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Bromodomains(BRDs)是一类能够特异性识别乙酰化赖氨酸残基的保守蛋白结构域,存在于染色质及与转录相关的蛋白中,其功能包括染色质重塑和转录调控,并在细胞内由乙酰化介导的蛋白-蛋白相互作用中发挥极为重要的作用,是多种疾病(包括癌症、炎症和自身免疫病)的表观遗传医学靶点。介绍BRDs的生物学功能、结构及分类,主要从BETbromodomain抑制剂和非BETbromodomain抑制剂两个方面对BRDs抑制剂的研究进展作一综述,为高活性和选择性的BRDs抑制剂研发提供参考。
Bromodomains (BRDs) are a class of conserved protein domains that specifically recognize acetylated lysine residues found in chromatin and transcription-related proteins, including chromatin remodeling and transcriptional regulation, Plays an extremely important role within acetylation-mediated protein-protein interactions and is an epigenetic target of many diseases, including cancer, inflammation and autoimmune diseases. The biological function, structure and classification of BRDs were introduced. The research progress of BRDs inhibitors from two aspects: BET - bromodomain inhibitors and non - BET - bromobondomain inhibitors were reviewed. The results provide references for the development of highly active and selective BRDs inhibitors.