Understanding of the functional significance of the wide structural diversity of G-protein-coupled receptors (GPCRs) — one of the most important families of drug targets — has advanced considerably in recent years. This article provides a comprehensive overview of the five main human GPCR families, discussing gene repertoire, general ligand preference, common and unique structural features, and the potential for future drug discovery.
- Malin C. Lagerström
- Helgi B. Schiöth
