BRD7/9 bromodomains蛋白化学探针研究进展

Advances in BRD7/9 Bromodomains Protein Chemical Probes

Bromodomains(BRDs)结构域可以特异性识别乙酰化的组蛋白赖氨酸,这是表观遗传调控过程中的关键步骤。目前对BRDs家族的研究主要集中在BET家族,对其他家族少有涉及。最近,靶向于BRD7/9的化学小分子探针陆续被发现。本文通过对BRD7/9 bromodomains结构、BRD7/9小分子探针的研究历程及其构效关系等多方面进行总结,以期进一步探索BRD7/9的生物学功能和疾病治疗中的潜在用途,为设计和开发高活性的BRD7/9 bromodomains小分子抑制剂提供参考依据。

The Bromodomains （BRDs） domain specifically recognizes the acetylated histone lysine, a key step in epigenetic regulation. At present, the research on the BRDs family mainly focuses on the BET family, but it is rarely involved in other families. Recently, chemical small molecule probes targeting BRD7/9 have been discovered one after another. This article summarizes the BRD7/9 bromodomains structure, BRD7/9 small molecule probes, and its structure-activity relationship, in order to further explore the biological functions of BRD7/9 and its potential use in disease treatment, and to develop highly active BRD7/9 bromodomains small molecule inhibitors for reference.