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通过药物重定位方法寻找新的MDM2/MDMX双抑制剂

Keting Li¹, Wenshu Hu¹, Yingjie Wang¹

¹School of Pharmacy, Nanjing University of Chinese Medicine, Nanjing, China.

Journal of enzyme inhibition and medicinal chemistry

|December 7, 2023

概括

一种现有的药物宁达尼布通过破坏p53相互作用有效地抑制MDM2/MDMX. 这种药物重定向策略为开发向p53通路的癌症疗法提供了一个有希望的新途径.

科学领域:

在瘤学瘤学.
药理学药理学是指药理学的学科.
结构生物学结构生物学

背景情况:

针对p53-MDM2/MDMX相互作用是癌症治疗的一个关键策略.
目前没有批准的MDM2/MDMX抑制剂,这凸显了对新型治疗方法的需求.
药物重新定位为识别新药候选药物提供了一条有效的途径.

研究的目的:

为了确定可以抑制p53-MDM2/MDMX相互作用的现有药物.
评估宁泰达尼布作为一种新型双重MDM2/MDMX抑制剂.
探索宁泰达尼布在癌症治疗中的治疗潜力.

主要方法:

销售药物的基于结构的虚拟选.
计算结构分析和生物化学测试.
机制研究以阐明药物向相互作用和细胞效应.

主要成果:

通过虚拟查,Nintedanib被确定为一种新的双重MDM2/MDMX抑制剂.
丁丁达尼布与MDM2/MDMX结合,类似于已知的抑制剂,如RO2443.
宁达达尼布破坏了p53-MDM2/MDMX相互作用,导致p53激活,细胞循环停止和癌细胞的生长抑制.
通过对宁泰达尼布的结构修改,产生了一种强效的类似物 (H3).

结论:

宁达达尼布是针对MDM2/MDMX的有希望的重用药物候选药物.
这项研究为开发基于忍者达尼布的MDM2/MDMX双抑制剂提供了基础.
药物再利用是发现新型癌症治疗方法的可行策略.

关键词:

药物重新定位是药物重新定位.在MDM2/MDMX中使用.双重抑制剂的双重抑制剂任天堂Danib 在线播放在 p53 里,p53 是一个 p53 号码.

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