Developments of Fms-like Tyrosine Kinase 3 Inhibitors as Anticancer Agents for AML Treatment

被引:1
作者
Ma, Chenchen [1 ,2 ,3 ]
Cui, Siyuan [4 ]
Xu, Ruirong [4 ,5 ,6 ]
机构
[1] Shandong Univ Tradit Chinese Med, Coll Integrated Tradit Chinese & Western Med, Jinan 250014, Peoples R China
[2] Shandong Univ Tradit Chinese Med, Cent Lab, Affiliated Hosp, Jinan 250014, Peoples R China
[3] Shandong Key Lab Dominant Dis Tradit Chinese Med, Jinan 250014, Peoples R China
[4] Shandong Univ Tradit Chinese Med, Dept Hematol, Affiliated Hosp, Jinan 250014, Peoples R China
[5] Shandong Univ Tradit Chinese Med, Inst Hematol, Jinan 250014, Peoples R China
[6] Shandong Univ Tradit Chinese Med, Shandong Prov Hlth Commiss Key Lab Hematol Integra, Affiliated Hosp, Jinan, Peoples R China
关键词
AML; FLT3; inhibitors; anticancer activity; structure modification; SARs; ACUTE MYELOID-LEUKEMIA; SELECTIVE FLT3 INHIBITOR; IN-VITRO; EFFICACIOUS INHIBITORS; POTENT INHIBITOR; PHASE-I; DISCOVERY; DERIVATIVES; IDENTIFICATION; MIDOSTAURIN;
D O I
10.2174/0109298673277543231205072556
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
Background FMS-like tyrosine kinase 3 (FLT3) is a commonly mutated gene in acute myeloid leukemia. As a receptor tyrosine kinase (RTK), FLT3 plays a role in the proliferation and differentiation of hematopoietic stem cells. As the most frequent molecular alteration in AML, FLT3 has drawn the attention of many researchers, and a lot of small molecule inhibitors targeting FLT3 have been intensively investigated as potential drugs for AML therapy.Methods In this paper, PubMed and SciFinder (R) were used as a tool; the publications about "FLT3 inhibitor" and "Acute myeloid leukemia" were surveyed from 2014 to the present with an exclusion of those published as patents.Results In this study, the structural characterization and biological activities of representative FLT3 inhibitors were summarized. The major challenges and future directions for further research are discussed.Conclusion Recently, numerous FLT3 inhibitors have been discovered and employed in FLT3-mutated AML treatment. In order to overcome the drug resistance caused by FLT3 mutations, screening multitargets FLT3 inhibitors has become the main research direction. In addition, the emergence of irreversible FLT3 inhibitors also provides new ideas for discovering new FLT3 inhibitors.
引用
收藏
页码:4657 / 4686
页数:30
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