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理性发现双FLT3/HDAC抑制剂作为潜在的AML治疗方法

Zhijie Wang¹, Donglin Wu², Xiaofei Zhao²

¹ShenZhen Hospital, Southern Medical University, Shenzhen, 518000, PR China; School of Science, China Pharmaceutical University, Nanjing, 211198, PR China.

European journal of medicinal chemistry

|September 2, 2023

概括

新型双重抑制剂针对Fms类型的氨酸激酶3 (FLT3) 和基因素脱甲基酶 (HDACs) 显示出治疗急性髓性白血病 (AML) 的前景. 这些化合物通过阻断FLT3和HDAC通路,有效地抑制癌细胞增殖.

科学领域:

在瘤学瘤学.
药用化学医学化学
分子生物学分子生物学

背景情况:

急性髓性白血病 (AML) 患者通常面临着糟糕的结果和复发,由于单一向药物的限制.
同时抑制多个瘤信号为AML提供了一个有前途的治疗策略.
以前的研究表明,结合Fms类型的氨酸激酶3 (FLT3) 和胰岛素脱乙酶 (HDAC) 抑制可以提高AML治疗的疗效.

研究的目的:

为AML治疗开发针对FLT3和HDAC途径的新型双重抑制剂.
评估这些新型化合物的抑制活性和抗增殖作用.
阐明最强大的双重抑制剂的作用机制.

主要方法:

基于合理结构的药物设计被用来创建新的双FLT3 / HDAC抑制剂.
实验室试验用于评估对FLT3-ITD和HDAC异型的抑制活性.
在MV4-11 AML细胞中分析了细胞增殖,细胞亡和细胞循环停止.

主要成果:

几种新型化合物表现出强大且相当于FLT3-ITD和HDAC1.1的抑制.
化合物63选择性抑制与瘤发生相关的HDAC类I和IIB异型.
化合物63有效地阻断了MV4-11细胞增殖,诱导了细胞亡,并以剂量依赖的方式停止了细胞循环,证实了双重FLT3/HDAC通路的抑制.

结论:

该研究成功开发了新的双FLT3 / HDAC抑制剂,对AML具有治疗潜力.
化合物63是AML治疗中进一步研究的有希望的候选物.
基于结构的药物设计策略为开发先进的抗AML疗法提供了有价值的方法.

关键词:

在AML,AML就是AML.双重抑制剂的双重抑制剂 FLT3 FLT3 在线播放在HDAC的基础上,HDAC是

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