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当代肿瘤药物靶点

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ISSN (Print): 1568-0096
ISSN (Online): 1873-5576

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Review Article

PROTACs（双功能小分子）：克服耐药性的表观遗传策略的有希望的方法

卷 21, 期 4, 2021

发表于: 02 February, 2021

页: [306 - 325] 页: 20

弟呕挨: 10.2174/1568009621666210203110857

价格: $65

摘要

基因表达的表观遗传调节对于哺乳动物细胞的组织特异性发育和维持至关重要。表观遗传过程的中断以及随后基因功能的改变可能导致各种细胞信号通路的不适当激活或抑制，从而导致癌症。对表观遗传学在癌症发生和进展中的作用的理解的最新进展揭示了 DNA 甲基化、组蛋白修饰、核小体定位和非编码 RNA 的功能。表观遗传疗法已显示出治疗血液系统恶性肿瘤的一些希望，并且多种基于表观遗传的药物正在进行临床试验。然而，在动态生存策略中，癌细胞利用其异质性群体，这经常导致快速获得治疗抗性。在这里，我们描述了针对表观基因组的药物发现的新方法，重点介绍了使用蛋白水解靶向嵌合体 (PROTAC) 选择性降解靶蛋白以解决耐药性的最新进展。

关键词: 癌症、肿瘤学、PROTAC、表观遗传学、耐药性、治疗耐药性。

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