酪氨酸激酶
吡嗪酰胺
化学
激酶
酪氨酸
生物化学
组合化学
信号转导
利福平
抗生素
作者
Xuan Zheng,Zhiwen Chen,Ming Guo,Hong Liang,Xiaojuan Song,Xuefeng B. Ling,Zhihuan Liao,Yan Zhang,Jing Guo,Yang Zhou,Zhimin Zhang,Zhengchao Tu,Qian Zhang,Yongheng Chen,Zhang Zhang,Xiaoyun Lu
出处
期刊:ACS pharmacology & translational science
[American Chemical Society]
日期:2024-04-11
卷期号:7 (5): 1485-1506
标识
DOI:10.1021/acsptsci.4c00071
摘要
Secondary mutations in Fms-like tyrosine kinase 3-tyrosine kinase domain (FLT3-TKD) (e.g., D835Y and F691L) have become a major on-target resistance mechanism of FLT3 inhibitors, which present a significant clinical challenge. To date, no effective drugs have been approved to simultaneously overcome clinical resistance caused by these two mutants. Thus, a series of pyrazinamide macrocyclic compounds were first designed and evaluated to overcome the secondary mutations of FLT3. The representative
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