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Interactive Pathways & Processes

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Platelet Activating GPCR Signaling

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alpha-2 Adrenergic R
P2Y12

Lyn

Fyn

G alpha i

Adenylyl Cyclase

cAMP

PKA

Granule
Release

PAR1,3,4
Thromboxane A2 R

Fyn

G alpha 12,13

G alpha q

p115 RhoGEF

RhoA

Granule
Release

ROCK

Myosin LC
Phosphatase

PLC-beta

PLC-gamma

IP₃

DAG

Calcium Release

PKC alpha
PKC beta

CalDAG-GEFI

Granule
Release

Rap1B

RIAM

Integrin
Activation

Lyn

Fyn

5-HT2A
P2Y1

G alpha q

G alpha 12,13

Fyn

PI 3-Kinase

Rap1B

Integrin
Activation

MAPK

PLA2G4A

Thromboxane Synthase

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.

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