FLT3激酶抑制剂及其在急性髓系白血病治疗领域的研究进展

Advances in the research of FLT3 inhibitors for acute myeloid leukemia

急性髓系细胞白血病(AML)是成年人最常见的急性白血病,FMS样酪氨酸激酶3(FLT3)突变是AML中发现的第1个突变,其所引发的AML预后甚差。近年来,一些FLT3靶向抑制剂显示出了对体内FLT3信号通路传导的抑制,为AML的治疗提供了新途径。本文对FLT3激酶抑制剂,按结构分成吲哚酮类、吲哚并咔唑类、苯并咪唑/吡唑类、喹啉、喹喔啉和喹唑啉类、三环类、嘧啶类等共7类进行综述。

Acute myeloid leukemia （AML） is one of the most common acute leukemias in adults. Those patients with FLT3 mutations have a particularly poor prognosis. Recently, the emergence of a variety of targeted inhibitors has shown the capability of suppressing FLT3 signaling in vivo, which provided a new way to treat AML. In this paper, we reviewed those inhibitors based on their structures, which include indolone-related inhibitors, indolocarbazo-related inhibitors, benzimidazole/benzopyrazole-related inhibitors, quinoline/quinoxaline/quinazoline-related inhibitors, tricyclic inhibitors, pyrimidine-related inhibitors and others.