The role of GRK6 in animal models of Parkinson's disease and L-DOPA treatment

Sci Rep. 2012:2:301. doi: 10.1038/srep00301. Epub 2012 Mar 5.

Abstract

G protein-coupled Receptor Kinase 6 (GRK6) belongs to a family of kinases that phosphorylate GPCRs. GRK6 levels were found to be altered in Parkinson's Disease (PD) and D(2) dopamine receptors are supersensitive in mice lacking GRK6 (GRK6-KO mice). To understand how GRK6 modulates the behavioral manifestations of dopamine deficiency and responses to L-DOPA, we used three approaches to model PD in GRK6-KO mice: 1) the cataleptic response to haloperidol; 2) introducing GRK6 mutation to an acute model of absolute dopamine deficiency, DDD mice; 3) hemiparkinsonian 6-OHDA model. Furthermore, dopamine-related striatal signaling was analyzed by assessing the phosphorylation of AKT/GSK3β and ERK1/2. GRK6 deficiency reduced cataleptic behavior, potentiated the acute effect of L-DOPA in DDD mice, reduced rotational behavior in hemi-parkinsonian mice, and reduced abnormal involuntary movements induced by chronic L-DOPA. These data indicate that approaches to regulate GRK6 activity could be useful in modulating both therapeutic and side-effects of L-DOPA.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cyclic AMP / metabolism
  • Disease Models, Animal*
  • Extracellular Signal-Regulated MAP Kinases / metabolism
  • G-Protein-Coupled Receptor Kinases / genetics*
  • Glycogen Synthase Kinase 3 / metabolism
  • Glycogen Synthase Kinase 3 beta
  • Levodopa / therapeutic use*
  • Locomotion
  • Mice
  • Mice, Inbred C57BL
  • Mice, Knockout
  • Mutation
  • Parkinson Disease / drug therapy
  • Parkinson Disease / enzymology*
  • Proto-Oncogene Proteins c-akt / metabolism
  • Signal Transduction

Substances

  • Levodopa
  • Cyclic AMP
  • Glycogen Synthase Kinase 3 beta
  • Gsk3b protein, mouse
  • Proto-Oncogene Proteins c-akt
  • G-Protein-Coupled Receptor Kinases
  • G-protein-coupled receptor kinase 6
  • Extracellular Signal-Regulated MAP Kinases
  • Glycogen Synthase Kinase 3