摘要
急性髓系白血病(acute myeloid leukemia,AML)是原始和幼稚髓性细胞在骨髓、外周血和其他组织中异常增殖或积聚,导致正常造血功能受损的一种基因异质性疾病。研究表明,大约30%的AML患者体内存在FMS样酪氨酸激酶3(FMS-like tyrosine kinase 3,FLT3)激活突变,FLT3的异常调节与AML的发生及发展密切相关。FLT3已经成为开发小分子靶向药物的重要靶点,截至目前,以FLT3为靶点开发出来了多种FLT3抑制剂和FLT3降解剂,相关化合物表现出较好的抗AML活性。本文总结了以FLT3为靶点的AML治疗药物的研究进展,以期为AML药物研发和设计提供参考。
Acute myeloid leukemia(AML)is a genetic heterogeneous disease in which primordial and juvenile myeloid cells proliferate or accumulate abnormally in bone marrow,peripheral blood and other tissues,resulting in damage to normal hematopoietic function.Studies have shown that about 30% of AML patients have FMS-like tyrosine kinase 3(FLT3),FLT3 abnormal regulation is closely related to the occurrence and development of AML.At present,FLT3 has become an important target for developing small molecular targeted drugs.Currently,a variety of FLT3 inhibitors and FLT3 degraders have been developed targeting FLT3,and some compounds have exhibited good anti-AML activity.This article summarizes and sorts out the current mainstream drugs for AML therapeutic targeting FLT3,in order to provide a reference for the development and design of AML drugs.
作者
贾会亚
杨波
张晓梦
弓建红
吴亚
支燕乐
JIA Hui-ya;YANG Bo;ZHANG Xiao-meng;GONG Jian-hong;WU Ya;ZHI Yan-le(Henan University of Chinese Medicine,Zhengzhou 450000,China)
出处
《药学学报》
CAS
CSCD
北大核心
2023年第3期605-615,共11页
Acta Pharmaceutica Sinica
基金
国家自然科学基金青年基金(82003566)
河南省科技攻关资助项目(192102310408)。
