Please wait a moment until all data is loaded. This message will disappear when all data is loaded.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ATP + a protein
ADP + a phosphoprotein
ATP + Ac-DEMEFTEAESNMN-NH2
ADP + Ac-DEMEFpTEAESNMN-NH2
-
highly specific substrate with phosphorylation sites at Thr409 and Ser413
-
-
?
ATP + Ac-DEMEFTHAESNMN-NH2
ADP + Ac-DEMEFpTHAESNMN-NH2
-
-
-
-
?
ATP + Ac-DEMKFTEAESNMN-NH2
ADP + Ac-DEMKFpTEAESNMN-NH2
-
-
-
-
?
ATP + Ac-DEMKFTHAESNMN-NH2
ADP + Ac-DEMKFpTHAESNMN-NH2
-
-
-
-
?
ATP + Ac-DEMSFTEAESNMN-NH2
ADP + Ac-DEMSFpTEAESNMN-NH2
-
-
-
-
?
ATP + Ac-DEMSFTHAEANMN-NH2
ADP + Ac-DEMSFpTHAEANMN-NH2
-
-
-
-
?
ATP + Ac-EEMEFSEAEANMN-NH2
ADP + Ac-EEMEFpSEAEANMN-NH2
-
-
-
-
?
ATP + Ac-EEMEFSEEAANMN-NH2
ADP + Ac-EEMEFpSEEAANMN-NH2
-
-
-
-
?
ATP + Ac-EEMEFTEVEANMN-NH2
ADP + Ac-EEMEFpTEVEANMN-NH2
-
-
-
-
?
ATP + AGDVESFLNEA
ADP + AGDVEpSFLNEA
-
-
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
ATP + alpha1 beta-adrenergic receptor
ADP + phosphorylated alpha1 beta-adrenergic receptor
ATP + alpha1-adrenergic receptor
ADP + alpha1-adrenergic receptor phosphate
-
-
-
?
ATP + alpha1D-adrenergic receptor
ADP + alpha1D-adrenergic receptor phosphate
ATP + alpha2-adrenergic receptor
ADP + phospho-alpha2-adrenergic receptor
ATP + alpha2A-adrenergic receptor
ADP + phosphorylated alpha2A-adrenergic receptor
ATP + angiotensin receptor
ADP + phosphorylated angiotensin receptor
ATP + beta-adrenergic receptor
ADP + beta-adrenergic receptor phosphate
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
ATP + beta-casein
ADP + phosphorylated beta-casein
-
recombinant HA-tagged wild-type and mutant GRK3
-
-
?
ATP + beta-synuclein
ADP + phosphorylated beta-synuclein
-
-
-
-
?
ATP + beta1-adrenergic receptor
ADP + beta1-adrenergic receptor phosphate
-
-
-
?
ATP + beta2-adrenergic receptor
ADP + beta2-adrenergic receptor phosphate
ATP + beta2-adrenergic receptor
ADP + phosphorylated beta2-adrenergic receptor
ATP + calcium-sensing receptor
ADP + calcium-sensing receptor phosphate
ATP + corticotropin-releasing factor receptor type 1
ADP + phosphorylated corticotropin-releasing factor receptor type 1
ATP + DEKKEESEESDDDMG
ADP + DEKKEEpSEESDDDMG
-
-
-
-
?
ATP + DEMEFTEAESNMN
ADP + DEMEFpTEAESNMN
ATP + DEMEFTEAESNMNDLVSEYQ
ADP + DEMEFpTEAESNMNDLVSEYQ
-
-
-
-
?
ATP + dephospho-beta-tubulin
ADP + phosphorylated beta-tubulin
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
ATP + dopamine D3 receptor
ADP + phosphorylated dopamine D3 receptor
ATP + DREAM
ADP + phosphorylated DREAM
ATP + EAYEMPSEEGYQD
ADP + EAYEMPpSEEGYQD
-
-
-
-
?
ATP + EEMEFSEAEANMN
ADP + EEMEFpSEAEANMN
-
-
-
-
?
ATP + epidermal growth factor receptor
ADP + phosphorylated epidermal growth factor receptor
-
-
-
-
?
ATP + epithelial Na+ channel
ADP + phosphorylated epithelial Na+ channel
ATP + ezrin
ADP + phosphorylated ezrin
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
ATP + GEGMDEMEFTEAESNMN
ADP + GEGMDEMEFpTEAESNMN
-
-
-
-
?
ATP + GMEGLGTDITVI
ADP + GMEGLGpTDITVI
-
-
-
-
?
ATP + GPEPWETISEEMNM
ADP + GPEPWEpTISEEMNM
-
-
-
-
?
ATP + GRDKYKTLRQIRQG
ADP + GRDKYKpTLRQIRQG
-
-
-
-
?
ATP + histone deacetylase 6
ADP + phosphorylated histone deacetylase 6
-
phosphorylation at Ser-670
-
-
?
ATP + insulin receptor substrate 1
ADP + phosphorylated insulin receptor substrate 1
ATP + insulin receptor substrate-1
ADP + phosphorylated insulin receptor substrate-1
-
phosphorylation at Ser-307
-
-
?
ATP + insulin receptor substrate-1
ADP + phosphorylated-insulin receptor substrate-1
-
-
-
-
?
ATP + KKELQSLYRGFK
ADP + KKELQpSLYRGFK
-
-
-
-
?
ATP + LDTMESDSEVEAI
ADP + LDTMESDpSEVEAI
-
-
-
-
?
ATP + LEESSSSDHAERPPG
?
-
-
-
-
?
ATP + M1 muscarinic acetylcholine receptor
ADP + phosphorylated M1 muscarinic acetylcholine receptor
ATP + MEPEGESYEDPPQ
ADP + MEPEGEpSYEDPPQ
-
-
-
-
?
ATP + micro-opioid receptor
ADP + phosphorylated micro-opioid receptor
-
mutant C221V GRK2 shows slightly higher effect on morphine-induced internalization of the micro-opioid receptor compared to the wild-type GRK2, while the effects of mutants L271G, L273Y, and L336F are reduced, overview
-
-
?
ATP + MNDLVSEYQQYQ
ADP + MNDLVpSEYQQYQ
-
-
-
-
?
ATP + Mst2 protein
ADP + phosphorylated Mst2 protein
-
-
-
-
?
ATP + muscarinic acetylcholine receptor
ADP + phospho-muscarinic acetylcholine receptor
-
agonist-dependent phosphorylation, subtype 2
-
-
?
ATP + muscarinic cholinergic receptor
ADP + phospho-muscarinic cholinergic receptor
ATP + myelin basic protein
ADP + phosphorylated myelin basic protein
-
recombinant HA-tagged wild-type and mutant GRK3
-
-
?
ATP + Nedd4
ADP + phosphorylated Nedd4
ATP + Nedd4 protein
ADP + phosphorylated Nedd4 protein
-
-
-
-
?
ATP + Nedd4-2
ADP + phosphorylated Nedd4-2
ATP + Nedd4-2 protein
ADP + phosphorylated Nedd4-2 protein
-
-
-
-
?
ATP + p38 MAP kinase
ADP + phosphorylated p38 MAP kinase
ATP + p38 mitogen-activated protein kinase
ADP + phosphorylated p38 mitogen-activated protein kinase
-
-
-
-
?
ATP + PDEgamma
ADP + phosphorylated PDEgamma
ATP + PDGFRbeta
ADP + phosphorylated PDGFRbeta
-
-
-
-
?
ATP + peptide
ADP + phosphopeptide
ATP + PGWEERTHTDGRVF
ADP + PGWEERpTHTDGRVF
-
-
-
-
?
ATP + phosducin
ADP + phosphorylated phosducin
ATP + phosphodiesterase gamma
ADP + phosphorylated phosphodiesterase gamma
-
-
-
-
?
ATP + platelet-activating factor receptor
ADP + phospho-platelet-activating factor receptor
PAF receptor acts as substrate
-
-
?
ATP + platelet-derived growth factor receptor-beta
ADP + phosphorylated platelet-derived growth factor receptor-beta
ATP + platelet-derived growth factor receptor-beta protein
ADP + phosphorylated platelet-derived growth factor receptor
-
-
-
-
?
ATP + PPLDDYTHSIPEN
ADP + PPLDDYpTHSIPEN
-
-
-
-
?
ATP + PRAEAEDSFL
ADP + PRAEAEDpSFL
-
-
-
-
?
ATP + protein
ADP + phosphoprotein
ATP + protein M33
ADP + phosphorylated protein M33
ATP + R-smad
ADP + phosphorylated R-smad
-
GRK2
-
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
ATP + rhodopsin
ADP + phosphorylated rhodopsin
ATP + rhodopsin
ADP + rhodopsin phosphate
-
cf. EC 2.7.11.14, rhodopsin is also a substrate of GRK2
-
-
?
ATP + ribosomal protein P2
ADP + phosphorylated ribosomal protein P2
ATP + RRRAEAAASAAA
ADP + RRRAEAAApSAAA
-
-
-
-
?
ATP + RRRAEASAA
ADP + RRRAEApSAA
-
poor peptide substrate
-
-
?
ATP + RRRASAAASAA
?
-
poor peptide substrate
-
-
?
ATP + RRRASASAA
?
-
poor peptide substrate
-
-
?
ATP + RRRASpAAASAA
ADP + RRRASpAAASpAA
-
poor peptide substrate, higher catalytic efficiency than RRRASAAASAA
-
-
?
ATP + RRRASpASAA
?
-
poor peptide substrate
-
-
?
ATP + RRREEEEESAAA
ADP + RRREEEEEpSAAA
-
-
-
-
?
ATP + Smad2 protein
ADP + phosphorylated Smad2 protein
-
-
-
-
?
ATP + Smo
ADP + phosphorylated Smo
ATP + Smoothened protein
ADP + phopshorylated Smoothened
-
a seven-transmembrane signaling protein
-
-
?
ATP + Smoothened protein
ADP + phosphorylated Smoothened
-
GRK2 promotes smoothened signal transduction involved in regulation of cellular proliferation and differentiation through activation of the transcription factor Gli, overview
-
-
?
ATP + synuclein
ADP + phosphorylated synuclein
ATP + tubulin
ADP + phosphorylated tubulin
ATP + VKCQKLTDDHVQF
ADP + VKCQKLpTDDHVQF
-
-
-
-
?
ATP + VPSDNIDSQGRNC
ADP + VPSDNIDpSQGRNC
-
-
-
-
?
ATP + VSKTETSQVAPA
ADP + VSKTETpSQVAPA
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
ATP + [beta2-adrenergic receptor]
ADP + phospho-[beta2-adrenergic receptor]
-
-
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
ATP + [delta opioid receptor]
ADP + phospho-[delta opioid receptor]
-
-
-
-
?
