Platelet Activating GPCR Signaling

alpha-2 Adrenergic R
P2Y12
alpha-2 Adrenergic R
P2Y12
Lyn
Lyn
Fyn
Fyn
G alpha i
G alpha i
Adenylyl Cyclase
Adenylyl Cyclase
cAMP
cAMP
PKA
PKA
Granule
Release
Granule
Release
PAR1,3,4
Thromboxane A2 R
PAR1,3,4
Thromboxane A2 R
Fyn
Fyn
G alpha 12,13
G alpha 12,13
G alpha q
G alpha q
p115 RhoGEF
p115 RhoGEF
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RhoA
RhoA
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Granule
Release
Granule
Release
ROCK
ROCK
Myosin LC
Phosphatase
Myosin LC
Phosphatase
PLC-beta
PLC-beta
PLC-gamma
PLC-gamma
IP3
IP3
DAG
DAG
Calcium Release
Calcium Release
PKC alpha
PKC beta
PKC alpha
PKC beta
CalDAG-GEFI
CalDAG-GEFI
Granule
Release
Granule
Release
Rap1B
Rap1B
RIAM
RIAM
Integrin
Activation
Integrin
Activation
Lyn
Lyn
Fyn
Fyn
5-HT2A
P2Y1
5-HT2A
P2Y1
G alpha q
G alpha q
G alpha 12,13
G alpha 12,13
Fyn
Fyn
PI 3-Kinase
PI 3-Kinase
Rap1B
Rap1B
Integrin
Activation
Integrin
Activation
MAPK
MAPK
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PLA2G4A
PLA2G4A
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Thromboxane Synthase
Thromboxane Synthase
Thromboxane A2
Production
Thromboxane A2
Production

Overview of Platelet Signaling Through Activating GPCRs

G protein-coupled receptors (GPCR) enahance platelet activation in response to 5-HT (serotonin), the purines ADP and ATP, prostaglandin E2, thromboxane A2, adenosine, norepinephrine, and thrombin. GPCR signaling leads to the activation of G proteins, Src familiy kinases, PKC, and PI-3 Kinase. GPCR signaling induces platelet granule release, integrin activation, and production of thromboxane A2. Pharmacologic blockade of the P2Y12 receptor is a key component of anti-thrombotic treatment.

Platelet Activating GPCR Signaling background image 1