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Annual review of LSD1/KDM1A inhibitors in 2020
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2021-02-03 , DOI: 10.1016/j.ejmech.2021.113254
Dong-Jun Fu , Jun Li , Bin Yu

Lysine-specific demethylase 1 (LSD1/KDM1A) has emerged as a promising target for the discovery of specific inhibitors as antitumor drugs. Based on the source of compounds, all LSD1 inhibitors in this review are divided into two categories: natural LSD1 inhibitors and synthetic LSD1 inhibitors. This review highlights the research progress of LSD1 inhibitors with the potential to treat cancer covering articles published in 2020. Design strategies, structure-activity relationships, co-crystal structure analysis and action mechanisms are also highlighted.



中文翻译:

2020年LSD1 / KDM1A抑制剂的年度回顾

赖氨酸特异性脱甲基酶1(LSD1 / KDM1A)已成为发现特定抑制剂作为抗肿瘤药物的有希望的靶标。基于化合物的来源,本综述中的所有LSD1抑制剂均分为两类:天然LSD1抑制剂和合成LSD1抑制剂。这篇综述着重介绍了具有治疗癌症潜力的LSD1抑制剂的研究进展,涵盖了2020年发表的文章。还重点介绍了设计策略,结构-活性关系,共晶体结构分析和作用机理。

更新日期:2021-02-10
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