Preso1 dynamically regulates group I metabotropic glutamate receptors

Nat Neurosci. 2012 Jun;15(6):836-44. doi: 10.1038/nn.3103.

Abstract

Group I metabotropic glutamate receptors (mGluRs), including mGluR1 and mGluR5, are G protein–coupled receptors (GPCRs) that are expressed at excitatory synapses in brain and spinal cord. GPCRs are often negatively regulated by specific G protein–coupled receptor kinases and subsequent binding of arrestin-like molecules. Here we demonstrate an alternative mechanism in which group I mGluRs are negatively regulated by proline-directed kinases that phosphorylate the binding site for the adaptor protein Homer, and thereby enhance mGluR–Homer binding to reduce signaling. This mechanism is dependent on a multidomain scaffolding protein, Preso1, that binds mGluR, Homer and proline-directed kinases and that is required for their phosphorylation of mGluR at the Homer binding site. Genetic ablation of Preso1 prevents dynamic phosphorylation of mGluR5, and Preso1(−/−) mice exhibit sustained, mGluR5-dependent inflammatory pain that is linked to enhanced mGluR signaling. Preso1 creates a microdomain for proline-directed kinases with broad substrate specificity to phosphorylate mGluR and to mediate negative regulation.

Publication types

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

MeSH terms

  • Amino Acid Sequence
  • Animals
  • Blotting, Western
  • Brain / metabolism
  • Carrier Proteins / chemistry
  • Carrier Proteins / metabolism*
  • HEK293 Cells
  • Homer Scaffolding Proteins
  • Humans
  • Immunohistochemistry
  • Immunoprecipitation
  • Male
  • Mice
  • Mice, Knockout
  • Molecular Sequence Data
  • Neurons / metabolism*
  • Phosphorylation
  • Post-Synaptic Density
  • Proline-Directed Protein Kinases / metabolism
  • Protein Binding
  • Protein Structure, Tertiary
  • Rats
  • Rats, Wistar
  • Receptors, Metabotropic Glutamate / chemistry
  • Receptors, Metabotropic Glutamate / metabolism*
  • Signal Transduction / physiology*
  • Transfection

Substances

  • Carrier Proteins
  • Homer Scaffolding Proteins
  • Receptors, Metabotropic Glutamate
  • Proline-Directed Protein Kinases