阿帕替尼抗肿瘤机制的研究进展

Research Progress in Anti-Tumor Mechanisms of Apatinib

阿帕替尼是一种靶向血管内皮生长因子受体2(VEGFR2)的口服小分子酪氨酸激酶抑制剂,在多种肿瘤的临床治疗中表现出一定的疗效。近年来,在针对胃癌、白血病、胆管细胞癌、肝细胞癌、非小细胞肺癌、结肠癌的体内外实验中阿帕替尼均显示了较强的抗瘤活性。它可以通过抑制VEGFR2,调节下游磷脂酶Cγ1/细胞外信号调节激酶1/2、磷脂酰肌醇-3-激酶/蛋白激酶B/哺乳动物雷帕霉素靶蛋白等多条信号通路,抑制肿瘤血管生成,阻止肿瘤细胞的增殖、侵袭和转移,诱导肿瘤细胞凋亡,发挥抗肿瘤作用。该药应用于部分肿瘤的研究仍集中于细胞实验及少数动物实验,仍需更深入的分子机制方面的研究及更多临床回顾性、前瞻性研究来验证其临床疗效。

Apatinib is an oral small molecule tyrosine kinase inhibitor targeting vascular endothelial growth factor receptor 2(VEGFR2),which has shown efficacy in the clinical treatment of gastric carcinoma,leukemia,cholangiocarcinoma ,hepatocellular carcinoma, non-small-cell lung cancer and colonic carcinoma.Recently,apatinib showed strong anti-tumor activity in several in vivo and in vitro researches of different tumors.It can play an anti-tumor effect by inhibiting the VEGFR2 ,regulating downstream signaling pathways such as phospholipase Cγ1-extracellular signal-regulated kinase 1/2,phosphatidylinositol-3-kinase/protein kinase B-mammalian target of rapamycin blocking tumor angiogenesis,inhibiting proliferation ,metastasis and invasion and inducing apoptosis of the tumor cells.Recently,studies of the drug are still focused on cell experiments and a few animal experiments.Further research on the molecular mechanisms and large-scale retrospective and prospective clinical studies are needed to verify the clinical efficacy.