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Literature summary for 2.7.11.15 extracted from

  • Kang, J.H.; Toita, R.; Kawano, T.; Murata, M.; Asai, D.
    Design of substrates and inhibitors of G protein-coupled receptor kinase 2 (GRK2) based on its phosphorylation reaction (2020), Amino Acids, 52, 863-870 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
balanol
-
Homo sapiens
CCG215022
-
Homo sapiens
CCG224061
-
Homo sapiens
CCG224406
-
Homo sapiens
CCG258748
-
Homo sapiens
CMPD101
-
Homo sapiens
CMPD103A
-
Homo sapiens
GSK180736A
-
Homo sapiens
additional information S-nitrosylation at Cys-340 inhibits isoform GRK2 activity Homo sapiens
paroxetine
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0324
-
DEMEFTEAESNMNDLVSEYQ pH and temperature not specified in the publication Homo sapiens
0.0339
-
DEMEFTEAESNMN pH and temperature not specified in the publication Homo sapiens
0.054
-
EEMEFSEAEANMN pH and temperature not specified in the publication Homo sapiens
0.1
-
GEGMDEMEFTEAESNMN Km above 0.1 mM, pH and temperature not specified in the publication Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein enzyme phosphorylation at Tyr-13, Try-86, and Try-92 by c-Src and phosphorylation at Ser-685 by protein kinase A are associated with increased enzyme activity, whereas phosphorylation at Ser-670 by CDK2/ERK1/2 negatively regulates enzyme activity Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + AGDVESFLNEA
-
Homo sapiens ADP + AGDVEpSFLNEA
-
?
ATP + beta2-adrenergic receptor
-
Homo sapiens ADP + phosphorylated beta2-adrenergic receptor
-
?
ATP + DEKKEESEESDDDMG
-
Homo sapiens ADP + DEKKEEpSEESDDDMG
-
?
ATP + DEMEFTEAESNMN
-
Homo sapiens ADP + DEMEFpTEAESNMN
-
?
ATP + DEMEFTEAESNMNDLVSEYQ
-
Homo sapiens ADP + DEMEFpTEAESNMNDLVSEYQ
-
?
ATP + EAYEMPSEEGYQD
-
Homo sapiens ADP + EAYEMPpSEEGYQD
-
?
ATP + EEMEFSEAEANMN
-
Homo sapiens ADP + EEMEFpSEAEANMN
-
?
ATP + GEGMDEMEFTEAESNMN
-
Homo sapiens ADP + GEGMDEMEFpTEAESNMN
-
?
ATP + GMEGLGTDITVI
-
Homo sapiens ADP + GMEGLGpTDITVI
-
?
ATP + GPEPWETISEEMNM
-
Homo sapiens ADP + GPEPWEpTISEEMNM
-
?
ATP + GRDKYKTLRQIRQG
-
Homo sapiens ADP + GRDKYKpTLRQIRQG
-
?
ATP + histone deacetylase 6 phosphorylation at Ser-670 Homo sapiens ADP + phosphorylated histone deacetylase 6
-
?
ATP + insulin receptor substrate-1 phosphorylation at Ser-307 Homo sapiens ADP + phosphorylated insulin receptor substrate-1
-
?
ATP + KKELQSLYRGFK
-
Homo sapiens ADP + KKELQpSLYRGFK
-
?
ATP + LDTMESDSEVEAI
-
Homo sapiens ADP + LDTMESDpSEVEAI
-
?
ATP + MEPEGESYEDPPQ
-
Homo sapiens ADP + MEPEGEpSYEDPPQ
-
?
ATP + MNDLVSEYQQYQ
-
Homo sapiens ADP + MNDLVpSEYQQYQ
-
?
ATP + PGWEERTHTDGRVF
-
Homo sapiens ADP + PGWEERpTHTDGRVF
-
?
ATP + PPLDDYTHSIPEN
-
Homo sapiens ADP + PPLDDYpTHSIPEN
-
?
ATP + PRAEAEDSFL
-
Homo sapiens ADP + PRAEAEDpSFL
-
?
ATP + rhodopsin
-
Homo sapiens ADP + phosphorylated rhodopsin
-
?
ATP + RRREEEEESAAA
-
Homo sapiens ADP + RRREEEEEpSAAA
-
?
ATP + VKCQKLTDDHVQF
-
Homo sapiens ADP + VKCQKLpTDDHVQF
-
?
ATP + VPSDNIDSQGRNC
-
Homo sapiens ADP + VPSDNIDpSQGRNC
-
?
ATP + VSKTETSQVAPA
-
Homo sapiens ADP + VSKTETpSQVAPA
-
?

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 2
-
Homo sapiens
GRK2
-
Homo sapiens