Target intelligence / Profile preview

Platelet glycoprotein VI receptor (GPVI)

Target
GPVI
Molecular classification
Receptor, Immunoglobulin superfamily member, Platelet collagen receptor
01

Overview

The Platelet glycoprotein VI receptor (GPVI) is a transmembrane glycoprotein expressed exclusively on platelets and their precursor megakaryocytes. It is the primary receptor responsible for collagen-induced platelet activation, which is a key event in hemostasis and pathological thrombosis following vessel injury or rupture of atherosclerotic plaques. Structurally, GPVI is a member of the immunoglobulin superfamily, consisting of two extracellular Ig-like domains that bind collagen, a mucin-like stalk, a transmembrane region, and a cytoplasmic tail. GPVI signals via an associated Fc receptor γ-chain (FcRγ) that contains an immunoreceptor tyrosine-based activation motif (ITAM), activating a tyrosine kinase cascade leading to platelet activation and thrombus formation. It is recognized as a promising antithrombotic drug target since its inhibition reduces thrombus formation with relatively limited effects on baseline hemostasis compared to other antiplatelet therapies.

Other names
Glycoprotein VICollagen receptor GPVIGP6 (gene symbol)CD36L1 (less common)GPVI-Fc (therapeutic fusion protein)
02

Mechanism of action

Inhibition of collagen-induced platelet activation Blockade of GPVI-collagen binding Prevention of thrombus formation

03

Biological functions

Platelet activationSignal transductionHemostasis and thrombosisPlatelet adhesion and aggregation
04

Disease associations

Cardiovascular disease (myocardial infarction, ischemic stroke, atherothrombosis, thrombosis)Bleeding disorders (rare, in congenital deficiency of GPVI)Inflammation (via platelet activation)Other (possible roles in immune modulation but less central)
05

Safety considerations

Increased bleeding risk (especially with potent GPVI inhibition, though less than some other antiplatelet drugs)Mild bleeding disorder (in congenital or acquired GPVI deficiency)Immunological reactions to biologics (e.g., anti-GPVI antibodies)
06

Interacting drugs

Revacept (a soluble GPVI fusion protein/GPVI-Fc, in clinical trials)

2 more in the full profile.

07

Biomarkers

Surface expression levels of GPVI on platelets (measured for bleeding tendency or platelet reactivity)Platelet activation markers (e.g., P-selectin expression)Plasma soluble GPVI (marker of platelet activation/shedding)

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