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Histone lysine specific demethylase 1 inhibitors
RSC Medicinal Chemistry ( IF 4.1 ) Pub Date : 2020-07-31 , DOI: 10.1039/d0md00141d
Samir Mehndiratta, Jing-Ping Liou

LSD1 plays a pivotal role in numerous biological functions. The overexpression of LSD1 is reported to be associated with different malignancies. Over the last decade, LSD1 has emerged as an interesting target for the treatment of acute myeloid leukaemia (AML). Numerous researchers have designed, synthesized, and evaluated various LSD1 inhibitors with diverse chemical architectures. Some of these inhibitors have entered clinical trials and are currently at different phases of clinical evaluation. This comprehensive review enlists recent research developments in LSD1 targeting pharmacophores reported over the last few years.

中文翻译:

组蛋白赖氨酸特异性去甲基酶 1 抑制剂

LSD1 在许多生物学功能中发挥着关键作用。据报道,LSD1 的过度表达与不同的恶性肿瘤有关。在过去的十年中,LSD1 已成为治疗急性髓系白血病 (AML) 的一个有趣的靶点。许多研究人员设计、合成和评估了具有不同化学结构的各种 LSD1 抑制剂。其中一些抑制剂已进入临床试验,目前正处于临床评估的不同阶段。这篇全面的综述收录了过去几年报道的针对 LSD1 药效团的最新研究进展。
更新日期:2020-09-23
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