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Histone deacetylase 3 (HDAC3) inhibitors as anticancer agents: A review
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-02-26 , DOI: 10.1016/j.ejmech.2020.112171
Rajat Sarkar , Suvankar Banerjee , Sk Abdul Amin , Nilanjan Adhikari , Tarun Jha

Among different Histone deacetylases (HDACs), histone deacetylase 3 (HDAC3) is an epigenetic drug target which is currently marked as potential therapeutic strategy to combat various cancers. HDAC3 inhibitors are effective ways for the treatment of cancers, different neurodegenerative disorders, diabetes mellitus, cardiac diseases, HIV, inflammatory diseases, rheumatoid arthritis (RA), etc. Inhibition of HDAC3 metalloenzyme is a dynamic approach for drug design and discovery. This approach has gained considerable interest in recent years. The development of an effective therapeutic agent against HDAC3 is still challenging. A lot of work is still in demand. This current communication is a part of our extended work on HDAC3 inhibitors to achieve deep insight of knowledge about the structural information of HDAC3 inhibitors. This article is unique in terms of detailed structure-activity relationships (SARs) analysis. This may help to find out some important clues to design better active HDAC3Is in the future.



中文翻译:

组蛋白脱乙酰基酶3(HDAC3)抑制剂作为抗癌药:综述

在不同的组蛋白脱乙酰基酶(HDACs)中,组蛋白脱乙酰基酶3(HDAC3)是一种表观遗传药物靶标,目前被标记为对抗各种癌症的潜在治疗策略。HDAC3抑制剂是治疗癌症,各种神经退行性疾病,糖尿病,心脏病,HIV,炎性疾病,类风湿性关节炎(RA)等的有效方法。抑制HDAC3金属酶是药物设计和发现的动态方法。近年来,这种方法引起了极大的兴趣。抗HDAC3的有效治疗剂的开发仍然具有挑战性。仍然需要大量工作。当前的交流是我们对HDAC3抑制剂的扩展工作的一部分,以深入了解HDAC3抑制剂的结构信息。本文在详细的结构-活动关系(SAR)分析方面是独一无二的。这可能有助于找出一些重要的线索,以便将来设计更好的有源HDAC3I。

更新日期:2020-02-27
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