小分子fms 样酪氨酸激酶3 抑制剂的研究进展 - 药学进展.pdf

PROGRESS IN PHARMACEUTICAL SCIENCES 2016,40 1 :11-19 ( ) 11 小分子 Fms 样酪氨酸激酶 3 抑制剂的研究进展 田皓中 , 施志浩 , 陆涛 * （中国药科大学理学院 , 江苏 南京 211198） [ 摘要 ] Fms 样酪氨酸激酶 3（FLT3）是一种重要的Ⅲ型受体酪氨酸激酶，对造血细胞和淋巴细胞的增殖起关键作用，其突变以及过度表 达是造成多种恶性肿瘤的关键因素。通过外源性抑制剂阻断细胞增殖信号的传导来促使肿瘤细胞凋亡是当前治疗肿瘤的重要手段。FLT3 小 分子抑制剂作为一类重要的外源性受体酪氨酸激酶抑制剂已应用于多种恶性肿瘤的治疗并引起广泛关注。综述近 5 年来 FLT3 小分子抑制剂 的研究进展。 [ 关键词 ] FLT3；抗肿瘤；受体酪氨酸激酶抑制剂；白血病 [ 中图分类号 ] R914.4; R979.1 [ 文献标志码 ] A [ 文章编号 ] 1001-5094（2016）01-0011-09 Advances in Research on Small-molecule Fms-like Tyrosine Kinase 3 Inhibitors TIAN Haozhong, SHI Zhihao, LU Tao (School of Science, China Pharmaceutical University, Nanjing 211198, China) [Abstract] Fms-like tyrosine kinase 3 (FLT3) is an important member of the class III receptor tyrosine kinase (TK) family, which promotes proliferation of hematopoietic cells and lymphocytes. The mutation and overexpression of FLT3 are major reasons for various malignancies. Blocking the transduction of proliferation signal by exogenous inhibitors to promote apoptosis of tumor cells emerges as an effective strategy for cancer therapy. As a group of important exogenous inhibitors of receptor tyrosine kinase, small molecule FLT3 inhibitors have been applied in the treatment of multiple malignancies and drawn extensive attention. The advances in research on FLT3 inhibitors in the past 5 years were reviewed in this paper. [Key words] FLT3; anti-tumor; receptor tyrosine kinase inhibitor; leukemia Fms 样酪氨酸激酶 3（FLT3），在小鼠中也称作胎 含有 ATP 的结合位点的柔性激酶插入结构域所组成 [1] 肝激酶 2（FLK2），其与干细胞生长因子受体（