ATP + [neurotensin receptor]
ADP + phospho-[neurotensin receptor]
-
the enzyme phosphorylates only the C-terminal serine residues
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
ezrin + ATP
phosphorylated ezrin + ADP
-
-
-
-
?
GTP + beta-adrenergic receptor
GDP + phospho-beta-adrenergic receptor
-
agonist-occupied form of beta-AR from hamster lung, GTP can substitute ATP, 2% as effective as ATP
-
?
histamine H2 receptor + ATP
phosphorylated histamine H2 receptor + ADP
-
-
-
-
?
moesin + ATP
phosphorylated moesin + ADP
-
-
-
-
?
radixin + ATP
phosphorylated radixin + ADP
-
-
-
-
?
tubulin + ATP
phosphorylated-tubulin + ADP
-
-
-
?
additional information
?
-
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + a protein
ADP + a phosphoprotein
-
the phosphorylase kinase phosphorylates proteins and proteolytic fragments thereof, phosphorylation of multiple residues in the substrate sequence
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
-
-
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
-
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 + alpha-synuclein
ADP + phosphorylated alpha-synuclein
-
phosphorylation at Ser129
-
-
?
ATP + alpha1 beta-adrenergic receptor
ADP + phosphorylated alpha1 beta-adrenergic receptor
-
-
-
?
ATP + alpha1 beta-adrenergic receptor
ADP + phosphorylated alpha1 beta-adrenergic receptor
substrate specificities of GRK2 and GRK3 in cardiac myocytes, overview
-
-
?
ATP + alpha1D-adrenergic receptor
ADP + alpha1D-adrenergic receptor phosphate
-
-
-
?
ATP + alpha1D-adrenergic receptor
ADP + alpha1D-adrenergic receptor phosphate
inhibition of vascular smooth muscle G protein-coupled receptor kinase 2 enhances alpha1D-adrenergic receptor constriction and signalling, overview
-
-
?
ATP + alpha2-adrenergic receptor
ADP + phospho-alpha2-adrenergic receptor
-
-
-
-
?
ATP + alpha2-adrenergic receptor
ADP + phospho-alpha2-adrenergic receptor
-
dependent on agonist occupancy by (-)-epinephrine, equally effective as beta-adrenergic receptor, incorporation of 7-8 mol phosphate/mol receptor
-
-
?
ATP + alpha2-adrenergic receptor
ADP + phospho-alpha2-adrenergic receptor
-
agonist-induced phosphorylation
-
-
?
ATP + alpha2-adrenergic receptor
ADP + phospho-alpha2-adrenergic receptor
-
from human platelets
-
-
?
ATP + alpha2A-adrenergic receptor
ADP + phosphorylated alpha2A-adrenergic receptor
-
-
-
-
?
ATP + alpha2A-adrenergic receptor
ADP + phosphorylated alpha2A-adrenergic receptor
-
interaction with GRK2 via the second and third intracellular loop of the receptor, determination of regions required for specific interaction and phosphorylation activity utilizing recombinant GST-tagged wild-type and several mutant alpha2A AR substrates, residues R225, R226, R218, K320, R322, and K358 are important, overview
-
-
?
ATP + angiotensin receptor
ADP + phosphorylated angiotensin receptor
-
-
-
-
?
ATP + angiotensin receptor
ADP + phosphorylated angiotensin receptor
-
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
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + beta-adrenergic receptor phosphate
-
the mechanism of myocardial beta-adrenergic receptor desensitization during cardiac surgery involves GRK2, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + beta-adrenergic receptor phosphate
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
phosphorylation sites
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
phosphorylation sites are located mainly at the C-terminal tail of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
incorporation of 7-8 mol phosphate/mol receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
incorporation of about 9 mol phosphate/mol receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
similar rates of beta-ARK 1 and 2 for beta2-adrenergic receptor phosphorylation
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
human beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
human beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
human beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
at a similar rate as muscarinic cholinergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
at a similar rate as alpha2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
substrates: wild-type and mutants of beta2-AR, synergistic action of beta-ARK and cAMP-dependent protein kinase depends on the palmitoylation state of the receptor, putative phosphorylation sites of beta2-AR
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
incorporation of up to 5 mol phosphate/mol receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
incorporation of up to 5 mol phosphate/mol receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-ARK 1, substrate specificity, the overall topological structure of the activated receptor plays a key role in regulating signal-dependent receptor phosphorylation
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-ARK 2 has a 25% lower specific activity than beta-ARK 1 towards rhodopsin and beta2-AR
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
incorporation of 6-8 mol phosphate/mol receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR from Sf9 cells
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR from hamster lung
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
beta-AR from hamster lung
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR from hamster lung
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR from hamster lung
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR from hamster lung
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR from hamster lung
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
beta-AR is a much better substrate than rhodopsin
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR is a much better substrate than rhodopsin
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR is a much better substrate than rhodopsin
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
natural substrate: beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
natural substrate: beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-ARK 1 and 2 may have a similar substrate specificity in vivo
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
regulation of the beta-AR function in vivo
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
plays, together with cAMP-dependent protein kinase, an important role in agonist-promoted receptor desensitization, coordinated regulatory mechanism involving sequential depalmitoylation and phosphorylation of the beta2-AR by the two kinases
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
human beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
human beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
incorporation of up to 5 mol phosphate/mol receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR from Sf9 cells
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-ARK 1: substrate recognition mechanism, consensus sequence required for substrates, 3-dimensional model structure of the catalytic domain, potential phosphorylation sites of human beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
presumably modulates some receptor-mediated immune functions
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
natural substrate: beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
functional role of the beta-ARK/beta-arrestin mechanism of receptor desensitization in immune cells
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
beta-ARK 1 might be involved in uncoupling and down-regulation of beta-AR, presumably both beta1- and beta2-AR, in failing hearts via receptor phosphorylation
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
phosphate is incorporated solely into Ser-residues
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-AR from hamster lung
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
role of beta-ARK 1 in heart failure, myocardial development and function
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
specifically phosphorylates the agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
beta-ARK 1 is more active than beta-ARK 2
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
beta-AR from hamster lung
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
general role in the desensitization of synaptic receptors
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates and inactivates beta-AR after stimulation by receptor agonists, facilitating the binding of the inhibitor protein beta-arrestin to the receptor, during myocardial ischemia the membrane activity of beta-ARK is increased
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
agonist-activated receptor substrate
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
G protein-coupled receptor kinase phosphorylation mediates beta-1 adrenergic receptor endocytosis via clathrin-coated pits
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
mouse wild-type receptor, cytosolic phosphorylation domain of the substrate, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
GRK3 and GRK2 are involved in down-regulation of the alpha2B-adrenoceptor, regulation of the pathway, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
in human heart failure, impaired beta-adrenergic receptor signaling compromises cardiac sensitivity to inotropic stimulation, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
phosphorylation by GRK2 preceeds the binding of arrestins, which inhibits the seven-transmembrane receptor, but initiates internalization, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
the enzyme is involved in regulation of the beta-adrenergic receptor signaling by inhibiting arrestin recruitment to the receptor and subsequent desensitization and internalization, regulation of GRK2 by S-nitrosylation, molecular mechanism, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
recombinantly expressed beta-adrenergic receptor in U2-OS cells, mapping of S-nitrosylation sites and regulatory locus in GRK2
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
betaARK1 is responsible for desensitization and down regulation of beta-adrenergic receptors
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
desensitization of the receptor by GRK2 and GRK3
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
the enzyme is involved in regulation of the beta-adrenergic receptor signaling by inhibiting arrestin recruitment to the receptor and subsequent desensitization and internalization, regulation of GRK2 by S-nitrosylation, molecular mechanism, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
mapping of S-nitrosylation sites and regulatory locus in GRK2
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
G-protein-coupled receptor kinase-2 and beta-arrestin-2 are involved in exercise-induced beta-adrenergic receptor trafficking from cytosol to membranes in adipocytes, role in beta-adrenergic receptor-ubiquitination in the ubiquitin-proteasome pathway
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
phosphorylation and internalization of the receptor requires clathrin, GRK2 specifically phosphorylates the activated form of the receptor that promotes the translocation of beta-arrestins to the plasma membrane, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
urea-treated rod outer segments as substrate
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
betaARK is involved in myocardial beta-adrenergic receptor signaling, enzyme dysfunction can cause heart failure, regulation mechanism and physiology, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
receptor desensitization by phosphorylation
-
-
?
ATP + beta2-adrenergic receptor
ADP + beta2-adrenergic receptor phosphate
-
-
-
-
?
ATP + beta2-adrenergic receptor
ADP + beta2-adrenergic receptor phosphate
-
role of GRK activity in the regulation of beta2 adrenergic signaling, feedback mechanism, overview
-
-
?
ATP + beta2-adrenergic receptor
ADP + phosphorylated beta2-adrenergic receptor
-
-
-
-
?
ATP + beta2-adrenergic receptor
ADP + phosphorylated beta2-adrenergic receptor
-
-
-
-
?
ATP + beta2-adrenergic receptor
ADP + phosphorylated beta2-adrenergic receptor
-
desensitization of the receptor with subsequent decline in the stimulatory effects of beta2-adrenergic agonists over time, the receptor is involved in alveolar Na+ and water clearance
-
-
?
ATP + calcium-sensing receptor
ADP + calcium-sensing receptor phosphate
GRK2
-
-
?
ATP + calcium-sensing receptor
ADP + calcium-sensing receptor phosphate
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 + corticotropin-releasing factor receptor type 1
ADP + phosphorylated corticotropin-releasing factor receptor type 1
-
-
-
-
?
ATP + corticotropin-releasing factor receptor type 1
ADP + phosphorylated corticotropin-releasing factor receptor type 1
-
i.e. CRFR1, phosphorylation leads to desensitization and downregulation of the receptor
-
-
?
ATP + corticotropin-releasing factor receptor type 1
ADP + phosphorylated corticotropin-releasing factor receptor type 1
-
-
-
-
?
ATP + corticotropin-releasing factor receptor type 1
ADP + phosphorylated corticotropin-releasing factor receptor type 1
-
i.e. CRFR1, phosphorylation leads to desensitization and downregulation of the receptor
-
-
?
ATP + DEMEFTEAESNMN
ADP + DEMEFpTEAESNMN
-
-
-
-
?
ATP + DEMEFTEAESNMN
ADP + DEMEFpTEAESNMN
-
best substrate
-
-
?
ATP + dephospho-beta-tubulin
ADP + phosphorylated beta-tubulin
-
-
-
-
?
ATP + dephospho-beta-tubulin
ADP + phosphorylated beta-tubulin
-
purified substrate from porcine brain or human GST-tagged protein recombinantly expressed in Escherichia coli, phosphorylation of betaI- and betaIII-tubulin at Thr409, Ser420, and, in betaIII-tubulin, also at Ser420 of the C-terminal outer surface of the substrate protein
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
phosphorylation by GRK2 has a regulatory role as part of the PI3K-PKC-GRK2 cascade
-
-
?
