Tyrosine kinase with immunoglobulin-like and EGF-like domains receptor (TIE)

The Tie receptors, comprising TIE1 and TIE2 (also known as TEK), are a specialized family of receptor tyrosine kinases predominantly expressed on endothelial cells and hematopoietic stem cells. They serve as the primary signaling interface for angiopoietins (Ang1, Ang2, Ang3, and Ang4), playing a fundamental role in vascular development, maturation, and the maintenance of vessel integrity. TIE2 is the better-characterized member, where its activation by Ang1 promotes vessel stability and survival, while Ang2 often acts as a context-dependent antagonist that facilitates vascular remodeling and permeability in the presence of inflammatory stimuli. In disease states, dysregulation of the Tie-Angiopoietin pathway is a hallmark of pathological angiogenesis in cancer and vascular leakage in retinal diseases like diabetic macular edema. Modern therapeutic approaches target this pathway through bispecific antibodies that neutralize Ang2 or small molecules that inhibit the kinase activity of the receptors to disrupt tumor blood supply.

Other names

Angiopoietin receptorTEK tyrosine kinaseTIE1TIE2CD202BTunica interna endothelial cell kinase

TIE2 activation (agonism) to promote vascular stability; TIE2 inhibition (antagonism) to suppress tumor angiogenesis; Angiopoietin-2 (Ang2) neutralization to prevent vascular leakage; VE-PTP inhibition to indirectly activate TIE2.