G-Protein Activation

1. When not activated, the alpha subunit binds GDP.

2. When the ligand binds to the GPCR, it changes conformation
and, in turn, alters the conformation of the G protein.
3. Altering the conformation of the alpha subunit allows it to
exchange GDP for GTP.
4. The binding of GTP to the alpha subunit results in dissociation
from the beta subunit.
5. These are now two independent entities: the alpha subunit and
the beta-gamma (bg) subunit.

6. GTP binding and dissociation of the bg subunit causes the

alpha subunit to adopt a new conformation enabling it to now
bind to intracellular signaling proteins.
7. The bg subunit does not change conformation, but its
dissociation from the alpha exposes this face of the beta
subunit. It can now also interact with signaling molecules.

8. The cycle is repeated by the hydrolysis of subunit-bound GTP to GDP,

resulting in the re-association of the and subunits.