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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。
FMS-like tyrosine kinase 3 (FLT-3) is a type III receptor tyrosine kinase that is widely found in the blood, immune and nervous systems. FLT-3 gene mutations (internal tandem repeat mutations and kinase domain point mutations) and over-expression will lead to tumorigenesis, small molecule FLT-3 receptor tyrosine kinase inhibitors through the inhibition of cell proliferation signal conduction to promote tumor Apoptosis, which treat cancer disease. In this paper, the small molecule FLT-3 receptor tyrosine kinase inhibitors which have been listed or are in the clinical research stage in recent years are classified into four classes according to their structures, such as aromatic ureas, pyrimidinamines, indolocarbazoles and others, and their representatives Compound efficacy and clinical research progress.