赖氨酸特异性去甲基化酶1抑制剂与肿瘤治疗的研究进展

Recent advances in inhibitors of lysine specific demethylase 1 in tumor therapies

组蛋白赖氨酸特异性去甲基化酶1（LSD1）是一种黄素腺嘌呤二核苷酸依赖的去甲基酶，能特异性催化组蛋白H3第4位赖氨酸和组蛋白H3第9位赖氨酸的脱一甲基、二甲基反应（H3K4me、H3K4me2、H3K9me、H3K9me2），调控靶基因的表达。研究证实，LSD1在多种恶性肿瘤组织中高表达，与肿瘤的发生、增殖、侵袭转移过程密切相关。LSDl及其抑制剂已经成为近年来的研究热点，本文就目前LSDl抑制剂与肿瘤治疗的研究成果作一综述。

Lysine specific demethylase 1 （LSD1）, a flavin adenine dinucleotidedependent demethylase, specifically catalyzes the demethylation of mono - and dimethylated histone H3 lysine 4 （H3K4） and histone H3 lysine 9 （H3K9）as well as functionally regulates target gene expression. Studies have shown that LSD1 is highly expressed in many malignant tumors and closely related to tumorigenesis, proliferation, invasion and metastasis. Therefore, LSD1 and its inhibitors have recently emerged as sharp research focus. In this review, the authors address the new research findings among the LSD1 inhibitors and tumor therapy.