Phosducin inhibits receptor phosphorylation by the beta-adrenergic receptor kinase in a PKA-regulated manner

FEBS Lett. 1994 Apr 25;343(2):120-4. doi: 10.1016/0014-5793(94)80302-1.

Abstract

Homologous or receptor-specific desensitization of beta-adrenergic receptors is thought to be triggered by receptor phosphorylation mediated by the beta-adrenergic receptor kinases (beta ARK). Upon receptor activation, cytosolic beta ARK translocates to the membrane, probably by binding to G-protein beta gamma-subunits. Using the purified proteins reconstituted into phospholipid vesicles we show here that this binding process can be inhibited by phosducin, a cytosolic protein that has recently been described as a regulator of G-protein-mediated signalling. Phosducin appears to complete very effectively with beta ARK for the G-protein beta gamma-subunits. These inhibitory effects of phosducin on receptor phosphorylation are antagonized following phosphorylation of phosducin by protein kinase A. It is proposed that phosducin may act as a regulator of homologous beta-adrenergic receptor desensitization.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Cell Line
  • Cyclic AMP-Dependent Protein Kinases / antagonists & inhibitors*
  • Cyclic AMP-Dependent Protein Kinases / metabolism*
  • Eye Proteins / pharmacology*
  • GTP-Binding Protein Regulators
  • GTP-Binding Proteins / metabolism
  • Humans
  • Molecular Sequence Data
  • Phosphoproteins / pharmacology*
  • Phosphorylation
  • Signal Transduction
  • beta-Adrenergic Receptor Kinases

Substances

  • Eye Proteins
  • GTP-Binding Protein Regulators
  • Phosphoproteins
  • phosducin
  • Cyclic AMP-Dependent Protein Kinases
  • beta-Adrenergic Receptor Kinases
  • GTP-Binding Proteins