小分子血管内皮生长因子受体抑制剂的抗肿瘤研究进展  

Recent advance of small molecular VEGFR-2 inhibitors for cancer treatment

作　　者：郭子煜[1] 刘兆鹏[1] 

机构地区：[1]山东大学药学院药物化学研究所化学生物学教育部重点实验室,山东济南250012

出　　处：《中国生化药物杂志》2015年第6期176-180,共5页Chinese Journal of Biochemical Pharmaceutics

摘　　要：血管内皮生长因子受体(vascular endothelial growth factor receptor,VEGFR)属于受体型酪氨酸激酶超家族,在肿瘤血管生成中发挥重要作用。异常活化的血管内皮生长因子(vascular endothelial growth factor,VEGF)可诱发包括癌症在内的众多疾病,其主要受体VEGFR-2是血管生成的关键性信号转导受体,已成为治疗肿瘤的最有效靶点之一。如今,靶向抑制VEGFR-2的抗血管生成治疗已成为癌症治疗最有效的临床策略。本文根据结构特征分类,简要介绍了这几类结构中代表性的小分子VEGFR-2抑制剂的生物活性和临床研究进程。Vascular endothelial growth factor receptors （ VEGFR ） belong to the receptor-type tyrosine kinase （ RTK ） super family and play important roles in tumor angiogenesis.Abnormal activation of VEGFR results in several disorders including cancer.VEGFR-2 is the major signal transducer for angiogenesis, and therefore, it becomes a good target for the inhibition of tumor development and metastasis.Nowadays, the VEGFR-based antiangiogenic therapy becomes one of the most powerful clinical strategies for cancer treatment.In this review, small molecular VEGFR-2 inhibitors are classified according to their structural features, their biological activities and current statue are briefly introduced.

关 键 词：抗肿瘤 抗血管生成 抑制剂 血管内皮生长因子 血管内皮生长因子受体 血管内皮生长因子受体-2 

分 类 号：R979.1[医药卫生—药品]