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
hyperserine phosphorylation by GRK2
-
-
?
ATP + dopamine D3 receptor
ADP + phosphorylated dopamine D3 receptor
-
-
-
-
?
ATP + dopamine D3 receptor
ADP + phosphorylated dopamine D3 receptor
-
the receptor is activated by GRK2 and GRK3 phosphorylation involving beta-arrestins, GRK-mediated regulation of receptor-filamin complex stability and receptor-G protein signaling potential, GRK2 reduces the dopamine D3 receptor signaling, overview
-
-
?
ATP + DREAM
ADP + phosphorylated DREAM
-
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 + DREAM
ADP + phosphorylated DREAM
-
i.e. downstream regulatory element antagonist modulator protein, GRK2 phosphorylates Ser95
-
-
?
ATP + epithelial Na+ channel
ADP + phosphorylated epithelial Na+ channel
-
-
-
-
?
ATP + epithelial Na+ channel
ADP + phosphorylated epithelial Na+ channel
-
channel inactivation
-
-
?
ATP + ezrin
ADP + phosphorylated ezrin
-
-
-
-
?
ATP + ezrin
ADP + phosphorylated ezrin
-
phosphorylation of ezrin affects the 7TM receptor mediated cytoskeletal reorganization
-
-
?
ATP + ezrin
ADP + phosphorylated ezrin
-
GRK2
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
-
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
desensitization by GRK2 of the ligand-activated receptor
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
desensitization of agonist-activated receptor
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
GRK2 performs desensitization of the ligand-activated receptor by phosphorylation
-
-
?
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 GRK2, 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
-
desensitization by GRK2 of the ligand-activated receptor
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
phosphorylation has a regulatory role, regulation of the signal transduction involving GRK2 and beta-arrestin, overview
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
regulation mechanism of GRK2, 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
-
regulation mechanism of GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview
-
-
?
ATP + insulin receptor substrate 1
ADP + phosphorylated insulin receptor substrate 1
-
role of GRK2 in insulin receptor IR signaling
-
-
?
ATP + insulin receptor substrate 1
ADP + phosphorylated insulin receptor substrate 1
-
phosphorylation at Ser307 by GRK2
-
-
?
ATP + M1 muscarinic acetylcholine receptor
ADP + phosphorylated M1 muscarinic acetylcholine receptor
-
-
-
-
?
ATP + M1 muscarinic acetylcholine receptor
ADP + phosphorylated M1 muscarinic acetylcholine receptor
-
phosphorylation-dependent and -independent mechanisms in the regulation of M1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 in hippocampal neurons, GRK2 can inhibit the receptor-dependent signaling via phospholipase C, overview
-
-
?
ATP + muscarinic cholinergic receptor
ADP + phospho-muscarinic cholinergic receptor
-
in vitro as good as beta-adrenergic receptor, phosphorylation depends on the presence of a muscarinic agonist ligand, not merely receptor occupancy, the agonist induces a conformational change, which allows phosphorylation, phosphorylation sites: 70% Ser- and 30% Thr-residues, incorporation of 3-4 mol phosphate/mol receptor
-
-
?
ATP + muscarinic cholinergic receptor
ADP + phospho-muscarinic cholinergic receptor
-
from chick heart
-
-
?
ATP + Nedd4
ADP + phosphorylated Nedd4
-
GRK2 interacts with and phosphorylates the ubiquitin protein ligase Nedd4 preventing the binding to proline-rich motifs present in the C-termini of epithelial Na+ channel subunits and inhibition of the channels, overview
-
-
?
ATP + Nedd4
ADP + phosphorylated Nedd4
-
recombinant GST-tagged wild-type Nedd-4, no activity with Nedd-4 mutant T466A, GRK2 interacts with and phosphorylates the ubiquitin protein ligase Nedd4 at multiple sites, mapping of phosphorylation sites, overview
-
-
?
ATP + Nedd4-2
ADP + phosphorylated Nedd4-2
-
GRK2 interacts with and phosphorylates the ubiquitin protein ligase Nedd4-2 preventing the binding to proline-rich motifs present in the C-termini of epithelial Na+ channel subunits and inhibition of the channels, overview
-
-
?
ATP + Nedd4-2
ADP + phosphorylated Nedd4-2
-
GRK2 interacts with and phosphorylates the ubiquitin protein ligase Nedd4-2 at multiple sites, mapping of phosphorylation sites, overview
-
-
?
ATP + p38 MAP kinase
ADP + phosphorylated p38 MAP kinase
-
GRK2 inactivates and regulates MAP kinase p38 modulating p38-dependent physiological processes, p38 and GRK2 are localized in a multimolecular complex
-
-
?
ATP + p38 MAP kinase
ADP + phosphorylated p38 MAP kinase
-
phosphorylation at Thr123 located in the docking groove
-
-
?
ATP + p38 MAP kinase
ADP + phosphorylated p38 MAP kinase
-
GRK2 inactivates and regulates MAP kinase p38 modulating p38-dependent physiological processes, p38 and GRK2 are localized in a multimolecular complex
-
-
?
ATP + p38 MAP kinase
ADP + phosphorylated p38 MAP kinase
-
phosphorylation at Thr123 located in the docking groove
-
-
?
ATP + PDEgamma
ADP + phosphorylated PDEgamma
-
-
-
-
?
ATP + PDEgamma
ADP + phosphorylated PDEgamma
-
phosphorylation of PDEgamma possibly stimulates EGFR-mediated ERK activation
-
-
?
ATP + peptide
ADP + phosphopeptide
-
beta-ARK 1 and 2 prefer peptide substrates with acidic amino acids N-terminal to a Ser-residue
-
-
?
ATP + peptide
ADP + phosphopeptide
-
beta-ARK 1 prefers peptides containing acidic residues on the N-terminal side of a serine or threonine, presence of activated receptor enhances peptide phosphorylation
-
-
?
ATP + peptide
ADP + phosphopeptide
-
e.g. Leu-Glu-Glu-Ser-Ser-Ser-Ser-Asp-His-Ala-Glu-Arg-Pro-Pro-Gly or Arg-Arg-Arg-Glu-Glu-Glu-Glu-Glu-Ser-Ala-Ala-Ala, role of acidic amino acids in peptide substrates, preference for negatively charged amino acids localized to the N-terminal side of a Ser- or Thr-residue, Ser-containing peptides are 4fold better than Thr-containing
-
-
?
ATP + peptide
ADP + phosphopeptide
-
synthetic
-
-
?
ATP + phosducin
ADP + phosphorylated phosducin
-
-
-
-
?
ATP + phosducin
ADP + phosphorylated phosducin
-
phosducin is activated to inhibit Gbetagamma protein
-
-
?
ATP + phosducin
ADP + phosphorylated phosducin
-
GRK2
-
-
?
ATP + platelet-derived growth factor receptor-beta
ADP + phosphorylated platelet-derived growth factor receptor-beta
-
feedback inhibition mechanism, overview
-
-
?
ATP + platelet-derived growth factor receptor-beta
ADP + phosphorylated platelet-derived growth factor receptor-beta
-
active with the wild-type and mutant Y740F/Y751F PDGFRbeta, GRK2 phosphorylation desensitizes the PDGF receptor-beta, feedback inhibition mechanism, overview
-
-
?
ATP + protein
ADP + phosphoprotein
specifically phosphorylates the agonist-occupied form of the beta-adrenergic and related G protein-coupled receptors
-
-
?
ATP + protein
ADP + phosphoprotein
specifically phosphorylates the agonist-occupied forms of the beta 2-adrenergic receptor and related G protein-coupled receptors
-
-
?
ATP + protein
ADP + phosphoprotein
the enzyme mediates agonist-dependent phosphorylation of the beta 2-adrenergic and related G protein-coupled receptors
-
-
?
ATP + protein M33
ADP + phosphorylated protein M33
-
GRK2 is a potent regulator of the mouse cytomegalovirus GPCR protein M33-induced Gq/11 signaling through its ability to phosphorylate M33 and sequester Galphaq/11 proteins dependent on an intact RH domain, the protein M33 is able to induce inositol phosphate accumulation, activate NF-kappaB, and promote smooth muscle cell migration, viral GPCRs like M33 play a role in viral dissemination in vivo, M33 is required for efficient murine cytomegalovirus replication in the mouse, and induces several signlaing pathways, overview
-
-
?
ATP + protein M33
ADP + phosphorylated protein M33
-
recombinant FLAG-tagged M33 expressed in HEK-293T cells
-
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
beta-ARK 2 has a 25% lower specific activity than beta-ARK 1 towards rhodopsin and beta2-AR
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
beta-AR is a much better substrate than rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
beta-AR is a much better substrate than rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
beta-AR is a much better substrate than rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
beta-AR is a much better substrate than rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
incorporation of 0.15 mol phosphate/mol rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
incorporation of 0.15 mol phosphate/mol rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
metarhodopsin II, poor substrate
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
recombinant beta-ARK 2: 40% of efficiency of beta-ARK 1 in phosphorylating rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
light-dependent, actual substrate: light-bleached rhodopsin
-
?
ATP + rhodopsin
ADP + phosphorhodopsin
-
in form of bovine rod outer segments
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
light-activated rhodopsin
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
dark-adapted and light-activated rhodopsin in urea-washed rod outer segment membranes
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
light-activated rhodopsin, both isozymes ARK1 and ARK2 prefer acidic amino acids N-terminal to a serine for phosphorylation
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
light-activated rhodopsin
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
substrate in dark-adapted, urea-stripped rod outer segment membranes
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
-
?
ATP + ribosomal protein P2
ADP + phosphorylated ribosomal protein P2
-
-
-
-
?
ATP + ribosomal protein P2
ADP + phosphorylated ribosomal protein P2
-
activation of P2
-
-
?
ATP + ribosomal protein P2
ADP + phosphorylated ribosomal protein P2
-
GRK2
-
-
?
ATP + RRREEEEESAAA
?
-
-
-
-
?
ATP + RRREEEEESAAA
?
-
nonreceptor peptide substrate
-
-
?
ATP + RRREEEEESAAA
?
-
good peptide substrate, but the activated receptor is a much better substrate
-
-
?
ATP + RRREEEEESAAA
?
-
-
-
-
?
ATP + Smo
ADP + phosphorylated Smo
-
-
-
?
ATP + Smo
ADP + phosphorylated Smo
GPRK2 participates in Hedgehog signaling in Drosophila melanogaster, and plays a key role in the Smo signal transduction pathway, when Gprk2 levels are lowered, Smo still accumulates at the cell membrane, but its activation is reduced, overview
-
-
?
ATP + synuclein
ADP + phosphorylated synuclein
-
-
-
-
?
ATP + synuclein
ADP + phosphorylated synuclein
-
GRK2
-
-
?
ATP + tubulin
ADP + phosphorylated tubulin
-
-
-
-
?
