New Insights into GPCR Function: Implications for HTS

G protein-coupled receptors (GPCRs) are a large family of proteins that represent targets for approximately 40% of all approved drugs. They possess unique structural motifs that allow them to interact with a diverse series of extracellular ligands, as well as intracellular signaling proteins, such as G proteins, RAMPs, arrestins, and indeed other receptors. Extensive efforts are under way to discover new generations of drugs against GPCRs with unique targeted therapeutic uses, including “designer” drugs such as allosteric regulators, inverse agonists, and drugs targeting hetero-oligomeric complexes. This has been facilitated by the development of new screening technologies to identify novel drugs against both known and orphan GPCRs.