International Union of Basic and Clinical Pharmacology. LXVII. Recommendations for the recognition and nomenclature of G protein-coupled receptor heteromultimers

Abstract

G protein-coupled receptors (GPCRs) have long been considered to be monomeric membrane proteins. Although numerous recent studies have indicated that GPCRs can form multimeric complexes, the functional and pharmacological consequences of this phenomenon have remained elusive. With the discovery that the functional GABA(B) receptor is an obligate heterodimer and with the use of energy transfer technologies, it is now accepted that GPCRs can form heteromultimers. In some cases, specific properties of such heteromers not shared by their respective homomers have been reported. Although in most cases these properties have only been observed in heterologous expression systems, there are a few reports describing data consistent with such heteromultimeric GPCR complexes also existing in native tissues. The present article illustrates well-documented examples of such native multimeric complexes, lists a number of recommendations for recognition and acceptance of such multimeric receptors, and gives recommendations for their nomenclature.