The ANG receptors TIE1 and TIE2 (also known as TEK), which were discovered 25 years ago, form a small subfamily of growth factor receptor tyrosine kinases. TIE1 and TIE2 are almost exclusively expressed in the endothelium, but there is some expression also in haematopoietic cells the angiopoietin (ANG)–TIE signalling pathway has emerged as an attractive vascular drug target. The ANG–TIE pathway is required for lymphatic and blood vessel development during mid-gestation, and this pathway controls vascular permeability, inflammation and pathological angiogenic responses in adult tissues. Investigational drugs that target the ANG–TIE pathway are expected to complement current anti-angiogenic strategies in the treatment of cancer and neovascular eye diseases in the future. The ANG–TIE pathway has a unique role in the control of vascular stability. Manipulation of this axis may thus be beneficial in conditions in which excess vessel growth is not a problem but vascular stabilization is crucial, such as in diabetic vascular complications, sepsis, organ transplantation and atherosclerosis.

References

1.Saharinen P,et al. Nat Rev Drug Discov. 2017 Sep;16(9):635-661.