肿瘤血管生成抑制剂  

Tumor Angiogenesis Inhibitors

作　　者：董缙[1] 姚硕蔚[1] 徐云根[1] 

机构地区：[1]中国药科大学药物化学教研室,南京210009

出　　处：《化学进展》2010年第10期1993-2002,共10页Progress in Chemistry

基　　金：教育部留学回国人员科研启动基金资助项目(2007);江苏省高校"青蓝工程"资助项目(2008)

摘　　要：肿瘤血管生成的药物治疗是当前有关肿瘤的热点研究领域,目前已经有数种肿瘤血管生成抑制剂上市。肿瘤血管生成抑制剂能够抑制肿瘤的生长和转移,甚至使肿瘤消退,此类药物的研究开发可为肿瘤患者提供高效、低毒且抗瘤谱更广的药物。本文综述了近年来血管生成抑制剂的研究进展,首先介绍了间接血管生成抑制剂,此类药物中作用于血管内皮细胞生长因子受体信号通路的药物是目前最成功的一类血管生成抑制剂;其次介绍了直接血管生成抑制剂,使用这类药物更有可能避免间接抑制剂所引起的血管生成援救反应;然后在其他途径肿瘤血管生成抑制剂部分,本文详细介绍了作用机制尚不明确的沙利度胺及其衍生物;最后,本文分析讨论了这类药物开发所遇到的一些问题,如抗血管生成治疗新理论的挑战和耐药性等,并指出了未来发展方向。At present,drug inhibition of angiogenesis has become a hot topic in the treatment of tumor and several tumor angiogenesis inhibitors （TAIs） have been marketed. TAIs can suppress tumor growth and metastasis, and even induce tumor regression. Research and development on TAIs holds the promise of supplying drugs with high potency,low toxicity and broad-spectrum antitumor activity for tumor patients. This review summarizes recent research progress in TAIs. First of all,indirect TAIs are introduced. Among indirect TAIs,VEGF inhibitors are the most successful TAIs currently. Secondly,direct TAIs,which are unlikely switch on the angiogenic rescue program,are introduced. Thirdly, in the miscellaneous TAIs part, thalidomide and its derivatives, whose mechanisms of activity have not been defined well,are described in detail. Finally,several problems encountered in the research and development of TAIs,such as challenge from novel theory of anti-angiogenenic therapy and resistance,are analyzed and discussed,and future research directions are pointed out.

关 键 词：肿瘤 血管生成抑制剂 VEGF 贝伐单抗 

分 类 号：Q5[生物学—生物化学] TQ46[化学工程—制药化工]