小分子血管内皮细胞生长因子受体激酶抑制剂研究进展

Small molecule inhibitors of vascular endothelial cell growth factor receptor: research advances

血管内皮生长因子受体(VEGFR)属于蛋白酪氨酸激酶家族,其异常表达与肿瘤的发生、发展及预后密切相关。目前,以VEGFR为靶点的肿瘤治疗已成为抗肿瘤研究中十分活跃的领域之一。本文综述了已上市或正处于研究阶段的小分子VEGFR酪氨酸激酶抑制剂及其在肿瘤治疗中的应用。

Vascular endothelial growth factor receptor（VEGFR） is a member of protein tyrosine kinases family,whose abnor- mal expression is closely related to the occurence, development and prognosis of many kinds of malignant cancers. At present, direct and indirect involvement of VEGFR family in tumor growth, metastasis and apoptosis has made them one of the most promising targets for anticancer drug development and cancer therapy. This review summarizes the small-molecule inhibitors of VEGFR family tyrosine kinase in the clinical use or clinical trial stages, focusing on their roles in cancer therapy.