Long-sought chemical inhibitors of β-arrestin proteins

Nature, Published online: 24 June 2026; doi:10.1038/d41586-026-01894-x

Proteins called β-arrestins regulate signalling through members of the G protein-coupled receptor (GPCR) superfamily. Small molecules that bind directly to the β-arrestins and inhibit their activities are the first chemical tools to probe their biology, opening avenues for transducer-targeted, pathway-specific GPCR therapeutics.