G protein-coupled receptors (GPCRs) are a highly validated drug target family – accounting for 30-35 percent of all approved drugs. Despite this, the therapeutic potential of targeting most GPCRs remains untapped, as only 10 percent of GPCRs have been drugged. In this article, Stephan Schann, Chief Scientific Officer at Domain Therapeutics, explains why this class of drug target is so useful despite the challenges they present.
GPCRs: the master cell signallers with huge therapeutic potential
GPCRs are the largest and most diverse group of cell-surface receptors in the body, with more than 800 known types in humans. They are at the heart of cellular communication, translating extracellular signals – such as hormones, smell, taste, light and neurotransmitters – into intracellular actions.
Moreover, GPCRs have a complex pharmacology, with each acting as a kind of signalling hub for an array of downstream signals, in contrast to simpler receptors which are generally responsible for one signal.
https://www.drugtargetreview.com/article/1626...y-disease/