Liganded Gs-activating GPCR acts as a GEF for Gs

Stable Identifier
Homo sapiens
Locations in the PathwayBrowser

The liganded receptor undergoes a conformational change, generating a signal that is propagated in a manner that is not completely understood to the the G-protein. This stimulates the exchange of GDP for GTP in the G-protein alpha subunit, activating the G-protein. This event is negatively regulated by some Activators of G protein signaling (AGS) proteins, a class of proteins identified in yeast functional screens for proteins able to activate G protein signaling in the absence of a G protein?coupled receptor (GPCR) (Cismowski et al. 1999, Takesono et al. 1999). AGS proteins contain G protein regulatory (GPR) motifs (also referred to as the GoLoco motif) that bind and stabilize the Galpha subunit in its GDP-bound conformation (Mochizuki et al. 1996, Peterson et al. 2000, Cao et al. 2004, Blumer & Lanier 2014). Some RGS proteins similarly bind to Galpha preventing the exchange of GDP for GTP (Soundararajan et al. 2008).

Participant Of
Catalyst Activity
Catalyst Activity
guanyl-nucleotide exchange factor activity of Ligand:GPCR complexes that activate Gs:Heterotrimeric G-protein Gs (inactive) [plasma membrane]
Physical Entity
Orthologous Events