Experimental strategies for studying g protein-coupled receptor homo- and heteromerization with radioligand binding and signal transduction methods

Before the molecular biology era, functional experiments on isolated organs and radioligand binding and biochemical experiments on animal tissues were widely used to characterize G protein-coupled receptors (GPCRs). The introduction of recombinant cell lines expressing a single GPCR type has been a big step forward for studying both drug receptor interactions and signal transduction. Before the introduction of the con- cept of receptor oligomerization, all data generated were attributed to the interaction of drugs with receptor monomers. Now, considerable data must be reinterpreted in light of receptor homo- and heteromerization. In this chapter, we will review some of the methods used to study radioligand binding and signal transduction modifications induced by GPCR homo- and heteromerization