Luo Yan, Wei Yu-quan
National Key Laboratory of Biotherapy, Cancer Center, West China Hospital, Sichuan University, Chengdu, Sichuan 610041, P.R.China.
Zhonghua Yi Xue Yi Chuan Xue Za Zhi. 2006 Feb;23(1):63-6.
Angiopoietins(ANGPT) and their endothelial cell-specific tyrosine kinase receptors TEK are the major regulators of blood vessels angiogenesis under physiological and pathologic conditions. ANGPT1 is essentially involved in maturation, stabilization, and remodeling of blood vessels through inducing TEK autophosphorylation, promoting endothelial cell migration and survival. Instead, ANGPT2 appears to act as a natural antagonist of ANGPT1, it can activate vascular remodeling with the presence of vascular endothelial growth factor(VEGF) or regress frank blood vessels under the absence of VEGF. High expression of angiopoietins and TEK is often detected in tumor tissues. Many studies showed that disrupting the ANGPT/TEK receptor pathway could inhibit the growth of a number of murine tumors and human tumors. Thus, it is possible that inhibitors targeting the ANGPT/TEK pathway will have broad clinical utility to treatment of cancer.
血管生成素（ANGPT）及其内皮细胞特异性酪氨酸激酶受体TEK是生理和病理条件下血管生成的主要调节因子。ANGPT1主要通过诱导TEK自身磷酸化、促进内皮细胞迁移和存活，参与血管的成熟、稳定和重塑。相反，ANGPT2似乎是ANGPT1的天然拮抗剂，在血管内皮生长因子（VEGF）存在的情况下，它可以激活血管重塑，而在没有VEGF的情况下，它可以使成熟血管退化。在肿瘤组织中经常检测到血管生成素和TEK的高表达。许多研究表明，破坏ANGPT/TEK受体途径可以抑制多种小鼠肿瘤和人类肿瘤的生长。因此，靶向ANGPT/TEK途径的抑制剂有可能在癌症治疗中具有广泛的临床应用价值。
