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Literature summary for 2.7.11.16 extracted from

  • Beyett, T.; Chen, Q.; Labudde, E.; Krampen, J.; Sharma, P.; Tesmer, J.
    Characterization of a hyperphosphorylated variant of G protein-coupled receptor kinase 5 expressed in E. coli (2020), Protein Expr. Purif., 168, 105547 .
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Escherichia coli BL21 Rosetta cells Homo sapiens

Protein Variants

Protein Variants Comment Organism
S500A the mutant shows decreased activity compared to the wild type enzyme Homo sapiens
T10A the mutant shows increased activity compared to the wild type enzyme Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
CCG-215022
-
Homo sapiens

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0012
-
rhodopsin recombinant mutant enzyme T10A, at pH 8.0 and 25°C Homo sapiens
0.0018
-
rhodopsin recombinant wild type enzyme, at pH 8.0 and 25°C Homo sapiens
0.014
-
ATP recombinant mutant enzyme T10A, at pH 8.0 and 25°C Homo sapiens
0.014
-
ATP recombinant wild type enzyme, at pH 8.0 and 25°C Homo sapiens
0.02
-
ATP recombinant mutant enzyme S500A, at pH 8.0 and 25°C Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P34947
-
-

Posttranslational Modification

Posttranslational Modification Comment Organism
phosphoprotein the enzyme is hyperphosphorylated Homo sapiens

Purification (Commentary)

Purification (Comment) Organism
HiTrap S column chromatography and HiTrap Q column chromatography Homo sapiens

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
ATP + rhodopsin
-
Homo sapiens ADP + phosphorylated rhodopsin
-
?

Subunits

Subunits Comment Organism
monomer 1 * 70000, SDS-PAGE Homo sapiens
monomer 1 * 68824, mass spectrometry Homo sapiens

Synonyms

Synonyms Comment Organism
G protein-coupled receptor kinase 5
-
Homo sapiens
GRK5
-
Homo sapiens

kcat/KM [mM/s]

kcat/KM Value [1/mMs-1] kcat/KM Value Maximum [1/mMs-1] Substrate Comment Organism Structure
2.9
-
rhodopsin recombinant wild type enzyme, at pH 8.0 and 25°C Homo sapiens
4.1
-
ATP recombinant mutant enzyme S500A, at pH 8.0 and 25°C Homo sapiens
5.9
-
ATP recombinant wild type enzyme, at pH 8.0 and 25°C Homo sapiens
6.5
-
rhodopsin recombinant mutant enzyme T10A, at pH 8.0 and 25°C Homo sapiens
8.7
-
ATP recombinant mutant enzyme T10A, at pH 8.0 and 25°C Homo sapiens