Target intelligence / Profile preview

Tyrosine-protein kinase Tie-2 (Tie2)

Target
Tie2
Molecular classification
Receptor tyrosine kinase, Enzyme, Receptor, Cell surface protein
01

Overview

Tyrosine-protein kinase Tie-2 is an endothelial-specific receptor tyrosine kinase encoded by the *TEK* gene. Located at the endothelial cell surface, Tie-2 binds the angiopoietins (primarily angiopoietin-1 and angiopoietin-2), which regulate its activation. Ligand engagement induces Tie2 dimerization and clustering, leading to autophosphorylation and activation of intracellular signaling cascades essential for blood vessel maturation, stabilization, and maintenance of vascular integrity. Dysregulation of Tie-2 signaling contributes to pathologies such as tumor angiogenesis, inflammatory vascular leakage, and primary congenital glaucoma. Therapeutic targeting of Tie-2 focuses on modulating angiopoietin binding or blocking its kinase activity to influence vascular remodeling in disease contexts[1][3][6][8].

Other names
TEK (gene name)Tunica interna endothelial cell kinaseTyrosine kinase with immunoglobulin-like and EGF-like domains 2
02

Biological functions

Signal transductionBlood vessel maturation and remodelingAngiogenesisEndothelial cell survivalVascular integrityCell proliferation
03

Disease associations

CancerCardiovascular diseaseInflammationVascular leakage (e.g., sepsis)Primary congenital glaucomaTumor angiogenesis
04

Safety considerations

Impaired vascular integrity (risk of edema, hemorrhage)Disruption of normal angiogenesis and vessel maintenanceRisk of hypertension or cardiovascular effectsOff-target effects on other tyrosine kinases
05

Interacting drugs

Trebananib (AMG 386)

4 more in the full profile.

06

Biomarkers

Tie2 phosphorylation status in endothelial cellsPlasma angiopoietin levels (especially Ang1 and Ang2)TEK gene variants (e.g., in congenital glaucoma)Endothelial Tie2 expression in tumor vasculature

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