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Review Article

CBP / p300 溴结构域抑制剂开发的最新进展

卷 27, 期 33, 2020

页: [5583 - 5598] 页: 16

弟呕挨: 10.2174/0929867326666190731141055

价格: $65

摘要

CBP和p300是两个密切相关的组蛋白乙酰转移酶（HAT），它们与众多转录因子相互作用，并起着增加其靶基因表达的作用。 两种蛋白质都含有一个位于HAT催化域侧翼的溴结构域，这对CBP / p300与染色质的结合很重要，这为开发蛋白质-蛋白质相互作用抑制剂提供了机会。 自2006年被发现以来，CBP / p300溴结构域引起了人们极大的兴趣，因为它们有望成为多种人类疾病的新表观遗传靶标，包括炎症，癌症，自身免疫性疾病和心血管疾病。 本文中，我们对最近几年开发的CBP / p300溴结构域的结构，功能和抑制剂进行了全面综述，有望对相关研究有所帮助。

关键词: CBP / p300，溴结构域，组蛋白乙酰转移酶，基因，抑制剂，药物发现。

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