Novel pharmacological applications of G-protein-coupled receptor-G protein fusions

Curr Opin Pharmacol. 2007 Oct;7(5):521-6. doi: 10.1016/j.coph.2007.06.007. Epub 2007 Aug 6.


Single, bi-functional polypeptides consisting of a G-protein-coupled receptor (GPCR) linked directly to a G protein alpha subunit have been employed for a number of years to study many aspects of signal initiation, including the roles of post-translational modifications, effects of mutations in both receptor and G protein and in the de-orphanisation of novel G-protein-coupled receptors. Recently, they have been used to improve signal-to-background in ligand assay screens and to study both agonist-directed signal trafficking and distinct conformational states of receptors. As well as such novel concepts in pharmacology, G-protein-coupled receptor-G protein fusions have recently been employed to examine receptor homo-dimerisation and hetero-dimerisation and are beginning to be used to explore allosteric effects within GPCR hetero-dimers.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Dimerization
  • GTP-Binding Protein alpha Subunits / metabolism*
  • Humans
  • Receptors, G-Protein-Coupled / metabolism*
  • Recombinant Fusion Proteins / metabolism*


  • GTP-Binding Protein alpha Subunits
  • Receptors, G-Protein-Coupled
  • Recombinant Fusion Proteins