Building the Next Generation of GPCR-Targeting Drugs

One-third of marketed drugs hit G-protein coupled receptors, a group of cell-membrane bound receptors that are involved in almost every possible biological system. Drugs targeting GPCRs span most therapy areas, specialist or primary care, and may be small molecules, peptides, or large proteins. Despite their ubiquity, there's plenty of untapped potential too. Small wonder that start-ups continue to appear in this field, each with its own approach to improving existing drugs and finding new ones. We profile four in this issue.