FLT-3受体酪氨酸激酶抑制剂的研究进展

FMS样酪氨酸激酶3 (FLT-3)是Ⅲ型受体酪氨酸激酶的一种，广泛存在于血液系统、免疫系统和神经系统中。FLT-3基因突变（内部串联重复突变和激酶区的点突变）以及过度表达将会导致肿瘤的发生，小分子FLT-3受体酪氨酸激酶抑制剂通过阻断细胞增殖信号的传导促使肿瘤细胞凋亡，从而对肿瘤疾病进行治疗。文中对近年来已上市或处于临床研究阶段的小分子FLT-3受体酪氨酸激酶抑制剂按结构分成芳香脲、嘧啶胺、吲哚并咔唑及其他共4类，并简要介绍其代表化合物的药效及临床研究进展。

Advances in the inhibitors of FLT-3 receptor tyrosine kinase

The FMS-like tyrosine kinase-3(FLT-3) is one of the class III receptor tyrosine kinases. FLT-3 is widely expressed in hematopoietic, immune and neural systems. The mutations (internal tandem duplication and point mutations in the tyrosine kinase domain) or its excessive expression can induce the tumor. Small molecular FLT-3 inhibitors are effective in the treatment of the tumor by blocking the conduction of the cell proliferation signals and accelerating the tumor cell apoptosis. Several small molecular FLT-3 inhibitors have been launched or are in the clinical stages. In this review, we described the classification based on their structures, which include four kinds: aryl ureas, pyrimidinamines, indolocarbazoles and others. Pharmacodynamics and results in clinical studies of some representative compounds are also introduced.