摘要
血管生成是肿瘤生长、增殖和迁移必不可少的过程。血管内皮生长因子受体(VEGFR)作为影响血管生成的关键信号因子,已成为抗肿瘤药物研发的重要靶点。已证实VEGFR是肾细胞癌、胃肠道间质瘤、肝细胞癌、白血病等多种类型肿瘤的治疗靶点。该文综述了临床应用的14个VEGFR抑制剂及处于临床试验阶段VEGFR小分子抑制剂的研究进展,就其结构特征和临床适应证进行了总结,并阐述了未来VEGFR抑制剂的研究方向及面临的挑战。
Angiogenesis is a necessary stage in tumor growth,proliferation and migration.As a key signaling factor of angiogenesis,vascular endothelial growth factor receptor(VEGFR)has become a pivotal target for the development of antitumor drugs in the past two decades.VEGFR has proven to be a therapeutic target for many types of tumors,including renal cell carcinoma,gastrointestinal stromal tumor,hepatocellular carcinoma and leukemia.This article reviews the research progress in 14 VEGFR inhibitors in clinical applications and some potential small-molecule inhibitors in clinical trials recently published,summarizes its structural characteristics and clinical indications,and points out the main spheres of research on VEGFR inhibitors anol challenges in the future.
作者
杨婷婷
李鹏运
郑志兵
YANG Ting-ting;LI Peng-yun;ZHENG Zhi-bing(Institute of Pharmacology and Toxicology,Academy of Military Medical Sciences,Academy of Military Sciences,Beijing 100850,China)
出处
《军事医学》
CAS
2021年第5期390-396,共7页
Military Medical Sciences
基金
国家重大新药创制重大专项课题资助项目(2018ZX09J18102)。
关键词
血管内皮生长因子受体
抑制剂
新生血管
抗肿瘤药物
vascular endothelial growth factor receptor
inhibitor
angiogenesis
anti-cancer agent
