Rescue of defective G protein-coupled receptor function in vivo by intermolecular cooperation

Proc Natl Acad Sci U S A. 2010 Feb 2;107(5):2319-24. doi: 10.1073/pnas.0906695106. Epub 2010 Jan 11.

Abstract

G protein-coupled receptors (GPCRs) are ubiquitous mediators of signaling of hormones, neurotransmitters, and sensing. The old dogma is that a one ligand/one receptor complex constitutes the functional unit of GPCR signaling. However, there is mounting evidence that some GPCRs form dimers or oligomers during their biosynthesis, activation, inactivation, and/or internalization. This evidence has been obtained exclusively from cell culture experiments, and proof for the physiological significance of GPCR di/oligomerization in vivo is still missing. Using the mouse luteinizing hormone receptor (LHR) as a model GPCR, we demonstrate that transgenic mice coexpressing binding-deficient and signaling-deficient forms of LHR can reestablish normal LH actions through intermolecular functional complementation of the mutant receptors in the absence of functional wild-type receptors. These results provide compelling in vivo evidence for the physiological relevance of intermolecular cooperation in GPCR signaling.

Publication types

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

MeSH terms

  • Animals
  • Cell Line
  • Chorionic Gonadotropin / metabolism
  • Genetic Complementation Test
  • Humans
  • Male
  • Mice
  • Mice, Knockout
  • Mice, Mutant Strains
  • Mice, Transgenic
  • Models, Biological
  • Models, Molecular
  • Mutation
  • Phenotype
  • Protein Binding
  • Protein Multimerization
  • Receptors, G-Protein-Coupled / chemistry*
  • Receptors, G-Protein-Coupled / metabolism*
  • Receptors, LH / chemistry*
  • Receptors, LH / deficiency
  • Receptors, LH / genetics
  • Receptors, LH / metabolism*
  • Recombinant Proteins / chemistry
  • Recombinant Proteins / genetics
  • Recombinant Proteins / metabolism
  • Signal Transduction
  • Testis / metabolism
  • Testis / pathology

Substances

  • Chorionic Gonadotropin
  • Receptors, G-Protein-Coupled
  • Receptors, LH
  • Recombinant Proteins