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G-protein coupled

receptors
G-protein composed of one
alpha, beta, and gamma
subunit
2 primary signaling
cascades: cAMP or
phosphatidylinositol
pathways
Cell
membrane


Pathway activated depends
GDP
on alpha subunit type
(Gs, Gi/o, Gq/11,
G12/13)
PicScience GDP bound to when
G-protein coupled
receptors
When a ligand binds, the receptor
changes conformation, allowing G-
protein to be activated (GDP is
exchanged for GTP)
G-protein dissociates from receptor
then subunits from each other.

Cell
membrane


GTP
GDP

GTP
cAMP pathway
Gs binds to Adenylate Cyclase
(AC) and stimulates cAMP
synthesis from ATP
Gi/o binds to AC and inhibits
cAMP synthesis

AC Cell
membrane
cAMP

GTP
GDP
ATP
GTP
Phosphatidylinositol
pathway
Gq/11 binds to Phospholipase C
(PLC) and catalyzes the cleavage of
phosphatidylinositol 4,5-
biphosphate (PIP2) into the second
messengers inositol (1,4,5)
trisphosphate (IP3) and
diacylglycerol (DAG).

PIP DAG
2
PLC P
P
IP3
GTP
GDP
P
GTP

To sarcoplasmic
6 Major classes of these
Class A (or 1) (Rhodopsin-like)
Class B (or 2) (Secretin receptor
family)
Class C (or 3) (Metabotropic
glutamate/pheromone)
Class D (or 4) (Fungal mating
pheromone receptors)
Class E (or 5) (Cyclic AMP
receptors)
Class F (or 6)
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