24 June 2026

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.

This is a summary of: Kahsai, A. W. et al. Small-molecule modulation of β-arrestins. Nature https://doi.org/10.1038/s41586-026-10683-5 (2026).

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