ATP + tubulin
ADP + phosphorylated tubulin
-
-
-
-
?
ATP + tubulin
ADP + phosphorylated tubulin
-
GRK2
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
-
-
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
-
recombinant FLAG-tagged beta2-adrenergic receptor stably expressed in HEK-293 cells
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
-
GRK2 and GRK3, receptor activation
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
-
GRK2 and GRK3
-
-
?
additional information
?
-
-
domain structure
-
-
?
additional information
?
-
-
domain structure
-
-
?
additional information
?
-
domain structure
-
-
?
additional information
?
-
-
beta-ARK interacts rapidly with a high affinity binding site present in salt-stripped rat liver microsomal membranes, modulation of binding of enzyme
-
-
?
additional information
?
-
-
mechanism and significance of the PH-domain function
-
-
?
additional information
?
-
-
phosphorylates G protein coupled receptors in an agonist-dependent manner
-
-
?
additional information
?
-
-
phosphorylates G protein coupled receptors in an agonist-dependent manner
-
-
?
additional information
?
-
-
role of the PH domain, ligand binding characteristics of the PH domain, distinct role for each ligand, i.e. betagamma subunits of G proteins and phosphatidylinositol 4,5-bisphosphate, in enzyme-mediated receptor phosphorylation
-
-
?
additional information
?
-
-
not: alpha1-adrenergic receptor
-
-
?
additional information
?
-
-
rhodopsin kinase, EC 2.7.11.14, is also capable of beta-adrenergic receptor phosphorylation
-
-
?
additional information
?
-
-
very poor substrates: casein, phosvitin
-
-
?
additional information
?
-
-
enzyme is important in mediating rapid agonist-specific desensitization
-
-
?
additional information
?
-
enzyme is important in mediating rapid agonist-specific desensitization
-
-
?
additional information
?
-
-
beta-ARK is probably a general adenylate cyclase-coupled receptor kinase
-
-
?
additional information
?
-
-
beta-ARK 1 is a key regulatory enzyme involved in the regulation of G protein-coupled receptors which associate with microsomal and plasma membranes
-
-
?
additional information
?
-
-
plays a pivotal role in phosphorylating and desensitizing G protein-coupled receptors by vitue of pleckstrin homology domain-mediated membrane translocation
-
-
?
additional information
?
-
-
beta-ARK activity is regulated by endogenous G proteins in different intracellular locations
-
-
?
additional information
?
-
-
phosphorylates and regulates receptors coupled to either stimulation or inhibition of adenylate cyclase
-
-
?
additional information
?
-
-
phosphorylates and regulates receptors coupled to either stimulation or inhibition of adenylate cyclase
-
-
?
additional information
?
-
-
dopamine D3 receptor binds to G proteins, the coupling is regulated by the filamin expression level
-
-
?
additional information
?
-
-
GRK2 is involved in A2 adenosine receptor response to agonists
-
-
?
additional information
?
-
-
GRK2 regulation mechanism of ERK activation involving interaction with mitogen-activated protein kinase, GRK2 diminishes the level of activating phosphorylation of ERK by CCL2 binding to chemokine receptor CCR2 in endothelial cells
-
-
?
additional information
?
-
-
phosphorylation of heptahelical receptors by GRK2 is a universal regulatory mehanism leading to desensitization of G protein signaling and to the activation of alternative signaling pathways
-
-
?
additional information
?
-
-
peptide phosphorylation study
-
-
?
additional information
?
-
-
the enzyme contains regulatory sites for Ca2+/calmodulin, protein kinase C, and clathrin
-
-
?
additional information
?
-
-
GRK2 regulates 7TM G-protein-coupled receptor activity, GRK2 promotes the association between active Smoothened and beta-arrestin 2, overview
-
-
?
additional information
?
-
-
carboxyl-terminus of GRK2 interacts with Hsp90. Reactive oxygen species (ROS)-mediated mitochrondrial localisation of GRK2 is dependent on Hsp90 binding
-
-
?
additional information
?
-
insulin-mediated dopamine D1 receptor desensitization and underlying molecular mechanism in opossum kidney cells, overview
-
-
?
additional information
?
-
Gprk2 is required for egg morphogenesis
-
-
?
additional information
?
-
-
GRK2 expression plays a role in the fly development, GRK2 expression is required in the germline for proper formation of the anterior egg structures, egg hatching, and for early and late embryogenesis
-
-
?
additional information
?
-
-
Gprk2, a Drosophila member of the G protein-coupled receptor kinases, plays a key role in the Smo, i.e. Smoothened, signal transduction pathway, overview. When Gprk2 levels are lowered, Smo still accumulates at the cell membrane, but its activation is reduced. Regulation of Gprk2 expression by Hh signaling in the wing disc, but Gprk2 is also required for Hh signaling in the wing disc, overview
-
-
?
additional information
?
-
Gprk2, a Drosophila member of the G protein-coupled receptor kinases, plays a key role in the Smo, i.e. Smoothened, signal transduction pathway, overview. When Gprk2 levels are lowered, Smo still accumulates at the cell membrane, but its activation is reduced. Regulation of Gprk2 expression by Hh signaling in the wing disc, but Gprk2 is also required for Hh signaling in the wing disc, overview
-
-
?
additional information
?
-
-
Gprk2 interacts with the Drosophila IkB homolog Cactus
-
-
?
additional information
?
-
-
domain structure
-
-
?
additional information
?
-
-
domain structure
-
-
?
additional information
?
-
-
beta-ARK 1 phosphorylates beta2-AR and other G protein-coupled receptors, substrate recognition mechanism, consensus sequence required for substrates, 3-dimensional model structure of the catalytic domain, residues 188-436
-
-
?
additional information
?
-
-
role for beta ARK in modulating some receptor-mediated immune functions
-
-
?
additional information
?
-
role for beta ARK in modulating some receptor-mediated immune functions
-
-
?
additional information
?
-
-
betaARK enhances the contractility in heart myocardium via inhibition of Gbetagamma subunits
-
-
?
additional information
?
-
-
betaARK1 inhibition improves beta-adrenergic signaling and contractile function in failing human myocytes
-
-
?
additional information
?
-
-
GRK2 and GRK3 are involved in methacholine-stimulated inositol 3-phosphate production
-
-
?
additional information
?
-
-
GRK2 mediates endothelin-1-induced insulin resistance via the inhibition of both Galphaq/11 and insulin receptor substrate-1 pathways in 3T3-L1 adipocytes, GRK2 does not affect insulin receptor tyrosine phosphorylation
-
-
?
additional information
?
-
-
GRKs are involved in diverse physiological processes and pathologies, overview
-
-
?
additional information
?
-
-
the enzyme is involved in G protein-coupled receptor signal transduction pathways and desensitization, GRK2 is a multiple domain kinase regulating by multiple mechanisms, overview
-
-
?
additional information
?
-
-
GRK2 functionally ineracts with clathrin, phosphoinositol 3-phosphate kinase-gamma, and G protein-coupled receptor kinase interacting protein, GIT
-
-
?
additional information
?
-
-
GRK2 interacts by direct binding with Galphaq/11, phosphorylation of agonist-activated seven-transmembrane receptors by GRK2
-
-
?
additional information
?
-
-
GRK2 interacts with calmodulin, substrate specificity, GRK2 phosphorylates serine and threonine residues with preceeding acidic amino acid residues
-
-
?
additional information
?
-
-
GRK2 prefers acidic protein sequences for phosphorylation
-
-
?
additional information
?
-
-
the M3 muscarinic acetylcholine receptor is no substrate for GRK2 and GRK3
-
-
?
additional information
?
-
-
GPCR-dependent kinases play a major role in agonist-induced phosphorylation and desensitization of G-protein coupled receptors, GRK2 is a component of neuronal and glial fibrillary tau deposits with no preference in tau isoform binding, GRK2 may play a role in hyperphosphorylation of tau in tauopathies
-
-
?
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, selective binding of activated Galphaq and Galpha-11 to RH domains of GRK2 and GRK3 selectively inhibits Gq signaling
-
-
?
additional information
?
-
-
GRK2 interacts with multiple signaling proteins and is involved in several cellular processes, e.g. expression and regulation of key cardiac seven-transmembrane receptors, 7TM receptors, such as the beta-adrenergic and angiotensin receptors, GRK2 interacts with NCS-1, mechanism, overview, GRK2 inhibition can ameliorate heart failure, molecular mechanism of GRK2 activity regulation, GRK2 is probably involved in regulation of hypertension, overview
-
-
?
additional information
?
-
-
GRK2 and tau do not crossreact
-
-
?
additional information
?
-
-
GRK2 binds to and inhibits Galphaq protein via its N-terminal RGS domain, GRK2 interacts with NCS-1
-
-
?
additional information
?
-
-
GRK2 interacts with a component of the MAPK pathway, as well as with the PI-3K substrate AKT, GRK2 and GRK3 bind the Gbetagamma subunit complex, a process that induces activation of the GRKs
-
-
?
additional information
?
-
-
GRK-mediated desensitization of beta2-adrenergic receptors is sufficient to cause declines in cAMP signals. GRK-mediated desensitization is primarily responsible for a sustained suppression of beta2AR signaling, overview
-
-
?
additional information
?
-
-
GRK2 also phosphorylates rhodopsin, cf. EC 2.7.11.14
-
-
?
additional information
?
-
-
GRK2 is also active with rhodopsin, cf. EC 2.7.11.14
-
-
?
additional information
?
-
-
substrate specificity, the enzyme depends on basic residues for substrate recognition, the residues at the substrate phosphorylation site greatly influence the enzyme activity, autoregulation by a pseudosubstrate mechanism, overview
-
-
?
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. Different mechanisms of signalling pathways modulation by GRK2, and regulation of GRK2, overview
-
-
?
additional information
?
-
-
GRK2 can also phosphorylate non-receptor substrates such as phosducins, synucleins, tubulin, ribosomal protein P2, ezrin, and receptor regulated Smads. The RH domain of GRK2 specifically interacts with Galphaq family members, although it does not stimulate the GTPase activity of Galphaq as efficiently as other classical RGS proteins do, interaction with other oroteins, detailed overview
-
-
?
additional information
?
-
-
domain structure
-
-
?
additional information
?
-
-
not: casein, histones
-
-
?
additional information
?
-
-
involved in the regulation of G protein-coupled receptor function, beta-ARK 1 appears to be the predominant GRK in early embryogenesis and plays a fundamental role in cardiac development, enzyme participates in intracellular signal transduction mechanisms, which regulate cardiogenesis
-
-
?
additional information
?
-
-
betaARK1 binds phosphoinositide 3-kinase, which is by this way targeted to agonist-stimulated beta-adrenergic receptors, where it regulates endocytosis, disruption of the betaARK1-PIK complex leads to restoration of beta-adrenergic receptor signaling and contractile function in heart failure, 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
?
