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GRK-biased adrenergic agonists for the treatment of type 2 diabetes and obesity

23 Jun 2025

Abstract excerpt

Biased agonism of G protein-coupled receptors (GPCRs) offers potential for safer medications. Current efforts have explored the balance between G proteins and β-arrestin; however, other transducers like GPCR kinases (GRKs) remain understudied. GRK2 is essential for β 2 adrenergic receptor (β 2 AR)-mediated glucose uptake, but β 2 AR agonists are considered poor clinical candidates for glycemic management due to G...

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PMID: 40555230
DOI: 10.1016/j.cell.2025.05.042

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