创新链/学科链/研发链/产业链

新药研发前沿动态 / 医药领域趋势进展

卞媛媛, 马宇, 陈亚东, 唐伟方. Bromodomains抑制剂及其在疾病治疗中的作用研究进展[J]. 药学进展, 2018, 42(3): 214-221.
引用本文: 卞媛媛, 马宇, 陈亚东, 唐伟方. Bromodomains抑制剂及其在疾病治疗中的作用研究进展[J]. 药学进展, 2018, 42(3): 214-221.
BIAN Yuanyuan, MA Yu, CHEN Yadong, TANG Weifang. Advances in Research on Bromodomain Inhibitors and Their Applications in Human Diseases[J]. Progress in Pharmaceutical Sciences, 2018, 42(3): 214-221.
Citation: BIAN Yuanyuan, MA Yu, CHEN Yadong, TANG Weifang. Advances in Research on Bromodomain Inhibitors and Their Applications in Human Diseases[J]. Progress in Pharmaceutical Sciences, 2018, 42(3): 214-221.

Bromodomains抑制剂及其在疾病治疗中的作用研究进展

Advances in Research on Bromodomain Inhibitors and Their Applications in Human Diseases

  • 摘要: Bromodomains(BRDs)是一类能够特异性识别乙酰化赖氨酸并形成驱动活性转录的蛋白质复合物的保守蛋白结构域,而组蛋白赖氨酸的N端乙酰化或去乙酰化修饰可改变染色质的结构,调控基因的转录激活和转录抑制。BRDs小分子抑制剂能够和乙酰化赖氨酸竞争性地与BRDs的疏水口袋结合,在表观遗传调控中发挥重要作用,在治疗肿瘤、炎症、自身免疫疾病和心血管疾病等方面也显示出巨大的研究潜力。综述BRDs抑制剂及其在疾病治疗中的作用研究进展,为高效、选择性BRDs小分子抑制剂的设计与开发提供参考。

     

    Abstract: Bromodomains (BRDs) are a type of conserved protein domains that recognize acetyl-lysine and facilitate the formation of protein complexes that drive active transcription. N-terminal acetylation or deacetylation of histone lysine modifies the structure of chromatin, thereby regulating transcriptional activation and inhibition. Small-molecule inhibitors of BRDs compete with acetyl-lysine in binding the hydrophobic pocket of BRDs, playing important roles in epigenetic regulation and showing great potential in the treatment of tumor, inflammation, autoimmune diseases and cardiovascular diseases. The progress in BRDs inhibitors and their roles in the treatment of diseases, so as to provide reference for the design and development of efficient and selective small-molecule inhibitors of BRDs.

     

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