Inhibiting the Inhibitor: Targeting Vascular Endothelial Protein Tyrosine Phosphatase to Promote Tumor Vascular Maturation
Menée in vitro, à l'aide de poissons-zèbres et de modèles murins, cette étude évalue l'effet d'un composé appelé AKB-9778, un inhibiteur de l'enzyme VE-PTP, sur la structure du réseau vasculaire tumoral et le processus métastatique
A landmark article by Goel et al. entitled “Effects of Vascular-Endothelial Protein Tyrosine Phosphatase Inhibition on Breast Cancer Vasculature and Metastatic Progression” is included in this issue of the Journal. In this study, the investigators tested the effects of AKB-9778, a novel, potent, and selective inhibitor of vascular endothelial protein tyrosine phosphatase (VE-PTP), on tumor growth and angiogenesis. VE-PTP (also known as PTPRB, HPTP
β, or RPTPβ) was only recently identified as an important player in the molecular regulation of angiogenesis, and in this regard it provides a new therapeutic target in our assault on tumor angiogenesis. VE-PTP
’s role in the endothelium has been linked most closely to its ability to selectively dephosphorylate and inactivate Tie2, a receptor tyrosine kinase expressed primarily on endothelial cells (ECs)...
Journal of the National Cancer Institute , éditorial, 2013