CATH Classification

Domain Context

CATH Clusters

Superfamily Phosphorylase Kinase; domain 1
Functional Family G protein-coupled receptor kinase

Enzyme Information

2.7.11.15
[Beta-adrenergic-receptor] kinase.
based on mapping to UniProt P25098
ATP + [beta-adrenergic receptor] = ADP + [beta-adrenergic receptor] phosphate.
-!- Acts on the agonist-occupied form of the receptor; also phosphorylates rhodopsin, but more slowly. -!- Does not act on casein or histones. -!- Inhibited by Zn(2+) and digitonin but is unaffected by cyclic-AMP (cf. EC 2.7.11.14 and EC 2.7.11.16). -!- Formerly EC 2.7.1.126.

UniProtKB Entries (2)

P63212
GBG2_BOVIN
Bos taurus
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2
P25098
ARBK1_HUMAN
Homo sapiens
Beta-adrenergic receptor kinase 1

PDB Structure

PDB 3V5W
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Paroxetine is a direct inhibitor of g protein-coupled receptor kinase 2 and increases myocardial contractility.
Thal, D.M., Homan, K.T., Chen, J., Wu, E.K., Hinkle, P.M., Huang, Z.M., Chuprun, J.K., Song, J., Gao, E., Cheung, J.Y., Sklar, L.A., Koch, W.J., Tesmer, J.J.
Acs Chem.Biol.