Metabotropic GABAB Receptor Activation Induced by G Protein Coupling

G protein-coupled receptors (GPCRs) play central roles in regulating cellular responses through heterotrimeric G proteins (GP). Extensive studies have elucidated the complex cellular signaling mediated by GPCRs that accompany dynamic conformational changes upon activation. However, there has been less focus on the role of the GP on the activation process, particularly for class C GPCRs that function as obligate dimers. Herein, we report the pivotal role of GP coupling on the dynamic activation process for the metabotropic γ-aminobutyric acid receptor (GABA