脱甲基酶
黄素腺嘌呤二核苷酸
组蛋白
生物化学
功能(生物学)
化学
生物
计算生物学
药理学
基因
细胞生物学
酶
辅因子
作者
Huimin Liu,Ying Zhou,He‐Xiang Chen,Jiang‐Wan Wu,Shi‐Kun Ji,Liang Shen,Shao‐Peng Wang,Hong‐Min Liu,Ying Liu,Xing‐Jie Dai,Yi‐Chao Zheng
摘要
Abstract Lysine‐specific demethylase 1 (LSD1) is a flavin adenine dinucleotide (FAD) dependent monoamine oxidase (MAO) that erases the mono‐, and dimethylation of histone 3 lysine 4 (H3K4), resulting in the suppression of target gene transcriptions. Besides, it can also demethylate some nonhistone substrates to regulate their biological functions. As reported, LSD1 is widely upregulated and plays a key role in several kinds of cancers, pharmacological or genetic ablation of LSD1 in cancer cells suppresses cell aggressiveness by several distinct mechanisms. Therefore, numerous LSD1 inhibitors, including covalent and noncovalent, have been developed and several of them have entered clinical trials. Herein, we systemically reviewed and discussed the biological function of LSD1 in tumors, lymphocytes as well as LSD1‐targeting inhibitors in clinical trials, hoping to benefit the field of LSD1 and its inhibitors.
科研通智能强力驱动
Strongly Powered by AbleSci AI