Editorial: Recent Advances in G Protein-Coupled Receptor Signalling: Impact of Intracellular Location, Environment and Biased Agonism

This is the authors' abstract. We don't add key points for this paper.

G protein-coupled receptors (GPCRs), the largest family of cell surface receptors, are targeted by approximately 35% of approved drugs that treat a wide variety of diseases including those of the cardiovascular, respiratory, metabolic, and reproductive systems, and of the central, and peripheral nervous system. Currently the great majority of approved drugs interact with orthosteric binding sites on the receptor as agonists, partial agonists, antagonists or inverse agonists. Of some 800 GPCRs only about 12% have been utilised therapeutically with the remainder being either olfactory or orphan receptors with many having poorly understood signalling mechanisms.