoviral gene transfer, co-expression of N-terminal deletion mutant of phosducin, leading to increase in contractility of the cells due to inhibition of Gbetagamma subunits rather than to beta-adrenergic receptor resensitization, betaARK additionally stimulates cAMP production
-
overexpression of wild-type and kinase-dead mutant GRK2 in murine 3T3-L1 adipocytes via adenovirus infection system leading to inhibition of Galphaq/11 signaling, including tyrosine phosphorylation of Galphaq11 and cdc42-associated phosphatidylinositol 3-kinase activity, overexpression of the inactive muant, but not of wild-type enzyme, inhibits endothelin-1-induced Ser612 phosphorylation of insulin receptor substrate-1, and restores activation of the pathway
-
regulation of GRK2 expression, analysis, overview
-
stable overexpression of GFP-fusion K220R mutant GRK2 and GFP-fusion K220R mutant GRK3 in SH-SY5Y neuroblastoma cells via adenovirus infection system
-
very similar sequences of bovine and human kinases
EXPRESSION
ORGANISM
UNIPROT
LITERATURE
a 4fold increase in GRK2 expression in the failing cardiac fibroblasts is detected compared with normal controls
-
APPLICATION
ORGANISM
UNIPROT
COMMENTARY hide
LITERATURE
diagnostics
-
GRK2 levels in heart and peripheral lymphocytes correlate well, therefore the lymphocytic enzyme level might be a very suitable marker for determination for the sympathetic drive to heart failure during clinical course and treatment of human congestive heart failure patients
medicine
REF.
AUTHORS
TITLE
JOURNAL
VOL.
PAGES
YEAR
ORGANISM (UNIPROT)
PUBMED ID
SOURCE
Benovic, J.L.; Stone, W.C.; Huebner, K.; Croce, C.; Caron, M.G.; Lefkowitz, R.J.
cDNA cloning and chromosomal localization of the human beta-adrenergic receptor kinase
FEBS Lett.
283
122-126
1991
Homo sapiens (P25098), Homo sapiens
Manually annotated by BRENDA team
Chuang, T.T.; Sallese, M.; Ambrosini, G.; Parruti, G.; De Blasi, A.
High expression of beta-adrenergic receptor kinase in human peripheral blood leukocytes. Isoproterenol and platelet activating factor can induce kinase translocation
J. Biol. Chem.
267
6886-6892
1992
Bos taurus, Homo sapiens, Homo sapiens (P25098)
Manually annotated by BRENDA team
Fushman, D.; Najmabadi-Haske, T.; Cahill, S.; Zheng, J.; LeVine, H.; Cowburn, D.
The solution structure and dynamics of the pleckstrin homology domain of G protein-coupled receptor kinase 2 (beta-adrenergic receptor kinase 1). A binding partner of Gbetagamma subunits
J. Biol. Chem.
273
2835-2843
1998
Homo sapiens (P25098)
Manually annotated by BRENDA team
Penn, R.B.; Benovic, J.L.
Structure of the human gene encoding the beta-adrenergic receptor kinase
J. Biol. Chem.
269
14924-14930
1994
Homo sapiens (P25098), Homo sapiens
Manually annotated by BRENDA team
Dunham, I.; Shimizu, N.; Roe, B.A.; Chissoe, S.; Hunt, A.R.; Collins, J.E.; Bruskiewich, R.; Beare, D.M.; Clamp, M.; Smink, L.J.; Ainscough, R.; Almeida, J.P.; Babbage, A.; Bagguley, C.; Bailey, J.; Barlow, K.; Bates, K.N.; Beasley, O.; Bird, C.P.; Blakey, S.; Bridgeman, A.M.; Buck, D.; Burgess, J.; Burrill, W.D.; O'Brien, K.P.; et al.
The DNA sequence of human chromosome 22
Nature
402
489-495
1999
Homo sapiens (P35626)
Manually annotated by BRENDA team
Parruti, G.; Ambrosini, G.; Sallese, M.; De Blasi, A.
Molecular cloning, functional expression and mRNA analysis of human beta-adrenergic receptor kinase 2
Biochem. Biophys. Res. Commun.
