A G protein-coupled receptor (GPCR) is a cell-surface transmembrane receptor that works with the help of a G-protein. Ch
GPCR activation promotes guanine nucleotide exchange on heterotrimeric G-alpha subunit, replacing GDP with GTP. GTP-bound alpha dissociates to regulate effectors like adenylyl cyclase. Intrinsic GTPase later hydrolyzes GTP to GDP terminating signaling cascade.
Ref: Alberts et al., Molecular Biology of the Cell, 6th Edition, Chapter 15 and Nelson and Cox, Lehninger Principles of Biochemistry, 7th Edition, Chapter 12 discuss GPCR signaling where heterotrimeric G-proteins bind GTP upon activation to modulate downstream effectors, published by Garland and Freeman.