《生命科学》 2007, 19(4):

肿瘤血管靶向药物的研究进展

任　萱，孙启明，林莉萍，丁 健^*

(中国科学院上海生命科学研究院上海药物研究所新药研究国家重点实验室，上海201203)

摘　要：

摘　要：肿瘤血管在实体瘤的发生发展中具有重要的作用，靶向肿瘤血管的新药研发已成为一个热点领域。抗肿瘤血管的治疗策略分为肿瘤新生血管生成抑制剂(tumor angiogenesis inhibitor, TAI)和肿瘤血管靶向药物(vascular targeting agents, VTAs)两方面的研究。肿瘤新生血管生成抑制剂旨在抑制肿瘤新生血管生成的过程，而肿瘤血管靶向药物则是通过快速而有选择性地破坏肿瘤血管功能，使肿瘤血供受阻，导致肿瘤坏死。 VTA类药物分为两类：一是小分子抑制剂(small molecule agents)，利用肿瘤血管和正常组织血管存在的差别选择性地破坏肿瘤血管；另一种是生物制剂(biological agents)，借助能够特异结合肿瘤血管的配体将毒素、凝血诱导剂、凋亡诱导分子等运送到肿瘤血管, 引起血管阻塞使肿瘤坏死。
关键词：肿瘤血管靶向药物；新生血管生成抑制剂；小分子VTAs；生物类VTAs
中图分类号：R978.7　　文献标识码：A

Tumor vascular targeting agents

REN Xuan, SUN Qiming, LIN Liping, DING Jian^*

(State Key Laboratory of Drug Reasearch, Shanghai Insititue of Meteria Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai201203, China)

Abstract:

Abstract: The tumor vasculature plays a critical role in the survival and continued growth of solid tumor masses, which make it a valuable target for cancer therapy. Two pharmacological strategies invovled in this field were tumor angiogenensis inhibitors (TAIs) and vascular targeting agents (VTAs). The former aimed to inhibit the processes of neo-vasculature from the pre-existed tumor blood, the latter induce a rapid and selective vascular shutdown in tumors so that the blood flow is arrested and tumor cell dead due to the resulting oxygen and nutrient deprivation and buildup of waste products occurs. VTAs are divided into two main classes, small molecule agents and biological agents. The small molecule agents exploit the physiological differences between tumor and normal tissue endothelium to disrupt the tumor blood vessel selectively; the biological agents use a targeting ligand to achieve selectivity of binding to and occluding tumor vasculature.
Key words: vascular targeting agents (VTAs); tumor angiogenensis inhibitors (TAIs); small molecule agents; biological agents