Tie2 receptor (also known as Tyrosine-protein kinase receptor Tie-2) (Tie2)

The Tie2 receptor is a receptor tyrosine kinase on vascular endothelial cells, essential for vascular development, stability, and quiescence[1][2][5][6]. Its principal ligands are Angiopoietin-1 (agonist) and Angiopoietin-2 (contextual antagonist/agonist), which modulate vessel integrity, inflammatory responses, and endothelial barrier function. Tie2 is critical during embryonic vascular development and in maintaining adult vascular homeostasis[2][3][5]. Dysregulation of the Tie2 pathway is involved in pathological angiogenesis, vascular leak syndromes, and inflammation associated with diseases such as cancer, retinal diseases, and critical illness (like sepsis)[1][2][3][6]. Drugs targeting the Tie2 pathway can restore endothelial stability, reduce vascular leakage, and modulate inflammation, but carry risks related to the balance of vessel stability and remodeling[2][6].

Other names

TEK (gene symbol)Tyrosine kinase with immunoglobulin-like and EGF-like domains 2CD202B

Agonism or activation of Tie2 receptor (restoring endothelial stability and reducing permeability) - Inhibition of upstream inhibitors (VE-PTP inhibitors increase Tie2 phosphorylation/activity) - Ang2 antagonism (blocking competitive inhibition of Tie2 by Ang2) - Ligand sequestration (trapping excess Ang1/2 to modulate pathway)