Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1
Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1
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DOI：
10.1021/acs.jmedchem.0c02176
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发表时间：
2021-02-23
影响因子：
7.3
通讯作者：
Liu, Hong-Min
中科院分区：
文献类型：
--
作者：
Dai, Xing-Jie;Liu, Ying;Liu, Hong-Min
赖氨酸特异性去甲基化酶1（LSD 1/KDM 1A）是一种黄素腺嘌呤二核苷酸（FAD）依赖的单胺氧化酶，作为转录共激活因子或共抑制因子，调控组蛋白3赖氨酸4和9（H3 K4/9）的甲基化，是一种很有前景的表观遗传治疗靶点。迄今为止，已经开发了许多针对LSD 1的抑制剂，其中一些正在进行癌症治疗的临床试验。虽然只有两种可逆的LSD 1抑制剂CC-90011和SP-2577处于临床阶段，但在过去的十年中，可逆的LSD 1抑制剂的开发取得了显着进展。本文就LSD 1可逆抑制剂的结构、生物学评价和构效关系（SAR）进行了综述。
As a flavin adenine dinucleotide (FAD)-dependent monoamine oxidase, lysine specific demethylase 1 (LSD1/KDM1A) functions as a transcription coactivator or corepressor to regulate the methylation of histone 3 lysine 4 and 9 (H3K4/9), and it has emerged as a promising epigenetic target for anticancer treatment. To date, numerous inhibitors targeting LSD1 have been developed, some of which are undergoing clinical trials for cancer therapy. Although only two reversible LSD1 inhibitors CC-90011 and SP-2577 are in the clinical stage, the past decade has seen remarkable advances in the development of reversible LSD1 inhibitors. Herein, we provide a comprehensive review about structures, biological evaluation, and structureactivity relationship (SAR) of reversible LSD1 inhibitors.