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)

P62871
GBB1_BOVIN
Bos taurus
Guanine nucleotide-binding protein G(I)/G(S)/G(T) subunit beta-1
P25098
ARBK1_HUMAN
Homo sapiens
Beta-adrenergic receptor kinase 1

PDB Structure

PDB 6C2Y
External Links
Method X-RAY DIFFRACTION
Organism
Primary Citation
Utilizing a structure-based docking approach to develop potent G protein-coupled receptor kinase (GRK) 2 and 5 inhibitors.
Waldschmidt, H.V., Bouley, R., Kirchhoff, P.D., Lee, P., Tesmer, J.J.G., Larsen, S.D.
Bioorg. Med. Chem. Lett.