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首页> 外文期刊>Journal of Biomolecular Structure and Dynamics >Computer-aided screening for suppressor of variegation 4-20 homolog 1 inhibitors and their preliminary activity validation in human osteosarcoma
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Computer-aided screening for suppressor of variegation 4-20 homolog 1 inhibitors and their preliminary activity validation in human osteosarcoma

机译：诸定抑制抑制剂的计算机辅助筛选4-20同源物1抑制剂及其在人骨瘤中的初步活性验证

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摘要

Histone methylation/demethylation facilitate to maintain balanced histone methylation levels and underpin gene regulation, playing the key roles in epigenetic regulation. Suppressor of variegation 4-20 homolog 1 (SUV420H1), a member of class Histone Lysine Methyltransferase and a key enzyme in the epigenetic regulation of the pathways controlling metabolism and tumorigenesis, is crucial to maintain cell homeostasis. The inhibition of SUV420H1 has emerged as a promising candidate for drug development and cancer therapy. Herein, two potential and potent SUV420H1 inhibitors (ZINC08398384, ZINC08439608) were identified through in silico approach and in vitro biological experiments. In vitro biological tests demonstrated that these compounds can inhibit the proliferation of U2OS cells and restrict its migration ability. And the level of dimethylation of lysine 20 on histone H4 (H4K20me2) was markedly decreased by these compounds-treatment in a dose-dependent manner. These results indicated that ZINC08398384 and ZINC08439608 are potential SUV420H1 inhibitors and could be developed as promising drug candidates applied to cancer epigenetic therapy. Communicated by Ramaswamy H. Sarma
机译：组蛋白甲基化/去甲基化有助于维持平衡的组蛋白甲基化水平，支持基因调控，在表观遗传调控中发挥关键作用。杂色4-20同系物1（SUV420H1）的抑制子是组蛋白赖氨酸甲基转移酶类的成员，是控制代谢和肿瘤发生途径的表观遗传调节中的关键酶，对维持细胞内环境稳定至关重要。SUV20H1作为一种有希望的癌症治疗候选药物出现了。在此，通过电子方法和体外生物学实验，确定了两种潜在且有效的SUV420H1抑制剂（ZINC0839384，ZINC08439608）。体外生物学试验表明，这些化合物可以抑制U2OS细胞的增殖并限制其迁移能力。赖氨酸20在组蛋白H4（H4K20me2）上的二甲基化水平通过这些化合物的剂量依赖性处理显著降低。这些结果表明ZINC08398384和ZINC08439608是潜在的SUV420H1抑制剂，有望成为应用于癌症表观遗传学治疗的候选药物。由拉玛斯瓦米·H·萨尔玛传达

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