190
475-481
1993
Bos taurus, Homo sapiens (P35626), Homo sapiens
Manually annotated by BRENDA team
Söhlemann, P.; Hekman, M.; Buchen, C.; Elce, J.S.; Lohse, M.J.
Purification and functional characterization of beta-adrenergic receptor kinase expressed in insect cells
FEBS Lett.
324
59-62
1993
Bos taurus, Homo sapiens
Manually annotated by BRENDA team
Petrofski, J.A.; Koch, W.J.
The beta-adrenergic receptor kinase in heart failure
J. Mol. Cell. Cardiol.
35
1167-1174
2003
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Iino, M.; Shibano, T.
Substrate recognition mechanism of human beta-adrenergic receptor kinase 1 based on a three-dimensional model structure
Drug Des. Discov.
14
145-155
1996
Homo sapiens
Manually annotated by BRENDA team
Haske, T.N.; DeBlasi, A.; LeVine, H.
An intact N terminus of the gamma subunit is required for the Gbetagamma stimulation of rhodopsin phosphorylation by human beta-adrenergic receptor kinase-1 but not for kinase binding
J. Biol. Chem.
271
2941-2948
1996
Homo sapiens
Manually annotated by BRENDA team
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, Rattus norvegicus
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Williams, M.L.; Hata, J.A.; Schroder, J.; Rampersaud, E.; Petrofski, J.; Jakoi, A.; Milano, C.A.; Koch, W.J.
Targeted beta-adrenergic receptor kinase (betaARK1) inhibition by gene transfer in failing human hearts
Circulation
109
1590-1593
2004
Homo sapiens
Manually annotated by BRENDA team
Yoshida, N.; Haga, K.; Haga, T.
Identification of sites of phosphorylation by G-protein-coupled receptor kinase 2 in beta-tubulin
Eur. J. Biochem.
270
1154-1163
2003
Homo sapiens
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Li, Z.; Laugwitz, K.L.; Pinkernell, K.; Pragst, I.; Baumgartner, C.; Hoffmann, E.; Rosport, K.; Munch, G.; Moretti, A.; Humrich, J.; Lohse, M.J.; Ungerer, M.
Effects of two Gbetagamma-binding proteins - N-terminally truncated phosducin and beta-adrenergic receptor kinase C terminus (betaARKct)--in heart failure
Gene Ther.
10
1354-1361
2003
Homo sapiens
Manually annotated by BRENDA team
Rapacciuolo, A.; Suvarna, S.; Barki-Harrington, L.; Luttrell, L.M.; Cong, M.; Lefkowitz, R.J.; Rockman, H.A.
Protein kinase A and G protein-coupled receptor kinase phosphorylation mediates beta-1 adrenergic receptor endocytosis through different pathways
J. Biol. Chem.
278
35403-35411
2003
Homo sapiens
Manually annotated by BRENDA team
Eichmann, T.; Lorenz, K.; Hoffmann, M.; Brockmann, J.; Krasel, C.; Lohse, M.J.; Quitterer, U.
The amino-terminal domain of G-protein-coupled receptor kinase 2 is a regulatory Gbeta gamma binding site
J. Biol. Chem.
278
8052-8057
2003
Homo sapiens
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Usui, I.; Imamura, T.; Babendure, J.L.; Satoh, H.; Lu, J.C.; Hupfeld, C.J.; Olefsky, J.M.
G protein-coupled receptor kinase 2 mediates endothelin-1-induced insulin resistance via the inhibition of both Galphaq/11 and insulin receptor substrate-1 pathways in 3T3-L1 adipocytes
Mol. Endocrinol.
19
2760-2768
2005
Homo sapiens
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Whalen, E.J.; Foster, M.W.; Matsumoto, A.; Ozawa, K.; Violin, J.D.; Que, L.G.; Nelson, C.D.; Benhar, M.; Keys, J.R.; Rockman, H.A.; Koch, W.J.; Daaka, Y.; Lefkowitz, R.J.; Stamler, J.S.
