Excessive signaling by G protein-coupled receptors (GPCRs) contributes to various human disorders, necessitating novel therapeutic strategies. Here, the authors identify a small molecule that enhances arrestin-3 binding to a specific GPCR β2-adrenergic receptor by stabilizing a pre-activated conformation, offering a promising approach for selective modulation of GPCR signaling in disease treatment.
- Han Kurt
- Ali Akyol
- Ozge Sensoy
