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基于PAP结构的棕甲基转移酶抑制剂的设计,合成和生物活性评估

Yibo Zhang¹, Han Liu¹, Jinze Li¹

¹Key Laboratory of Pharmaceutical Quality Control of Hebei Province, College of Pharmaceutical Sciences, Hebei University, Baoding, China.

Chemistry & biodiversity

|February 24, 2026

概括

研究人员开发了新的pyrazolo[3,4-d]pyrimidine衍生物作为棕醇转移酶 (DHHC) 抑制剂. 化合物C9通过抑制DHHC,减少细胞迁移和诱导亡,显示出强大的抗癌活性.

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:

蛋白质棕化是一种关键的翻译后修饰,影响癌症病原性.
棕甲基转移酶 (DHHC) 酶在癌症的发展中起着重要作用.
向DHHC为恶性瘤提供了一个潜在的治疗策略.

研究的目的:

设计和合成基于酸盐-腺-5'-二酸盐 (PAP) 配体的新型DHHC抑制剂.
为了评估合成的pyrazolo[3,4-d]pyrimidine衍生物的抗癌潜力.
为了研究最强效的化合物的作用机制.

主要方法:

合成pyrazolo[3,4-d]pyrimidine衍生物的合成方法.
在体外测定抗繁殖,迁移,入侵和亡.
细胞周期分析 (G0/G1停止).
分子对接和分子动力学模拟.

主要成果:

化合物C9表现出优异的DHHC抑制活性和强大的抗增殖作用对低毒性MC38细胞.
C9有效地抑制了癌细胞的迁移和入侵,促进了细胞亡,并诱导了G0/G1细胞循环停止.
分子建模证实了C9与DHHC活性部位的稳定结合.

结论:

化合物C9是一种有前途的新型DHHC抑制剂,具有显著的抗癌特性.
C9值得进一步研究,因为它是癌症治疗的潜在治疗剂.
通过DHHC抑制向蛋白质棕化是瘤学中可行的策略.

关键词:

这是一种DHHC抑制剂.它具有抗瘤活性.分子对接的分子对接.棕甲基转移酶的作用 pyrazolo[3,4‐d]pyrimidine的使用情况

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