G-protein-coupled receptor heterodimers: pharmacology, function and relevance to drug discovery

Drug Discov Today. 2006 Jun;11(11-12):541-9. doi: 10.1016/j.drudis.2006.04.007.


The growing recognition that members of the rhodopsin-like family A G-protein-coupled receptors (GPCRs) exist and function as dimers or higher-order oligomers, and that GPCR hetero-dimers and -oligomers are present in physiological tissues, offers novel opportunities for drug discovery. Differential pharmacology, function and regulation of GPCR hetero-dimers and -oligomers suggest means to selectively target GPCRs in different tissues and hint that the mechanism of function of several pharmacological agents might be different in vivo than anticipated from simple ligand-screening programmes that rely on heterologous expression of a single GPCR.

Publication types

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

MeSH terms

  • Animals
  • Drug Design*
  • Heterotrimeric GTP-Binding Proteins* / chemistry
  • Heterotrimeric GTP-Binding Proteins* / metabolism
  • Heterotrimeric GTP-Binding Proteins* / physiology
  • Humans
  • Ligands
  • Receptors, G-Protein-Coupled* / chemistry
  • Receptors, G-Protein-Coupled* / metabolism
  • Receptors, G-Protein-Coupled* / physiology


  • Ligands
  • Receptors, G-Protein-Coupled
  • Heterotrimeric GTP-Binding Proteins