-
-
GRK2 regulation mechanism of ERK activation involving interaction with mitogen-activated protein kinase, GRK2 diminishes the level of activating phosphorylation of ERK by CCL2 binding to chemokine receptor CCR2 in endothelial cells
-
-
?
additional information
?
-
-
GRKs are involved in diverse physiological processes and pathologies, overview
-
-
?
additional information
?
-
-
betaARK1 interacts with recombinant phosphoinositide 3-kinase expressed in transgenic mice
-
-
?
additional information
?
-
-
GRK2 functionally ineracts with clathrin, phosphoinositol 3-phosphate kinase-gamma, and G protein-coupled receptor kinase interacting protein, GIT
-
-
?
additional information
?
-
-
the GRKs are specific for GPCRs and arrestins, overview
-
-
?
additional information
?
-
-
adrenal GRK2 upregulation mediates sympathetic overdrive in heart failure, adrenal gland-specific GRK2 inhibition reverses alpha2 beta-adrenergic receptor dysregulation in heart failure, resulting in lowered plasma catecholamine levels, improved cardiac beta-adrenergic signaling and function, and increased sympatholytic efficacy of a alpha2 beta-adrenergic agonist
-
-
?
additional information
?
-
-
GRK2 is essential, and GRK2-deficient mice are embryonically lethal
-
-
?
additional information
?
-
-
GRK2 negatively regulates glycogen synthesis in mouse liver FL83B cells, regulates basal and insulin-stimulated glycogen synthesis via a post-IR signaling mechanism, and GRK2 may contribute to reduced IR expression and function during chronic insulin exposure
-
-
?
additional information
?
-
-
GRK2 plays a role in sodium transport regulation and is involved in the development of essential hypertension, 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
?
-
-
GRK2 in cardiac myocytes catalyzes phosphorylation and desensitization of different G protein-coupled receptors through specificity controlled by their carboxyl-terminal pleckstrin homology domain, overview
-
-
?
additional information
?
-
GRK2 is important for myocardial regulation, and is up-regulated in the dysfunctional heart
-
-
?
additional information
?
-
-
GRK3 in cardiac myocytes catalyzes phosphorylation and desensitization of different G protein-coupled receptors through specificity controlled by its carboxyl-terminal pleckstrin homology domain. GRK3 controls cardiac alpha1-adrenergic receptor responsiveness, distinct functions of GRK3 in regulation of cardiac contractility and growth, overview
-
-
?
additional information
?
-
no activity of GRK2 with alpha1-adrenergic receptor. GRK2 does not show class II histone deacetylase kinase activity or interaction with histone deacetylase kinases in vivo
-
-
?
additional information
?
-
-
GRK2 is essential, and GRK2-deficient mice are embryonically lethal
-
-
?
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
?
-
general role in the desensitization of synaptic receptors
-
-
?
additional information
?
-
general role in the desensitization of synaptic receptors
-
-
?
additional information
?
-
general function in desensitizing of many G protein-coupled receptor systems
-
-
?
additional information
?
-
general function in desensitizing of many G protein-coupled receptor systems
-
-
?
additional information
?
-
-
GRK3 is essential for induction of germinal vesicle breakdown, GRK3 forms a complex with beta-arrestin-2 causing G protein-coupled receptor desensitization
-
-
?
additional information
?
-
-
GRKs are involved in diverse physiological processes and pathologies, overview
-
-
?
additional information
?
-
-
GRK2 functionally ineracts with clathrin, phosphoinositol 3-phosphate kinase-gamma, and GIT
-
-
?
additional information
?
-
-
adrenal GRK2 upregulation mediates sympathetic overdrive in heart failure, adrenal gland-specific GRK2 inhibition reverses alpha2 beta-adrenergic receptor dysregulation in heart failure, resulting in lowered plasma catecholamine levels, improved cardiac beta-adrenergic signaling and function, and increased sympatholytic efficacy of a alpha2 beta-adrenergic agonist
-
-
?
additional information
?
-
-
GRK2 activity leads to translocation of parts of beta-adrenergic receptors to endocytic vesicles
-
-
?
additional information
?
-
GRK2 causes enhanced catecholamine secretion by desensitizing sympatho-inhibitory alpha2-adrenergic receptors of chromaffin cells and thereby aggravating heart failure
-
-
?
additional information
?
-
-
GRK2 substrate specificity in adult rat cardiac myocytes, overview. GRK2 completely lacks the capacity to attenuate phenylephrine-stimulated IP generation
-
-
?
additional information
?
-
GRK2 substrate specificity in adult rat cardiac myocytes, overview. GRK2 completely lacks the capacity to attenuate phenylephrine-stimulated IP generation
-
-
?
additional information
?
-
-
GRK3 substrate specificity in adult rat cardiac myocytes, overview
-
-
?
additional information
?
-
GRK3 substrate specificity in adult rat cardiac myocytes, overview
-
-
?
additional information
?
-
-
GRK2 substrate specificity, overview. GRK2 also shows activity with rhodopsin as substrate, cf. EC 2.7.11.14
-
-
?
additional information
?
-
GRK2 substrate specificity, overview. GRK2 also shows activity with rhodopsin as substrate, cf. EC 2.7.11.14
-
-
?
additional information
?
-
-
GRK3 substrate specificity, overview. GRK3 also shows activity with rhodopsin as substrate, cf. EC 2.7.11.14
-
-
?
additional information
?
-
GRK3 substrate specificity, overview. GRK3 also shows activity with rhodopsin as substrate, cf. EC 2.7.11.14
-
-
?
additional information
?
-
-
GRK2 interacts with Hsp90. Reactive oxygen species (ROS)-mediated mitochrondrial localisation of GRK2 is dependent on Hsp90 binding
-
-
?
additional information
?
-
-
RhoAGTP is a binding partner for enzyme GRK2
-
-
?
additional information
?
-
-
adenovirus-mediated overexpression of phosphoinositide 3-kinase restore contractile function of cardiac myocytes isolated from failing hearts, the recombinant PIK replaces the endogenous PIK in the transgenic pigs, the endogenous PIK shows abnormally increased activity in complex with betaARK1, overview
-
-
?
additional information
?
-
-
brain death induction, as well as sham-operation of pigs, lead to uncoupling of the beta-adrenergic receptor with acutely increased myocardial beta-adrenergic receptor kinase activity leading to left ventricular dysfunction
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
ATP + a protein
ADP + a phosphoprotein
-
-
-
-
?
ATP + alpha-synuclein
ADP + phosphorylated alpha-synuclein
-
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 + alpha1 beta-adrenergic receptor
ADP + phosphorylated alpha1 beta-adrenergic receptor
substrate specificities of GRK2 and GRK3 in cardiac myocytes, overview
-
-
?
ATP + alpha1-adrenergic receptor
ADP + alpha1-adrenergic receptor phosphate
-
-
-
?
ATP + alpha1D-adrenergic receptor
ADP + alpha1D-adrenergic receptor phosphate
inhibition of vascular smooth muscle G protein-coupled receptor kinase 2 enhances alpha1D-adrenergic receptor constriction and signalling, overview
-
-
?
ATP + alpha2A-adrenergic receptor
ADP + phosphorylated alpha2A-adrenergic receptor
-
-
-
-
?
ATP + angiotensin receptor
ADP + phosphorylated angiotensin receptor
-
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
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
ATP + beta1-adrenergic receptor
ADP + beta1-adrenergic receptor phosphate
-
-
-
?
ATP + beta2-adrenergic receptor
ADP + beta2-adrenergic receptor phosphate
-
role of GRK activity in the regulation of beta2 adrenergic signaling, feedback mechanism, overview
-
-
?
ATP + beta2-adrenergic receptor
ADP + phosphorylated beta2-adrenergic receptor
ATP + calcium-sensing receptor
ADP + calcium-sensing receptor phosphate
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 + corticotropin-releasing factor receptor type 1
ADP + phosphorylated corticotropin-releasing factor receptor type 1
ATP + dopamine D1 receptor
ADP + phosphorylated dopamine D1 receptor
phosphorylation by GRK2 has a regulatory role as part of the PI3K-PKC-GRK2 cascade
-
-
?
ATP + dopamine D3 receptor
ADP + phosphorylated dopamine D3 receptor
-
the receptor is activated by GRK2 and GRK3 phosphorylation involving beta-arrestins, GRK-mediated regulation of receptor-filamin complex stability and receptor-G protein signaling potential, GRK2 reduces the dopamine D3 receptor signaling, overview
-
-
?
ATP + DREAM
ADP + phosphorylated DREAM
-
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
-
channel inactivation
-
-
?
ATP + ezrin
ADP + phosphorylated ezrin
-
phosphorylation of ezrin affects the 7TM receptor mediated cytoskeletal reorganization
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
ATP + insulin receptor substrate 1
ADP + phosphorylated insulin receptor substrate 1
-
role of GRK2 in insulin receptor IR signaling
-
-
?
ATP + insulin receptor substrate-1
ADP + phosphorylated-insulin receptor substrate-1
-
-
-
-
?
ATP + M1 muscarinic acetylcholine receptor
ADP + phosphorylated M1 muscarinic acetylcholine receptor
-
phosphorylation-dependent and -independent mechanisms in the regulation of M1 muscarinic acetylcholine receptors by G protein-coupled receptor kinase 2 in hippocampal neurons, GRK2 can inhibit the receptor-dependent signaling via phospholipase C, overview
-
-
?
ATP + Nedd4
ADP + phosphorylated Nedd4
-
GRK2 interacts with and phosphorylates the ubiquitin protein ligase Nedd4 preventing the binding to proline-rich motifs present in the C-termini of epithelial Na+ channel subunits and inhibition of the channels, overview
-
-
?
ATP + Nedd4-2
ADP + phosphorylated Nedd4-2
-
GRK2 interacts with and phosphorylates the ubiquitin protein ligase Nedd4-2 preventing the binding to proline-rich motifs present in the C-termini of epithelial Na+ channel subunits and inhibition of the channels, overview
-
-
?
ATP + p38 MAP kinase
ADP + phosphorylated p38 MAP kinase
ATP + PDEgamma
ADP + phosphorylated PDEgamma
-
phosphorylation of PDEgamma possibly stimulates EGFR-mediated ERK activation
-
-
?
ATP + PDGFRbeta
ADP + phosphorylated PDGFRbeta
-
-
-
-
?
ATP + phosducin
ADP + phosphorylated phosducin
-
phosducin is activated to inhibit Gbetagamma protein
-
-
?
ATP + platelet-derived growth factor receptor-beta
ADP + phosphorylated platelet-derived growth factor receptor-beta
-
feedback inhibition mechanism, overview
-
-
?
