Ligand-dependent G protein dynamics underlying opioid efficacy
Activation of heterotrimeric G proteins by G-protein-coupled receptors (GPCRs) requires large-scale opening of the Gα α-helical domain (AHD) to expose the nucleotide-binding site and facilitate GDP–GTP exchange. Although orthosteric ligands are known to modulate GPCR conformation, how these effects propagate to the bou...