血管内皮细胞生长因子受体酪氨酸激酶抑制剂

Advances in VEGF Receptor Tyrosine Kinase Inhibitors

血管生成是人体肿瘤生长和转移的必要条件 ,抑制肿瘤细胞介导的血管生成已成为近年来寻找新型抗肿瘤药物的一个主要研究方向。血管内皮细胞生长因子 (VEGF)是体内活性最强、专属性最高的促血管生成因子 ,故成为寻找血管生成抑制剂的重要靶点 ,其中靶向 VEGF受体酪氨酸激酶的抑制剂令人最为关注。本文综述 VEGF及其受体酪氨酸酶抑制剂的研究进展 。

Angiogenesis is a fundamental process of tumor growth and metastasis, and thus inhibition of angiogenesis induced by tumors has become an important trend in research and development of novel antineoplastic drugs. The vascular endothelial growth factor (VEGF), known as the most potent and specific angiogenetic factor, represents an key target for the discovery of anti angiogenesis inhibitors. Receptor tyrosine kinase (RTK) inhibitors targeting VEGF receptor is one of the most promising agents. Recent developments of these inhibitors were reviewed, and their structure activity relationship was discussed.