Target intelligence / Profile preview

Angiogenic endothelial cell surface receptors and extracellular matrix components

Molecular classification
Receptor tyrosine kinase, Integrin, Extracellular matrix protein, Cell adhesion molecule
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Overview

This target group encompasses a diverse array of proteins expressed on the surface of proliferating endothelial cells and within the remodeled extracellular matrix (ECM) during pathological angiogenesis. Key components include receptor tyrosine kinases like Vascular Endothelial Growth Factor Receptors (VEGFRs) and Tie-2, as well as adhesion molecules such as integrins (e.g., αvβ3). The ECM components, such as the extra-domain B (ED-B) of fibronectin and tenascin-C, are often specifically expressed in neovascularized tissues but are largely absent in normal adult tissues. These targets play a critical role in the formation of new blood vessels, which is essential for tumor growth, metastasis, and various ocular and inflammatory conditions. Therapeutic strategies targeting these molecules aim to inhibit blood supply to diseased tissues or utilize these markers for the site-specific delivery of imaging agents and cytotoxic drugs.

Other names
Angiogenesis-related targetsVascular endothelial targetsTumor vasculature markersNeovascular targets
02

Mechanism of action

Inhibition of ligand-receptor binding, inhibition of intracellular tyrosine kinase activity, disruption of cell-matrix adhesion, and antibody-mediated delivery of therapeutic payloads to the vasculature.

03

Biological functions

AngiogenesisCell adhesionSignal transductionCell migrationVascular permeabilityExtracellular matrix remodeling
04

Disease associations

CancerAge-related macular degenerationDiabetic retinopathyPsoriasisRheumatoid arthritis
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Safety considerations

HypertensionProteinuriaHemorrhageImpaired wound healingGastrointestinal perforationArterial thromboembolic events
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Interacting drugs

Bevacizumab

8 more in the full profile.

07

Biomarkers

Circulating VEGF levelsSoluble VEGFR-2 (sVEGFR2)Circulating endothelial cells (CECs)Dynamic contrast-enhanced MRI (DCE-MRI) parametersED-B fibronectin expression

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