小分子Fms样酪氨酸激酶3抑制剂的研究进展

Advances in Research on Small-molecule Fms-like Tyrosine Kinase 3 Inhibitors

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。

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.