CATH Domain 5he2A02

CATH Classification

Level	CATH Code	Description
	1	Mainly Alpha
	1.10	Orthogonal Bundle
	1.10.167	Regulator of G-protein Signalling 4; domain 2
	1.10.167.10	Regulator of G-protein Signalling 4, domain 2

Domain Context

CATH Clusters

Superfamily	Regulator of G-protein Signalling 4, domain 2
Functional Family

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	5HE2
External Links	PDBSum Proteopedia
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.