CATH Domain 3v5wA02

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 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	PDBSum Proteopedia
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.