Nano‐G s Protein Peptidomimetics: Rational Design of Gα C‐Terminus‐Derived Peptides Mimicking Key Components of G s ‐β 2 AR Interactions

G protein-coupled receptors (GPCRs) are involved in most human physiological processes and one of the largest families of approved drug-targeted proteins. Heterotrimeric Gαβɣ proteins bind to the intracellular cavity of the activated receptor mainly through the C-terminal α5 helix of the Gα subunit (GαCT). Modulation of GPCR activity through intracellular GPCR binding sites is emerging. Here we develop highly active Gα_sCT-derived peptidomimetics that stabilize the β₂ adrene