Review Article

组蛋白去乙酰化酶抑制剂作为抗癌药物的研究进展

卷 27, 期 15, 2020

页: [2449 - 2493] 页: 45

弟呕挨: 10.2174/0929867325666181016163110

价格: $65

摘要

组蛋白去乙酰化酶(HDAC)抑制剂是一类相对较新的抗癌药物,在癌症细胞的表观或非表观调控、诱导死亡、凋亡和细胞周期阻滞中发挥重要作用。最近,它们在癌症患者中的应用已得到临床验证,FDA批准了四种HDAC抑制剂伏立诺他、罗米地辛、贝利司他和帕比司他,用于治疗皮肤/外周t细胞淋巴瘤和多发性骨髓瘤。更多的HDAC抑制剂正处于不同的临床发展阶段,用于治疗血液恶性肿瘤和实体肿瘤。此外,几种HDAC抑制剂作为抗癌药物(单独使用或与其他抗癌疗法联合使用)的临床试验正在进行中。在加强努力发现新的,希望更有效的治疗HDAC抑制剂,基于分子模型的合理药物设计发挥了重要作用。在这篇综述中,我们总结四大结构类型的HDAC抑制剂(异羟肟酸衍生物, 氨基苯甲酰胺,环肽和短链脂肪酸)的临床试验和不同的计算机建模工具的结构修改作为指导发现额外的HDAC抑制剂更大的治疗效用。

关键词: 组蛋白去乙酰化酶抑制剂(HDACis),表观遗传学,组蛋白去乙酰化酶与癌症,HDACis作为抗肿瘤药物,天然HDACis

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