Oligomers of D-2 dopamine receptors - Evidence from ligand binding

Strange, P. G. (2005) Oligomers of D-2 dopamine receptors - Evidence from ligand binding. Journal of Molecular Neuroscience, 26 (2-3). pp. 155-159. ISSN 0895-8696 doi: 10.1385/jmn/26:02:155

Abstract/Summary

There is increasing evidence that G protein-coupled receptors form oligomers and that this might be important for their function. We have studied this phenomenon for the D-2 dopamine receptor and have shown-using a variety of biochemical and biophysical techniques-that this receptor forms dimers or higher-order oligomers. Using ligand-binding studies, we have also found evidence that this oligomer formation has functional relevance. Thus, for the receptor expressed in either CHO cells or Sf 9 insect cells, the binding properties of several radioligands (in saturation, competition, and dissociation assays) do not conform to those expected for a monomeric receptor with a single binding site. We propose that the receptors exist in oligomers with homotropic and heterotropic negatively cooperative interactions between ligands.