CATH Classification

Domain Context

CATH Clusters

Superfamily Transferase(Phosphotransferase) domain 1
Functional Family G protein-coupled receptor kinase

Enzyme Information

2.7.11.15
[Beta-adrenergic-receptor] kinase.
based on mapping to UniProt P21146
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)

P21146
ARBK1_BOVIN
Bos taurus
Beta-adrenergic receptor kinase 1
P59768
GBG2_HUMAN
Homo sapiens
Guanine nucleotide-binding protein G(I)/G(S)/G(O) subunit gamma-2

PDB Structure

PDB 5HE3
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Structure-Based Design, Synthesis, and Biological Evaluation of Highly Selective and Potent G Protein-Coupled Receptor Kinase 2 Inhibitors.
Waldschmidt, H.V., Homan, K.T., Cruz-Rodriguez, O., Cato, M.C., Waninger-Saroni, J., Larimore, K.M., Cannavo, A., Song, J., Cheung, J.Y., Kirchhoff, P.D., Koch, W.J., Tesmer, J.J., Larsen, S.D.
J.Med.Chem.