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

作　　者：刘航 丁杰[1] 刘振华[1] 董奇[1] 糜睿[1] 蒋专 李显 樊斐 张旭阳 张龙凤 曾蓉[2] 张忠民 Liu Hang;Ding Jie;Liu Zhenhua;Dong Qi;Mi Rui;Jiang Zhuan;Li Xian;Fan Fei;Zhang Xuyang;Zhang Longfeng;Zeng Rong;Zhang Zhongmin(Department of Gastrointestinal Surgery,Guizhou Provincial People＇s Hospital,Guiyang 550002,China（Liu H,Ding J,Liu ZH,Dong Q,Mi R,Jiang Z,Li X,Fan F,Zhang LF,Zhang ZM;Operating Room,Gui Zhou Provincial People＇s Hospital,Guiyang 550002,China（Zeng R;Clinical Medical College,Zunyi Medical Univercity,Zunyi 563003,China（Liu H,Zhang XY)

机构地区：[1]贵州省人民医院胃肠外科,贵阳550002 [2]贵州省人民医院手术室,贵阳550002 [3]遵义医学院临床医学院,563003

出　　处：《中华实验外科杂志》2018年第10期1980-1983,共4页Chinese Journal of Experimental Surgery

基　　金：国家自然科学基金（81360366、81302169）;贵州省科学技术基金（黔科合J字[2013]2178号）;贵州省社会发展攻关项目（黔科合SY字[2014]3023号）;贵州省优秀青年科技人才培养对象（黔科合平台人才[2017]5602）;贵州省高层次创新型人才培养对象（GZSYQCC[2014]001）

摘　　要：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.

关 键 词：赖氨酸特异性去甲基化酶1 抑制剂 肿瘤治疗 

分 类 号：R730.2[医药卫生—肿瘤]