ATP + protein
ADP + phosphoprotein
ATP + protein M33
ADP + phosphorylated protein M33
-
GRK2 is a potent regulator of the mouse cytomegalovirus GPCR protein M33-induced Gq/11 signaling through its ability to phosphorylate M33 and sequester Galphaq/11 proteins dependent on an intact RH domain, the protein M33 is able to induce inositol phosphate accumulation, activate NF-kappaB, and promote smooth muscle cell migration, viral GPCRs like M33 play a role in viral dissemination in vivo, M33 is required for efficient murine cytomegalovirus replication in the mouse, and induces several signlaing pathways, overview
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
ATP + ribosomal protein P2
ADP + phosphorylated ribosomal protein P2
-
activation of P2
-
-
?
ATP + Smo
ADP + phosphorylated Smo
GPRK2 participates in Hedgehog signaling in Drosophila melanogaster, and plays a key role in the Smo signal transduction pathway, when Gprk2 levels are lowered, Smo still accumulates at the cell membrane, but its activation is reduced, overview
-
-
?
ATP + Smoothened protein
ADP + phosphorylated Smoothened
-
GRK2 promotes smoothened signal transduction involved in regulation of cellular proliferation and differentiation through activation of the transcription factor Gli, overview
-
-
?
ATP + synuclein
ADP + phosphorylated synuclein
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
ATP + [beta2-adrenergic receptor]
ADP + phospho-[beta2-adrenergic receptor]
-
-
-
-
?
ATP + [beta2-adrenergic receptor]
ADP + [beta2-adrenergic receptor] phosphate
-
-
-
-
?
ATP + [delta opioid receptor]
ADP + phospho-[delta opioid receptor]
-
-
-
-
?
ATP + [neurotensin receptor]
ADP + phospho-[neurotensin receptor]
-
the enzyme phosphorylates only the C-terminal serine residues
-
-
?
ATP + [TSH receptor]
ADP + [TSH receptor]phosphate
-
GRK2 and GRK3, receptor activation
-
-
?
ezrin + ATP
phosphorylated ezrin + ADP
-
-
-
-
?
histamine H2 receptor + ATP
phosphorylated histamine H2 receptor + ADP
-
-
-
-
?
moesin + ATP
phosphorylated moesin + ADP
-
-
-
-
?
radixin + ATP
phosphorylated radixin + ADP
-
-
-
-
?
additional information
?
-
ATP + beta-adrenergic receptor
ADP + beta-adrenergic receptor phosphate
-
the mechanism of myocardial beta-adrenergic receptor desensitization during cardiac surgery involves GRK2, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + beta-adrenergic receptor phosphate
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
natural substrate: beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
natural substrate: beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
beta-ARK 1 and 2 may have a similar substrate specificity in vivo
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
regulation of the beta-AR function in vivo
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
plays, together with cAMP-dependent protein kinase, an important role in agonist-promoted receptor desensitization, coordinated regulatory mechanism involving sequential depalmitoylation and phosphorylation of the beta2-AR by the two kinases
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
presumably modulates some receptor-mediated immune functions
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
natural substrate: beta2-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
functional role of the beta-ARK/beta-arrestin mechanism of receptor desensitization in immune cells
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
beta-ARK 1 might be involved in uncoupling and down-regulation of beta-AR, presumably both beta1- and beta2-AR, in failing hearts via receptor phosphorylation
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
role of beta-ARK 1 in heart failure, myocardial development and function
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
general role in the desensitization of synaptic receptors
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
specifically phosphorylates and inactivates beta-AR after stimulation by receptor agonists, facilitating the binding of the inhibitor protein beta-arrestin to the receptor, during myocardial ischemia the membrane activity of beta-ARK is increased
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
agonist-occupied form of the receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
-
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phospho-beta-adrenergic receptor
involved in homologous desensitization of beta-adrenergic receptor
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
agonist-activated receptor substrate
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
G protein-coupled receptor kinase phosphorylation mediates beta-1 adrenergic receptor endocytosis via clathrin-coated pits
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
GRK3 and GRK2 are involved in down-regulation of the alpha2B-adrenoceptor, regulation of the pathway, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
in human heart failure, impaired beta-adrenergic receptor signaling compromises cardiac sensitivity to inotropic stimulation, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
phosphorylation by GRK2 preceeds the binding of arrestins, which inhibits the seven-transmembrane receptor, but initiates internalization, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
the enzyme is involved in regulation of the beta-adrenergic receptor signaling by inhibiting arrestin recruitment to the receptor and subsequent desensitization and internalization, regulation of GRK2 by S-nitrosylation, molecular mechanism, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
betaARK1 is responsible for desensitization and down regulation of beta-adrenergic receptors
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
desensitization of the receptor by GRK2 and GRK3
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
the enzyme is involved in regulation of the beta-adrenergic receptor signaling by inhibiting arrestin recruitment to the receptor and subsequent desensitization and internalization, regulation of GRK2 by S-nitrosylation, molecular mechanism, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
G-protein-coupled receptor kinase-2 and beta-arrestin-2 are involved in exercise-induced beta-adrenergic receptor trafficking from cytosol to membranes in adipocytes, role in beta-adrenergic receptor-ubiquitination in the ubiquitin-proteasome pathway
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
phosphorylation and internalization of the receptor requires clathrin, GRK2 specifically phosphorylates the activated form of the receptor that promotes the translocation of beta-arrestins to the plasma membrane, overview
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
-
-
-
?
ATP + beta-adrenergic receptor
ADP + phosphorylated beta-adrenergic receptor
-
betaARK is involved in myocardial beta-adrenergic receptor signaling, enzyme dysfunction can cause heart failure, regulation mechanism and physiology, overview
-
-
?
ATP + beta2-adrenergic receptor
ADP + phosphorylated beta2-adrenergic receptor
-
-
-
-
?
ATP + beta2-adrenergic receptor
ADP + phosphorylated beta2-adrenergic receptor
-
desensitization of the receptor with subsequent decline in the stimulatory effects of beta2-adrenergic agonists over time, the receptor is involved in alveolar Na+ and water clearance
-
-
?
ATP + corticotropin-releasing factor receptor type 1
ADP + phosphorylated corticotropin-releasing factor receptor type 1
-
i.e. CRFR1, phosphorylation leads to desensitization and downregulation of the receptor
-
-
?
ATP + corticotropin-releasing factor receptor type 1
ADP + phosphorylated corticotropin-releasing factor receptor type 1
-
i.e. CRFR1, phosphorylation leads to desensitization and downregulation of the receptor
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
desensitization by GRK2 of the ligand-activated receptor
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
desensitization of agonist-activated receptor
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
GRK2 performs desensitization of the ligand-activated receptor by phosphorylation
-
-
?
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 GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
desensitization by GRK2 of the ligand-activated receptor
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
phosphorylation has a regulatory role, regulation of the signal transduction involving GRK2 and beta-arrestin, overview
-
-
?
ATP + G protein-coupled receptor
ADP + phosphorylated G protein-coupled receptor
-
regulation mechanism of GRK2, 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
-
regulation mechanism of GRK2, overview, regulation by phosphorylation at specific sites via distinct specific kinases, overview
-
-
?
ATP + p38 MAP kinase
ADP + phosphorylated p38 MAP kinase
-
GRK2 inactivates and regulates MAP kinase p38 modulating p38-dependent physiological processes, p38 and GRK2 are localized in a multimolecular complex
-
-
?
ATP + p38 MAP kinase
ADP + phosphorylated p38 MAP kinase
-
GRK2 inactivates and regulates MAP kinase p38 modulating p38-dependent physiological processes, p38 and GRK2 are localized in a multimolecular complex
-
-
?
ATP + protein
ADP + phosphoprotein
specifically phosphorylates the agonist-occupied form of the beta-adrenergic and related G protein-coupled receptors
-
-
?
ATP + protein
ADP + phosphoprotein
specifically phosphorylates the agonist-occupied forms of the beta 2-adrenergic receptor and related G protein-coupled receptors
-
-
?
ATP + protein
ADP + phosphoprotein
the enzyme mediates agonist-dependent phosphorylation of the beta 2-adrenergic and related G protein-coupled receptors
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
light-activated rhodopsin
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
-
-
?
ATP + rhodopsin
ADP + phosphorylated rhodopsin
-
light-activated rhodopsin
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
ATP + [beta-adrenergic receptor]
ADP + phospho-[beta-adrenergic receptor]
-
-
-
-
?
additional information
?
-
-
enzyme is important in mediating rapid agonist-specific desensitization
-
-
?
additional information
?
-
enzyme is important in mediating rapid agonist-specific desensitization
-
-
?
additional information
?
-
-
beta-ARK is probably a general adenylate cyclase-coupled receptor kinase
-
-
?
additional information
?
-
-
beta-ARK 1 is a key regulatory enzyme involved in the regulation of G protein-coupled receptors which associate with microsomal and plasma membranes
-
-
?
additional information
?
-
-
plays a pivotal role in phosphorylating and desensitizing G protein-coupled receptors by vitue of pleckstrin homology domain-mediated membrane translocation
-
-
?
additional information
?
-
-
beta-ARK activity is regulated by endogenous G proteins in different intracellular locations
-
-
?
additional information
?
-
-
phosphorylates and regulates receptors coupled to either stimulation or inhibition of adenylate cyclase
-
-
?
additional information
?
-
-
phosphorylates and regulates receptors coupled to either stimulation or inhibition of adenylate cyclase
-
-
?
additional information
?
-
-
dopamine D3 receptor binds to G proteins, the coupling is regulated by the filamin expression level
-
-
?
additional information
?
-
-
GRK2 is involved in A2 adenosine receptor response to agonists
-
-
?
additional information
?
-
-
GRK2 regulation mechanism of ERK activation involving interaction with mitogen-activated protein kinase, GRK2 diminishes the level of activating phosphorylation of ERK by CCL2 binding to chemokine receptor CCR2 in endothelial cells
-
-
?
additional information
?
-
-
phosphorylation of heptahelical receptors by GRK2 is a universal regulatory mehanism leading to desensitization of G protein signaling and to the activation of alternative signaling pathways
-
-
?
additional information
?
-
-
GRK2 regulates 7TM G-protein-coupled receptor activity, GRK2 promotes the association between active Smoothened and beta-arrestin 2, overview
-
-
?
additional information
?
-
-
carboxyl-terminus of GRK2 interacts with Hsp90. Reactive oxygen species (ROS)-mediated mitochrondrial localisation of GRK2 is dependent on Hsp90 binding
-
-
?
additional information
?
-
insulin-mediated dopamine D1 receptor desensitization and underlying molecular mechanism in opossum kidney cells, overview
-
-
?
additional information
?
-
Gprk2 is required for egg morphogenesis
-
-
?
additional information
?
-
-
GRK2 expression plays a role in the fly development, GRK2 expression is required in the germline for proper formation of the anterior egg structures, egg hatching, and for early and late embryogenesis
-
-
?
additional information
?
