Receptors are areas of certain proteins and glycoproteins which are conveying different stimuli upon activating by specific ligands. Activating of a receptor enables a signal transduction pathway usually by activating specific proteins. Receptors which bind G proteins upon activation are called G protein-coupled receptors (GCPRs). According to the traditional two-state model of receptor theory, GPCRs were considered as operating in equilibrium between two functional conformations, an active and inactive state. It also was thought that GPCRs were to activate only G proteins to induce response. More recent data show that numerous other signalling proteins, such as β-arrestins and phosphorylating enzymes, may interact with GPCRs and activate different intracellular signalling pathways. This also may involve pathways that are independent of G proteins. Various ligands that affect GPCR in a different way and activate specific signalling pathways have been discovered that gave rise to a concept called (among others) ligand-directed receptor trafficking. A ligand might act as an agonist for one signalling pathway while behaving as an antagonist, partial agonist, or have no effect for another signalling pathway. Side effects can arise not only because of the drug binding to different receptors but also by activating different signalling pathways of the same receptor. Challenge for new drug development may therefore not only be to discover compounds with high receptor specificity, but also compounds that can distinguish between the signalling pathways of a particular receptor.

The work was partially supported by the Polish Norwegian Research Program grant Pol-Nor/198887/73/2013.

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