Development of Generic G Protein Peptidomimetics Able to Stabilize Active State Gs and Gq Protein-Coupled Receptors for Application in Drug Discovery
G protein-coupled receptors (GPCRs) are central to many therapeutic areas, but their conformational flexibility—favoring a basal state—makes agonist discovery challenging. To address this, we developed peptidomimetics that mimic the α5 helix of G proteins, effectively stabilizing the active conformations of β2-adrenergic (β2AR) and dopamine D1 (D1R) receptors. These molecules enabled the identi...
2025-06-06