-
-
Gprk2, a Drosophila member of the G protein-coupled receptor kinases, plays a key role in the Smo, i.e. Smoothened, signal transduction pathway, overview. When Gprk2 levels are lowered, Smo still accumulates at the cell membrane, but its activation is reduced. Regulation of Gprk2 expression by Hh signaling in the wing disc, but Gprk2 is also required for Hh signaling in the wing disc, overview
-
-
?
additional information
?
-
Gprk2, a Drosophila member of the G protein-coupled receptor kinases, plays a key role in the Smo, i.e. Smoothened, signal transduction pathway, overview. When Gprk2 levels are lowered, Smo still accumulates at the cell membrane, but its activation is reduced. Regulation of Gprk2 expression by Hh signaling in the wing disc, but Gprk2 is also required for Hh signaling in the wing disc, overview
-
-
?
additional information
?
-
-
Gprk2 interacts with the Drosophila IkB homolog Cactus
-
-
?
additional information
?
-
-
role for beta ARK in modulating some receptor-mediated immune functions
-
-
?
additional information
?
-
role for beta ARK in modulating some receptor-mediated immune functions
-
-
?
additional information
?
-
-
betaARK enhances the contractility in heart myocardium via inhibition of Gbetagamma subunits
-
-
?
additional information
?
-
-
betaARK1 inhibition improves beta-adrenergic signaling and contractile function in failing human myocytes
-
-
?
additional information
?
-
-
GRK2 and GRK3 are involved in methacholine-stimulated inositol 3-phosphate production
-
-
?
additional information
?
-
-
GRK2 mediates endothelin-1-induced insulin resistance via the inhibition of both Galphaq/11 and insulin receptor substrate-1 pathways in 3T3-L1 adipocytes, GRK2 does not affect insulin receptor tyrosine phosphorylation
-
-
?
additional information
?
-
-
GRKs are involved in diverse physiological processes and pathologies, overview
-
-
?
additional information
?
-
-
the enzyme is involved in G protein-coupled receptor signal transduction pathways and desensitization, GRK2 is a multiple domain kinase regulating by multiple mechanisms, overview
-
-
?
additional information
?
-
-
GPCR-dependent kinases play a major role in agonist-induced phosphorylation and desensitization of G-protein coupled receptors, GRK2 is a component of neuronal and glial fibrillary tau deposits with no preference in tau isoform binding, GRK2 may play a role in hyperphosphorylation of tau in tauopathies
-
-
?
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, selective binding of activated Galphaq and Galpha-11 to RH domains of GRK2 and GRK3 selectively inhibits Gq signaling
-
-
?
additional information
?
-
-
GRK2 interacts with multiple signaling proteins and is involved in several cellular processes, e.g. expression and regulation of key cardiac seven-transmembrane receptors, 7TM receptors, such as the beta-adrenergic and angiotensin receptors, GRK2 interacts with NCS-1, mechanism, overview, GRK2 inhibition can ameliorate heart failure, molecular mechanism of GRK2 activity regulation, GRK2 is probably involved in regulation of hypertension, overview
-
-
?
additional information
?
-
-
GRK-mediated desensitization of beta2-adrenergic receptors is sufficient to cause declines in cAMP signals. GRK-mediated desensitization is primarily responsible for a sustained suppression of beta2AR signaling, overview
-
-
?
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. Different mechanisms of signalling pathways modulation by GRK2, and regulation of GRK2, overview
-
-
?
additional information
?
-
-
involved in the regulation of G protein-coupled receptor function, beta-ARK 1 appears to be the predominant GRK in early embryogenesis and plays a fundamental role in cardiac development, enzyme participates in intracellular signal transduction mechanisms, which regulate cardiogenesis
-
-
?
additional information
?
-
-
betaARK1 binds phosphoinositide 3-kinase, which is by this way targeted to agonist-stimulated beta-adrenergic receptors, where it regulates endocytosis, disruption of the betaARK1-PIK complex leads to restoration of beta-adrenergic receptor signaling and contractile function in heart failure, 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
?
-
-
GRK2 regulation mechanism of ERK activation involving interaction with mitogen-activated protein kinase, GRK2 diminishes the level of activating phosphorylation of ERK by CCL2 binding to chemokine receptor CCR2 in endothelial cells
-
-
?
additional information
?
-
-
GRKs are involved in diverse physiological processes and pathologies, overview
-
-
?
additional information
?
-
-
adrenal GRK2 upregulation mediates sympathetic overdrive in heart failure, adrenal gland-specific GRK2 inhibition reverses alpha2 beta-adrenergic receptor dysregulation in heart failure, resulting in lowered plasma catecholamine levels, improved cardiac beta-adrenergic signaling and function, and increased sympatholytic efficacy of a alpha2 beta-adrenergic agonist
-
-
?
additional information
?
-
-
GRK2 is essential, and GRK2-deficient mice are embryonically lethal
-
-
?
additional information
?
-
-
GRK2 negatively regulates glycogen synthesis in mouse liver FL83B cells, regulates basal and insulin-stimulated glycogen synthesis via a post-IR signaling mechanism, and GRK2 may contribute to reduced IR expression and function during chronic insulin exposure
-
-
?
additional information
?
-
-
GRK2 plays a role in sodium transport regulation and is involved in the development of essential hypertension, 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
?
-
-
GRK2 in cardiac myocytes catalyzes phosphorylation and desensitization of different G protein-coupled receptors through specificity controlled by their carboxyl-terminal pleckstrin homology domain, overview
-
-
?
additional information
?
-
GRK2 is important for myocardial regulation, and is up-regulated in the dysfunctional heart
-
-
?
additional information
?
-
-
GRK3 in cardiac myocytes catalyzes phosphorylation and desensitization of different G protein-coupled receptors through specificity controlled by its carboxyl-terminal pleckstrin homology domain. GRK3 controls cardiac alpha1-adrenergic receptor responsiveness, distinct functions of GRK3 in regulation of cardiac contractility and growth, overview
-
-
?
additional information
?
-
-
GRK2 is essential, and GRK2-deficient mice are embryonically lethal
-
-
?
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
?
-
general role in the desensitization of synaptic receptors
-
-
?
additional information
?
-
general role in the desensitization of synaptic receptors
-
-
?
additional information
?
-
general function in desensitizing of many G protein-coupled receptor systems
-
-
?
additional information
?
-
general function in desensitizing of many G protein-coupled receptor systems
-
-
?
additional information
?
-
-
GRK3 is essential for induction of germinal vesicle breakdown, GRK3 forms a complex with beta-arrestin-2 causing G protein-coupled receptor desensitization
-
-
?
additional information
?
-
-
GRKs are involved in diverse physiological processes and pathologies, overview
-
-
?
additional information
?
-
-
adrenal GRK2 upregulation mediates sympathetic overdrive in heart failure, adrenal gland-specific GRK2 inhibition reverses alpha2 beta-adrenergic receptor dysregulation in heart failure, resulting in lowered plasma catecholamine levels, improved cardiac beta-adrenergic signaling and function, and increased sympatholytic efficacy of a alpha2 beta-adrenergic agonist
-
-
?
additional information
?
-
-
GRK2 activity leads to translocation of parts of beta-adrenergic receptors to endocytic vesicles
-
-
?
additional information
?
-
GRK2 causes enhanced catecholamine secretion by desensitizing sympatho-inhibitory alpha2-adrenergic receptors of chromaffin cells and thereby aggravating heart failure
-
-
?
additional information
?
-
-
GRK2 substrate specificity in adult rat cardiac myocytes, overview. GRK2 completely lacks the capacity to attenuate phenylephrine-stimulated IP generation
-
-
?
additional information
?
-
GRK2 substrate specificity in adult rat cardiac myocytes, overview. GRK2 completely lacks the capacity to attenuate phenylephrine-stimulated IP generation
-
-
?
additional information
?
-
-
GRK3 substrate specificity in adult rat cardiac myocytes, overview
-
-
?
additional information
?
-
GRK3 substrate specificity in adult rat cardiac myocytes, overview
-
-
?
additional information
?
-
-
GRK2 interacts with Hsp90. Reactive oxygen species (ROS)-mediated mitochrondrial localisation of GRK2 is dependent on Hsp90 binding
-
-
?
additional information
?
-
-
RhoAGTP is a binding partner for enzyme GRK2
-
-
?
additional information
?
-
-
adenovirus-mediated overexpression of phosphoinositide 3-kinase restore contractile function of cardiac myocytes isolated from failing hearts, the recombinant PIK replaces the endogenous PIK in the transgenic pigs, the endogenous PIK shows abnormally increased activity in complex with betaARK1, overview
-
-
?
additional information
?
-
-
brain death induction, as well as sham-operation of pigs, lead to uncoupling of the beta-adrenergic receptor with acutely increased myocardial beta-adrenergic receptor kinase activity leading to left ventricular dysfunction
-
-
?
