Target intelligence / Profile preview

Glycoprotein VI (collagen receptor) (GPVI)

Target
GPVI
Molecular classification
Receptor, Immunoglobulin superfamily (for GPVI), Integrin family (for α2β1), Platelet membrane glycoprotein
01

Overview

Glycoprotein VI (GPVI) is a platelet-specific membrane receptor and major component of the platelet response to collagen exposure during vascular injury. GPVI is a member of the immunoglobulin superfamily and associates with the Fc receptor gamma chain, which carries an ITAM motif essential for downstream tyrosine kinase signaling[4][5]. Collagen binding to dimeric GPVI activates this pathway, leading to platelet activation, aggregation, and thrombus formation[2][5][7]. Integrin α2β1 plays a complementary role in mediating platelet adhesion but not activation. Variations in GPVI expression can influence thrombosis risk and bleeding disorders, making it a central therapeutic and diagnostic target in platelet biology[1][5][7].

Other names
Platelet collagen receptorGlycoprotein VIGPVIIntegrin α2β1 (secondary/adhesive collagen receptor)Collagen receptor of plateletsCD36 and the GPIIb/IIIa do not serve as signaling collagen receptors in platelets
02

Mechanism of action

Drugs/inhibitors block GPVI-collagen interaction to prevent platelet activation - Inhibition of ITAM phosphorylation and downstream tyrosine kinase signaling - Preventing GPVI dimerization or signalling blocks thrombus formation

03

Biological functions

Platelet activationSignal transductionAdhesion to collagenThrombus formation (thrombogenesis)Hemostasis
04

Disease associations

Cardiovascular disease (thrombosis, myocardial infarction, stroke)InflammationCancer metastasisAutoimmune diseases (involvement suggested via platelet activation)Other: bleeding disorders when mutated or absent
05

Safety considerations

Excessive inhibition may increase bleeding risk (impaired hemostasis)Patient variability due to GPVI and integrin polymorphismsDifficulty targeting GPVI without affecting essential platelet functions
06

Interacting drugs

Experimental inhibitors/antagonists of GPVI

2 more in the full profile.

07

Biomarkers

GPVI expression level (as a marker for platelet function)GPVI dimerization status (active form during thrombosis)

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