小分子血管内皮生长因子受体抑制剂的抗肿瘤研究进展

摘要

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.%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。