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Long-sought chemical inhibitors of β-arrestin proteins

Nature

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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. ...

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By making key signaling molecules called β-arrestins into druggable targets, scientists crack long-standing challenge

Small-molecule modulation of β-arrestins

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