Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 2.7.11.15 extracted from

  • Tesmer, J.J.; Tesmer, V.M.; Lodowski, D.T.; Steinhagen, H.; Huber, J.
    Structure of human G protein-coupled receptor kinase 2 in complex with the kinase inhibitor balanol (2010), J. Med. Chem., 53, 1867-1870.
    View publication on PubMedView publication on EuropePMC

Cloned(Commentary)

Cloned (Comment) Organism
expressed in Sf9 clls using the baculovirus expression system Homo sapiens

Crystallization (Commentary)

Crystallization (Comment) Organism
crystal structures of human GRK2 in complex with Gbetagamma in the presence and absence of the AGC (protein kinase A, kinase G, and kinase C subfamily) kinase inhibitor balanol is determined. Balanol stabilizes the kinase domain of GRK2 in a slightly more closed conformation distinct from that of the protein kinase A balanol complex Homo sapiens

Inhibitors

Inhibitors Comment Organism Structure
balanol
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P25098
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
GRK2
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
20
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00005
-
pH 7.4, 20°C Homo sapiens balanol