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Recent Advances in the Development of CBP/p300 Bromodomain Inhibitors.
Current Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-09-30 , DOI: 10.2174/0929867326666190731141055
Ying Xiong 1 , Mingming Zhang 2 , Yingxia Li 2
Affiliation  

CBP and p300 are two closely related Histone Acetyltransferases (HATs) that interact with numerous transcription factors and act to increase the expression of their target genes. Both proteins contain a bromodomain flanking the HAT catalytic domain that is important in binding of CBP/p300 to chromatin, which offers an opportunity to develop protein-protein interaction inhibitors. Since their discovery in 2006, CBP/p300 bromodomains have attracted much interest as promising new epigenetic targets for diverse human diseases, including inflammation, cancer, autoimmune disorders, and cardiovascular disease. Herein, we present a comprehensive review of the structure, function, and inhibitors of CBP/p300 bromodomains developed in the last several years, which is expected to be beneficial to relevant studies.



中文翻译:

CBP / p300 Bromodomain抑制剂开发的最新进展。

CBP和p300是两个密切相关的组蛋白乙酰基转移酶(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。两种蛋白质都包含一个位于HAT催化结构域两侧的溴结构域,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溴结构域作为有希望成为多种人类疾病(包括炎症,癌症,自身免疫性疾病和心血管疾病)的新表观遗传靶标,引起了人们的极大兴趣。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的综述,有望对相关研究有所帮助。

更新日期:2020-10-08
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