Target intelligence / Profile preview

Platelet aggregation targets

Molecular classification
G protein-coupled receptor, Enzyme, Integrin, Cell adhesion molecule
01

Overview

Platelet aggregation targets encompass a diverse group of proteins and enzymes that regulate the activation and clumping of platelets, a process essential for hemostasis but also central to pathological thrombosis [ahajournals.org, 2015]. Key targets include the P2Y12 receptor, which mediates ADP-induced activation; Cyclooxygenase-1 (COX-1), which produces the pro-aggregatory mediator thromboxane A2; and the Glycoprotein IIb/IIIa (integrin αIIbβ3) receptor, which serves as the final common pathway for platelet-platelet bridging via fibrinogen [nih.gov, 2024]. Other significant targets include the protease-activated receptor 1 (PAR-1) for thrombin and the collagen receptor GPVI [nih.gov, 2024]. Drugs targeting these molecules, such as clopidogrel, aspirin, and abciximab, are cornerstones in the management of cardiovascular diseases like myocardial infarction and stroke [nih.gov, 2024]. While highly effective at preventing ischemic events, these therapies carry a significant risk of bleeding due to the systemic inhibition of normal clotting mechanisms [clinpgx.org, 2024].

Other names
Antiplatelet targetsPlatelet receptorsThrombotic targetsPlatelet activation targets
02

Mechanism of action

Cyclooxygenase-1 inhibition, P2Y12 receptor antagonism, Glycoprotein IIb/IIIa inhibition, and Protease-activated receptor 1 (PAR-1) antagonism.

03

Biological functions

Platelet aggregationHemostasisThrombosisCell adhesionSignal transduction
04

Disease associations

Cardiovascular diseaseMyocardial infarctionStrokeAcute coronary syndromePeripheral artery disease
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Safety considerations

Increased risk of major bleedingGastrointestinal hemorrhageIntracranial hemorrhageThrombocytopenia
06

Interacting drugs

Aspirin

7 more in the full profile.

07

Biomarkers

Light transmission aggregometryVerifyNow P2Y12 assayP-selectin expressionBleeding time

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