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以结构为导向的发现,用于用于癌症治疗的基架基PFKFB4抑制剂是二-1,3-二醇 (NBD)

Yiliang Chen¹, Shihong Wei¹, Qi Wang¹

¹School of Chemistry and Chemical Engineering, Anhui University of Technology, Ma'anshan, 243032, Anhui, PR China.

European journal of medicinal chemistry

|September 9, 2025

概括

新型二-1,3- (NBD) 化合物,特别是2v,通过抑制果糖-2,6-双酸酶4 (PFKFB4) 和减少瘤生长,显示出强大的抗癌活性. 这突显了NBD支架作为癌症治疗的有前途的治疗策略.

科学领域:

生物化学生物化学
药用化学医学化学
在瘤学瘤学.

背景情况:

由于耐药性,癌症治疗面临着挑战,需要新的向疗法.
果糖-2,6-双酸酶4 (PFKFB4) 在许多癌症中过度表达,导致瘤生长和预后不佳.
准PFKFB4为开发新的抗癌药物提供了一个有前途的战略.

研究的目的:

通过虚拟查和实验验证,识别新的PFKFB4抑制剂.
评估已识别的化合物的抗增殖和细胞毒性作用.
研究化合物的作用机制和体内疗效.

主要方法:

基于二-1,3-醇 (NBD) 支架的化合物的虚拟选.
在癌症细胞系中的体外抗增殖试验 (MCF-7,A549,HepG2) 和正常肝细胞中的细胞毒性试验 (HL7702).
机理学研究包括蛋白质水平分析,分子对接,细胞周期分析,细胞亡测定和体内异种移植研究.

主要成果:

化合物2v,具有6 - 酸部分,表现出最强大的抗增殖活性.
化合物2v降低了细胞内PFKFB4蛋白水平,并对PFKFB4的ATP结合部位进行了有利的结合.
在体外,2v在MCF-7细胞中表现出抗增殖,促细胞缩和抗迁移的作用. 在体内,2v在乳腺癌异种移植模型中实现了71.9%的瘤生长抑制.

结论:

该NBD支架是开发新型PFKFB4抑制剂的宝贵药源.
化合物2v代表了针对PFKFB4.4的抗癌药物开发的有希望的主要候选人.
抑制PFKFB4是一种可行的治疗策略,用于各种癌症.

关键词:

抗癌疗法是一种抗癌治疗.分子对接是分子对接.尼特罗二氧化-1,3-二醇这是一种PFKFB4抑制剂.瘤生长抑制剂瘤生长抑制剂

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