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
(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-(3-((2,6-bis(trifluoromethyl)benzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-((2,6-dichlorobenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-((2,6-difluorobenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-((2,6-dimethoxybenzyl)carbamoyl)-4-fluorophenyl)-N-(1Hindazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-((2,6-dimethylbenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5 carboxamide
-
4-(3-((2,6-dimethylbenzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-N,6-dimethyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-((2,6-dimethylphenethyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-((3,5-bis(trifluoromethyl)benzyl)carbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-(2-((2,6-bis(trifluoromethyl)benzyl)amino)-2-oxoethyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-(2-((2,6-dimethoxybenzyl)amino)-2-oxoethyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-(2-((2,6-dimethylbenzyl)amino)-2-oxoethyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(3-(benzylcarbamoyl)-4-fluorophenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-(((3-methylpyridin-2-yl)methyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-((2-(pyridin-2-yl)ethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-((2-(pyridin-4-yl)ethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-((2-methoxybenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-((3-fluorobenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-((3-methoxybenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-((4-methoxybenzyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-((isoquinolin-1-ylmethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-((pyridin-2-ylmethyl)carbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
4-(4-fluoro-3-(methylcarbamoyl)phenyl)-N-(1H-indazol-5-yl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
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
-
4-amino-1-tert-butyl-3-(1'-naphthyl)pyrrazolo[3,4-d]pyrimidine
-
i.e. 1-Na-PP1, inhibits mutant C221V mediated morphine-induced internalization of the micro-opioid receptor, but not wild-type GRK2 and mutant L271G activities
5-(4-fluorophenyl)-N-[[(3S,5R,8aR)-hexahydro-1H-pyrrolo[2,1-c][1,4]oxazin-3-yl]methyl]-5-oxopentanamide
-
5-(5-((1H-indazol-5-yl)carbamoyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidin-4-yl)-2-fluorobenzoic acid
-
5-fluoro-N-(imidazo[1,2-a]pyridin-2-ylmethyl)-2-methoxybenzamide
-
alpha2-adrenergic antagonist
-
co-incubation completely blocks phosphorylation of alpha2-adrenergic receptor
-
Alprenolol
-
beta-adrenergic antagonist, blocks phosphorylation
atropine
-
receptor antagonist
beta adrenergic receptor kinase C-terminal peptide
-
-
-
Chloropromazine
-
IC50: 0.043 mM
chondroitin sulfate B
-
weak
chondroitin sulfate C
-
less inhibitory than heparin
concanavalin A
-
inhibitor of clathrin-mediated receptor endocytosis via clathrin binding domain of beta-arrestin-2, inhibitor reduces the GRK3/beta-arrestin-2 induction activity of germinal vesicle breakdown
-
corticotropin-releasing factor
-
reduces GRK2 expression in pituitary cells, suppressed by astressin, opposite effect compared to corticotroph tumor cells AtT20
-
D-glucosamine 2,6-disulfate
-
inhibits in the millimolar range, weak, IC50: 7.3 mM with rhodopsin as substrate
D-sphingosine
-
IC50: 0.027 mM
Dextran sulfate
-
strong, IC50: 0.00015 mM with rhodopsin as substrate
-
heparan sulfate
-
less inhibitory than heparin
Inositol hexaphosphate
-
weak, IC50: 3.6 mM with rhodopsin as substrate
McN-A343
-
weak, partial antagonist
monodansyl cadaverin
-
inhibitor of clathrin-mediated receptor endocytosis via clathrin binding domain of beta-arrestin-2, inhibitor reduces the GRK3/beta-arrestin-2 induction activity of germinal vesicle breakdown
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-(benzo[d][1,3]dioxol-5-yl)-4-(4-fluoro-3-((pyridin-2-ylmethyl)-carbamoyl)phenyl)-6-methyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxamide
-
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
-
NaF
-
as efficient as Cl-, I-, NO2- or acetate, less efficient than citrate, phosphate or sulfate
NaI
-
as efficient as Cl-, F-, NO2- or acetate, less efficient than citrate, phosphate or sulfate
NaNO2
-
as efficient as Cl-, I-, F- or acetate, less efficient than citrate, phosphate or sulfate
phosphatidylinositol 4,5-bisphosphate
-
inhibits receptor phosphorylation, causes membrane association, 30% inhibition of phosphorylation of RRREEEEESAAA
propranolol
-
beta-adrenergic antagonist, in presence no phosphorylation
Protein kinase C inhibitor H7
-
quinpirole
-
inhibits GRK2 and GRK3
Raf kinase inhibitor protein
-
RKIP
-
rhodopsin
-
intact light-activated rhodopsin slightly inhibits phosphorylation of RRREEEEESAAA
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
-
Sangivamycin
-
IC50: 0.067 mM
Sodium acetate
-
as efficient as Cl-, I-, NO2- or F-, less efficient than citrate, phosphate or sulfate
Sodium citrate
-
20 mM, 97% inhibition, more efficient than phosphate, sulfate, Cl-, F-, I-, NO2- or acetate
Sodium phosphate
-
20 mM, 76% inhibition, less efficient than citrate, as good as sulfate, more efficient than Cl-, F-, I-, NO2- or acetate
Sodium sulfate
-
less efficient than citrate, as good as phosphate, more efficient than Cl-, F-, I-, NO2- or acetate
spermidine
-
weak, less potent than polylysine
tamoxifen
-
IC50: 0.04 mM
Trifluoperazine
-
IC50: 0.035 mM
Triton X-100
-
IC50: 0.054 mM
Tween 20
-
IC50: 0.027 mM
Yohimbine
-
alpha2-adrenergic antagonist, co-incubation completely blocks phosphorylation of alpha2-adrenergic receptor
Zn2+
-
0.1-0.2 mM ZnCl2, 94-98% inhibition
2,3-diphosphoglycerate
-
weak
2,3-diphosphoglycerate
-
inhibits in the millimolar range, IC50: 1.1 mM with rhodopsin as substrate; weak
actinin
-
inhibits GRK2
-
actinin
-
inhibits GRK2
-
actinin
-
inhibits GRK2
-
balanol
-
betaARKct
-
the isolated C-terminal sequence of the enzyme acts as a peptide inhibitor
-
betaARKct
a GRK2 inhibitor
-
betaARKct
-
injection of betaARKct is associated with decreased levels of betaARK1 at 7, 14, and 21 days
-
C-terminus of beta-ARK
-
betaARKmini, inhibits
-
C-terminus of beta-ARK
-
betaARKmini, inhibits
-
Ca2+/calmodulin
-
-
-
Ca2+/calmodulin
-
inhibit GRK2 with an IC50 of about 0.002 mM, inhibition mechanism via direct binding
-
Calmodulin
-
inhibits GRK2
Calmodulin
-
inhibits GRK2
Calmodulin
-
inhibits GRK2
caveolin
-
microsomal anchor protein, inhibits GRK2
-
caveolin
-
microsomal anchor protein, inhibits GRK2
-
caveolin
-
microsomal anchor protein, inhibits GRK2
-
CCG-224406
-
CCG224406
-
-
CMPD101
-
specific inhibitor, i.e. 3-[(4-methyl-5-pyridin-4-yl-1,2,4-triazol-3-yl)methylamino]-N-[[2-(trifluoromethyl)phenyl]methyl]benzamide hydrochloride
-
Digitonin
-
IC50: 0.05 mM
Digitonin
-
0.05-0.1%, 93-95% inhibition
GRK2ct
C-terminal portion of GRK2
-
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
-
most potent inhibitor to date
heparin
-
de-N-sulfated heparin is 8fold less effective; most potent inhibitor to date; polylysine, spermine or spermidine at lower concentrations partially reverses; strong, kinetics, IC50: 0.00003 mM with beta-AR as substrate, 0.00015 mM with rhodopsin as substrate
heparin
-
0.001 mM, complete inhibition of muscarinic cholinergic receptor phosphorylation
heparin
-
beta-ARK 1: IC50 is 0.0014 mM, beta-ARK 2: IC50 is 0.0011 mM; inhibits both isozymes ARK1 and ARK2 potently with IC50 of 0.0014 mM and 0.0011 mM, respectively; most potent inhibitor to date
heparin
-
potent inhibitor of beta-ARK 1
heparin
rhodopsin phosphorylation, in a dose-dependent manner
heparin
-
specific inhibitor, 1 mM/l: almost complete inhibition of rhodopsin phosphorylation
Inositol hexasulfate
-
good inhibitor; IC50: 0.0135 mM with rhodopsin as substrate
Inositol hexasulfate
-
270fold more potent than inositol hexaphosphate; IC50: 0.0135 mM with rhodopsin as substrate
NaCl
-
0.1 M, 90% inhibition
NaCl
-
20 mM, 48% inhibition, as efficient as F-, I-, NO2- or acetate, less efficient than citrate, phosphate or sulfate
nitric oxide
-
inhibits GRK2 by S-nitrosylation at Cys340, regulatory function of S-nitrosylation
nitric oxide
-
inhibits GRK2 by S-nitrosylation at Cys340, regulatory function of S-nitrosylation
paroxetine
-
paroxetine
modest inhibitory activity
paroxetine
selective inhibitor
peptide
-
synthetic peptides from a variety of intracellular regions of beta2-AR specifically inhibit phosphorylation of the intact receptor, but not of peptide substrates
peptide
-
synthetic peptides derived from the receptor intracellular loop inhibit
Polyaspartic acid
-
good inhibitor; IC50: 0.0013 mM with rhodopsin as substrate
Polyaspartic acid
-
IC50: 0.0013 mM with rhodopsin as substrate
Polyglutamic acid
-
good inhibitor
Polyglutamic acid
-
IC50: 0.002 mM with rhodopsin as substrate
polylysine
-
IC50: 0.069 mM with rhodopsin as substrate
polylysine
-
IC50: 0.069 mM with rhodopsin as substrate; weak, more potent than spermine and spermidine
Protein kinase C inhibitor H7
-
IC50: 0.25 mM; weak
-
Protein kinase C inhibitor H7
-
weak
-
Protein kinase C inhibitor H7
weak
-
pyridoxal 5'-phosphate
-
weak, IC50: 0.9 mM with rhodopsin as substrate
pyridoxal 5'-phosphate
-
inhibits in the millimolar range; weak, IC50: 0.9 mM with rhodopsin as substrate
S-nitrosothiols
-
inhibit GRK2 by S-nitrosylation at Cys340, regulatory function of S-nitrosylation
-
S-nitrosothiols
-
inhibit GRK2 by S-nitrosylation at Cys340, regulatory function of S-nitrosylation
-
spermine
-
IC50: 1.6 mM; weak, less potent than polylysine
spermine
-
weak, less potent than polylysine
additional information
-
-
-
additional information
-
alprenolol is no inhibitor with alpha2-adrenergic receptor as substrate
-
additional information
-
not affected by Ca2+ or Co2+
-
additional information
-
marked inhibition of rhodopsin or synthetic peptide phosphorylation in the presence of increasing amounts of microsomal membranes, bound enzyme is less able to interact with its substrate
-
additional information
-
platelet-derived growth factor receptor-beta activates the enzyme by tyrosine phosphorylation, the wild-type PDGFRbeta is 60fold more active with GRK2 than PDGFRbeta mutant Y857F, GRK2 activation also increases GRK2 degradation and downregulation
-
additional information
-
not inhibited by protein kinase A inhibitor PKI; not inhibited by staurosporine
-
additional information
not inhibited by protein kinase A inhibitor PKI; not inhibited by staurosporine
-
additional information
-
phosphorylation by ERK1/2 inhibits GRK2
-
additional information
-
clathrin inhibitors inhibit the internalization of the beta-adrenergic receptor by GRK
-
additional information
-
deletion mutants of the enzyme, comprising parts of the C-terminus or the N-terminus, are able to inhibit the full-length wild-type enzyme, overview
-
additional information
-
quantitative determination of S-nitrosylation of GRK2 by the biotin-switch assay
-
additional information
-
ERK phosphorylates and inhibits GRK2, protein kinase C phosphorylated GRK2 at Ser685 and induces RKIP binding, RKIP binds to GRK2 and inhibits it after it has been phosphorylated by protein kinase C
-
additional information
-
S-nitrosylation at Cys-340 inhibits isoform GRK2 activity
-
additional information
-
autoregulation by a pseudosubstrate mechanism, overview
-
additional information
-
not inhibited by cAMP, cGMP, cAMP-dependent protein kinase inhibitor, Ca2+/calmodulin, Ca2+/phospholipid, phorbol esters
-
additional information
-
phosphorylation by ERK1/2 inhibits GRK2
-
additional information
-
isolated pleckstrin homology domains of GRK2 and GRK3 can act as enzyme inhibitors preventing interaction of the enzymes with the G protein subunits
-
additional information
-
quantitative determination of S-nitrosylation of GRK2 by the biotin-switch assay
-
additional information
-
not inhibited by staurosporine
-
additional information
-
phosphorylation by ERK1/2 inhibits GRK2
-
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.
Please wait a moment until the data is sorted. This message will disappear when the data is sorted.