Characterization of constitutively active mutants of G protein-coupled receptors

Methods Mol Biol. 2006:332:129-39. doi: 10.1385/1-59745-048-0:129.

Abstract

The ability of G protein-coupled receptors to transduce signaling typically is induced by the binding of an appropriate ligand (agonist), resulting in a conformational change of the receptor and the subsequent interaction with the G protein heterotrimer. Some mutants of G protein-coupled receptors, known as constitutively active mutants, have the capacity to activate the G protein-signaling cascade even in the absence of ligand. In this chapter, we describe three methods that most directly allow characterization of constitutively active mutants and discriminate them from the wild-type receptors. All methods are based on the spontaneous signaling function in the absence of ligand and its consequences on the receptor.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • CHO Cells
  • Cricetinae
  • Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
  • Humans
  • Ligands
  • Mutation*
  • Phosphorylation
  • Protein Binding
  • Receptors, CXCR4 / genetics
  • Receptors, CXCR4 / metabolism
  • Receptors, G-Protein-Coupled / chemistry
  • Receptors, G-Protein-Coupled / genetics
  • Receptors, G-Protein-Coupled / metabolism*
  • Second Messenger Systems / physiology*

Substances

  • Ligands
  • Receptors, CXCR4
  • Receptors, G-Protein-Coupled
  • Guanosine 5'-O-(3-Thiotriphosphate)