可药性
脱甲基酶
生物
癌症
药物发现
计算生物学
癌症研究
癌基因
药理学
生物化学
细胞周期
遗传学
表观遗传学
基因
作者
Yi‐Chao Zheng,Bin Yu,Zhe‐Sheng Chen,Ying Li
出处
期刊:Epigenomics
[Future Medicine]
日期:2016-05-01
卷期号:8 (5): 651-666
被引量:73
标识
DOI:10.2217/epi-2015-0002
摘要
Since the first lysine-specific demethylase (KDM), lysine-specific demethylase 1 (LSD1), was characterized in 2004, several families of KDMs have been identified. LSD1 can specifically demethylate H3K4me1/2, H3K9me1/2 as well as some nonhistone substrates. It has been demonstrated to be an oncogene as well as a drug target. Hence, tens of small-molecule LSD1 inhibitors have been designed, synthesized and applied for cancer treatment. However, the two LSD1 inhibitors that have been advanced into early phase clinical trials are trans-2-phenylcyclopropylamine (TCP) derivatives, which indicate that TCP is a druggable scaffold for LSD1 inhibitor. Here, we review the design, synthesis and properties of reported TCP-based LSD1 inhibitors as well as their biological roles.
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