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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

组蛋白去乙酰化酶(HDAC) 1抑制剂的抗癌研究进展

卷 23, 期 1, 2023

发表于: 20 August, 2022

页: [47 - 70] 页: 24

弟呕挨: 10.2174/1568009622666220624090542

价格: $65

摘要

组蛋白去乙酰化酶(HDACs)是通过催化组蛋白去乙酰化维持体内平衡所必需的。HDACs的异常表达与多种人类疾病相关。尽管HDAC抑制剂在临床中被作为有效的化疗药物，但由于弱亚型选择性引起的相关副作用，其应用仍受到限制。HDAC1具有独特的结构和细胞定位以及多种底物，比其他亚型具有更广泛的生物学功能。HDAC1显示出一种独特的结构，主要在细胞核中发现，并参与表观遗传和转录调控。HDAC1广泛表达，并与Sin3、NuRD和CoRest转录抑制复合体相关，负责不同的细胞过程，如细胞增殖和存活。HDAC1抑制剂已被有效用于治疗各种癌症，如胃癌、乳腺癌、大肠癌、前列腺癌、结肠癌、肺癌、卵巢癌、胰腺癌和炎症，而不产生明显的毒性作用。本文综述了HDAC1抑制剂的四种主要结构类(羟肟酸衍生物、苯甲酰胺类、肼类和硫醇类)及其结构活性关系。本文综述了HDAC1抑制剂的研究进展，旨在深入了解HDAC1抑制剂的结构信息。这为开发新的选择性HDAC1抑制剂作为抗癌药物提供了最新的方向。

关键词: 组蛋白去乙酰化酶1(HDAC1)，抗癌，羟肟酸衍生物，苯酰胺，肼，硫醇。

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