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Small-molecule modulation of β-arrestins

Nature

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Nature, Published online: 24 June 2026; doi:10.1038/s41586-026-10683-5
Integrated pharmacological, biochemical, biophysical and structural analyses of small-molecule β-arrestin inhibitors show how they block β-arrestin engagement with activated GPCRs, revealing their mechanism of action and uncovering a previously unrecognized allosteric regulatory site. ...

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

Long-sought chemical inhibitors of β-arrestin proteins

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