Regulation of beta-adrenergic receptor signaling by S-nitrosylation of G-protein-coupled receptor kinase 2
Cell
129
511-522
2007
Homo sapiens, Mus musculus
Manually annotated by BRENDA team
Ruiz-Gomez, A.; Mellstroem, B.; Tornero, D.; Morato, E.; Savignac, M.; Holguin, H.; Aurrekoetxea, K.; Gonzalez, P.; Gonzalez-Garcia, C.; Cena, V.; Mayor, F.; Naranjo, J.R.
G protein-coupled receptor kinase 2-mediated phosphorylation of downstream regulatory element antagonist modulator regulates membrane trafficking of Kv4.2 potassium channel
J. Biol. Chem.
282
1205-1215
2007
Homo sapiens
Manually annotated by BRENDA team
Takahashi, M.; Uchikado, H.; Caprotti, D.; Weidenheim, K.M.; Dickson, D.W.; Ksiezak-Reding, H.; Pasinetti, G.M.
Identification of G-protein coupled receptor kinase 2 in paired helical filaments and neurofibrillary tangles
J. Neuropathol. Exp. Neurol.
65
1157-1169
2006
Homo sapiens
Manually annotated by BRENDA team
Desai, A.N.; Salim, S.; Standifer, K.M.; Eikenburg, D.C.
Involvement of G protein-coupled receptor kinase (GRK) 3 and GRK2 in down-regulation of the alpha2B-adrenoceptor
J. Pharmacol. Exp. Ther.
317
1027-1035
2006
Homo sapiens
Manually annotated by BRENDA team
Hansen, J.L.; Theilade, J.; Aplin, M.; Sheikh, S.P.
Role of G-protein-coupled receptor kinase 2 in the heart--do regulatory mechanisms open novel therapeutic perspectives?
Trends Cardiovasc. Med.
16
169-177
2006
Homo sapiens
Manually annotated by BRENDA team
Yang, W.; Xia, S.
Mechanisms of regulation and function of G-protein-coupled receptor kinases
World J. Gastroenterol.
12
7753-7757
2006
Homo sapiens
Manually annotated by BRENDA team
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
Homo sapiens (P25098), Homo sapiens
Manually annotated by BRENDA team
Bulcao, C.F.; Pandalai, P.K.; DSouza, K.M.; Merrill, W.H.; Akhter, S.A.
Uncoupling of myocardial beta-adrenergic receptor signaling during coronary artery bypass grafting: the role of GRK2
Ann. Thorac. Surg.
86
1189-1194
2008
Homo sapiens
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Lorenz, S.; Frenzel, R.; Paschke, R.; Breitwieser, G.E.; Miedlich, S.U.
Functional desensitization of the extracellular calcium-sensing receptor is regulated via distinct mechanisms: role of G protein-coupled receptor kinases, protein kinase C and beta-arrestins
Endocrinology
148
2398-2404
2007
Homo sapiens (P35626)
Manually annotated by BRENDA team
Xin, W.; Tran, T.M.; Richter, W.; Clark, R.B.; Rich, T.C.
Roles of GRK and PDE4 activities in the regulation of beta2 adrenergic signaling
J. Gen. Physiol.
131
349-364
2008
Homo sapiens
Manually annotated by BRENDA team
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
Manually annotated by BRENDA team
Kahsai, A.; Zhu, S.; Fenteany, G.
G protein-coupled receptor kinase 2 activates radixin, regulating membrane protrusion and motility in epithelial cells
Biochim. Biophys. Acta
1803
300-310
2010
Homo sapiens
Manually annotated by BRENDA team
DSouza, K.M.; Malhotra, R.; Philip, J.L.; Staron, M.L.; Theccanat, T.; Jeevanandam, V.; Akhter, S.A.
G protein-coupled receptor kinase-2 is a novel regulator of collagen synthesis in adult human cardiac fibroblasts
J. Biol. Chem.
286
15507-15516
2011
Homo sapiens
Manually annotated by BRENDA team
Valanne, S.; Myllymaeki, H.; Kallio, J.; Schmid, M.R.; Kleino, A.; Murumaegi, A.; Airaksinen, L.; Kotipelto, T.; Kaustio, M.; Ulvila, J.; Esfahani, S.S.; Engstroem, Y.; Silvennoinen, O.; Hultmark, D.; Parikka, M.; Raemet, M.
