Target intelligence / Profile preview

Integrin alpha-V beta3 (αVβ3)

Target
αVβ3
Molecular classification
Integrin, Cell Surface Receptor
01

Overview

Integrin αVβ3 is a heterodimeric cell surface receptor composed of αV and β3 subunits. It mediates cell adhesion to the extracellular matrix via RGD motifs, primarily found in vitronectin, fibronectin, fibrinogen, laminin, thrombospondin, vWF, osteopontin and tenascin. It plays a critical role in angiogenesis, bone resorption, and cell signaling, and is implicated in cancer, cardiovascular disorders, and autoimmune diseases. It is a target for antiangiogenic therapies.

Other names
Integrin αVβ3alphaVbeta3 integrinVitronectin receptor
02

Mechanism of action

αVβ3 antagonists inhibit angiogenesis by blocking the interaction of αVβ3 with ECM proteins and growth factors, leading to reduced endothelial cell proliferation, migration, and survival. Some antagonists, like ProAgio, induce apoptosis by recruiting caspase 8 to the receptor.

03

Biological functions

Cell adhesionSignal transductionAngiogenesisBone resorptionCell migrationCell proliferationCell survivalPhagocytosis
04

Disease associations

CancerCardiovascular disordersAutoimmune diseases
05

Safety considerations

Potential for off-target effects due to RGD sequence similarity in other integrinsThrombocytopenia (due to interaction with platelet αIIbβ3)
06

Interacting drugs

Etaracizumab (Vitaxin)

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