G-protein-coupled receptor kinase 5 phosphorylates p53 and inhibits DNA damage-induced apoptosis

J Biol Chem. 2010 Apr 23;285(17):12823-30. doi: 10.1074/jbc.M109.094243. Epub 2010 Feb 2.

Abstract

G-protein-coupled receptor kinases (GRKs) are an important family of Ser/Thr kinases that specifically phosphorylate and desensitize the activated receptor in response to environmental stimulation. Here we identify p53, a key tumor suppressor, as a novel GRK substrate in vivo, revealing a previously unknown function of GRKs in regulation of genome stability. Knockdown GRK5 in osteosarcoma cells inhibits DNA damage-induced apoptosis via a p53-mediated mechanism. Furthermore, GRK5, but not GRK2 or GRK6, phosphorylates p53 at Thr-55, which promotes the degradation of p53, leading to inhibition of p53-dependent apoptotic response to genotoxic damage. Consistently, the increase of p53 and irradiation-induced apoptosis were observed in GRK5-deficient mice. These results demonstrate GRK5 as a novel kinase of p53, as well as a negative regulator of p53-mediated signal transduction.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Apoptosis / drug effects
  • Apoptosis / physiology*
  • Apoptosis / radiation effects
  • Cell Line, Tumor
  • DNA Damage / drug effects
  • DNA Damage / genetics
  • DNA Damage / physiology*
  • DNA Damage / radiation effects
  • G-Protein-Coupled Receptor Kinase 5 / genetics
  • G-Protein-Coupled Receptor Kinase 5 / metabolism*
  • Gamma Rays / adverse effects
  • Humans
  • Mice
  • Mice, Knockout
  • Phosphorylation / drug effects
  • Phosphorylation / physiology
  • Phosphorylation / radiation effects
  • Signal Transduction / drug effects
  • Signal Transduction / physiology*
  • Signal Transduction / radiation effects
  • Tumor Suppressor Protein p53 / genetics
  • Tumor Suppressor Protein p53 / metabolism*

Substances

  • TP53 protein, human
  • Tumor Suppressor Protein p53
  • G-Protein-Coupled Receptor Kinase 5
  • GRK5 protein, human
  • Grk5 protein, mouse