Genome-wide RNA interference in Drosophila cells identifies G protein-coupled receptor kinase 2 as a conserved regulator of NF-kappaB signaling
J. Immunol.
184
6188-6198
2010
Danio rerio, Drosophila melanogaster, Homo sapiens
Manually annotated by BRENDA team
Tesmer, J.J.; Tesmer, V.M.; Lodowski, D.T.; Steinhagen, H.; Huber, J.
Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol
J. Med. Chem.
53
1867-1870
2010
Homo sapiens (P25098), Homo sapiens
Manually annotated by BRENDA team
Asai, D.; Murata, M.; Toita, R.; Kawano, T.; Nakashima, H.; Kang, J.H.
Role of amino acid residues surrounding the phosphorylation site in peptide substrates of G protein-coupled receptor kinase 2 (GRK2)
Amino Acids
48
2875-2880
2016
Homo sapiens
Manually annotated by BRENDA team
Inagaki, S.; Ghirlando, R.; Vishnivetskiy, S.A.; Homan, K.T.; White, J.F.; Tesmer, J.J.; Gurevich, V.V.; Grisshammer, R.
G protein-coupled receptor kinase 2 (GRK2) and 5 (GRK5) exhibit selective phosphorylation of the neurotensin receptor in vitro
Biochemistry
54
4320-4329
2015
Homo sapiens
Manually annotated by BRENDA team
Asai, D.; Toita, R.; Murata, M.; Katayama, Y.; Nakashima, H.; Kang, J.H.
Peptide substrates for G protein-coupled receptor kinase 2
FEBS Lett.
588
2129-2132
2014
Homo sapiens
Manually annotated by BRENDA team
So, C.H.; Michal, A.; Komolov, K.E.; Luo, J.; Benovic, J.L.
G protein-coupled receptor kinase 2 (GRK2) is localized to centrosomes and mediates epidermal growth factor-promoted centrosomal separation
Mol. Biol. Cell
24
2795-2806
2013
Homo sapiens
Manually annotated by BRENDA team
Asai, D.; Murata, M.; Toita, R.; Kawano, T.; Nakashima, H.; Kang, J.
A high-affinity peptide substrate for G protein-coupled receptor kinase 2 (GRK2)
Amino Acids
51
973-976
2019
Homo sapiens
Manually annotated by BRENDA team
Kang, J.H.; Toita, R.; Kawano, T.; Murata, M.; Asai, D.
Design of substrates and inhibitors of G protein-coupled receptor kinase 2 (GRK2) based on its phosphorylation reaction
Amino Acids
52
863-870
2020
Homo sapiens
Manually annotated by BRENDA team
Kuwasako, K.; Sekiguchi, T.; Nagata, S.; Jiang, D.; Hayashi, H.; Murakami, M.; Hattori, Y.; Kitamura, K.; Kato, J.
Inhibitory effects of two G protein-coupled receptor kinases on the cell surface expression and signaling of the human adrenomedullin receptor
Biochem. Biophys. Res. Commun.
470
894-899
2016
Homo sapiens (P25098)
Manually annotated by BRENDA team
Xu, G.; Gaul, M.D.; Liu, Z.; DesJarlais, R.L.; Qi, J.; Wang, W.; Krosky, D.; Petrounia, I.; Milligan, C.M.; Hermans, A.; Lu, H.R.; Huang, D.Z.; Xu, J.Z.; Spurlino, J.C.
Hit-to-lead optimization and discovery of a potent, and orally bioavailable G protein coupled receptor kinase 2 (GRK2) inhibitor
Bioorg. Med. Chem. Lett.
30
127602
2020
Homo sapiens (P25098), Homo sapiens
Manually annotated by BRENDA team
Ye, W.; Yang, S.; Zhang, L.; Deng, Z.; Li, W.; Zhang, J.; Zhang, L.; Yun, Y.; Chen, A.; Cao, D.
Multistep virtual screening for rapid identification of G protein-coupled receptors kinase 2 inhibitors for heart failure treatment
Chemometr. Intell. Lab. Syst.
185
32-40
2019
Homo sapiens (P25098)
-
Manually annotated by BRENDA team
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