Targeting the ANGPT-TIE2 pathway in malignancy.
Angiopoietins (ANGPTs) are ligands of the endothelial cell receptor TIE2 and have crucial roles in the tumour angiogenic switch. Increased expression of ANGPT2 relative to ANGPT1 in tumours correlates with poor prognosis. The biological effects of the ANGPT-TIE system are context dependent, which brings into question what the best strategy is to target this pathway. This Review presents an encompassing picture of what we know about this important axis in tumour biology. The various options for therapeutic intervention are discussed to identify the best path forwards.
Huang
Hanhua
H
CovX, Pfizer Inc., San Diego, CA 92121, USA.
Bhat
Abhijit
A
Woodnutt
Gary
G
Lappe
Rodney
R
D042682:Angiopoietins / Q000037:antagonists & inhibitors* / Q000502:physiology; D000818:Animals; D006801:Humans; D007249:Inflammation / Q000209:etiology; D042583:Lymphangiogenesis; D009362:Neoplasm Metastasis; D009369:Neoplasms / Q000098:blood supply / Q000188:drug therapy*; D009389:Neovascularization, Pathologic / Q000209:etiology; D042787:Receptor, TIE-2 / Q000037:antagonists & inhibitors* / Q000502:physiology; D015398:Signal Transduction / Q000187:drug effects*; D042461:Vascular Endothelial Growth Factor A / Q000037:antagonists & inhibitors
D042682:Angiopoietins; D042461:Vascular Endothelial Growth Factor A; D042787:Receptor, TIE-2