Target intelligence / Profile preview

Tyrosine kinase with Immunoglobulin-like and EGF-like domains 2 (Tie2)

Target
Tie2
Molecular classification
Receptor, Receptor Tyrosine Kinase
01

Overview

Tie2, also known as the angiopoietin-1 receptor, CD202B, or tyrosine-protein kinase receptor TEK, is a receptor tyrosine kinase primarily expressed on vascular endothelial cells. It plays a central role in blood vessel maturation, stability, and remodeling by mediating signals from its ligands—the angiopoietins. Activation by Ang1 or high concentrations of Ang2 stimulates PI3K-Akt pathway leading to eNOS phosphorylation, nitric oxide production, enhanced cell survival, vascular quiescence, and angiogenesis. It is critical for vascular stability and endothelial cell-smooth muscle communication during venous morphogenesis. Defects in the TEK gene are associated with inherited venous malformations. In cancer patients, subpopulations of monocytes expressing Tie2 contribute to tumor neovascularization.

Other names
Angiopoietin-1 receptorTEKCD202B
02

Mechanism of action

Inhibition or modulation of the ANGPT/Tie2 pathway.

03

Biological functions

AngiogenesisVascular stabilityEndothelial cell survivalVessel maturationVessel remodelingEndothelial cell-smooth muscle communication
04

Disease associations

Venous malformationsTumor neovascularizationCancer
05

Safety considerations

Potential for off-target effects due to the involvement of Tie2 in normal vascular function.Development of resistance to anti-angiogenic therapies.

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