Janardhan Avilala, Kathera Chandrasekhar, Darsi Amrutha, Ali Wajid, He Lingfeng, Yang Yanhua, Luo Libo, Guo Zhigang
The No. 7 People's Hospital of Changzhou, Changzhou, China.
Jiangsu Key Laboratory for Molecular and Medical Biotechnology, College of Life Sciences, Nanjing Normal University, Nanjing, China.
Oncotarget. 2018 Jan 25;9(76):34429-34448. doi: 10.18632/oncotarget.24319. eCollection 2018 Sep 28.
Protein methylation has an important role in the regulation of chromatin, gene expression and regulation. The protein methyl transferases are genetically altered in various human cancers. The enzymes that remove histone methylation have led to increased awareness of protein interactions as potential drug targets. Specifically, Lysine Specific Demethylases (LSD) removes methylated histone H3 lysine 4 (H3K4) and H3 lysine 9 (H3K9) through formaldehyde-generating oxidation. It has been reported that LSD1 and its downstream targets are involved in tumor-cell growth and metastasis. Functional studies of LSD1 indicate that it regulates activation and inhibition of gene transcription in the nucleus. Here we made a discussion about the summary of histone lysine demethylase and their functions in various human cancers.
蛋白质甲基化在染色质调控、基因表达及调节中发挥着重要作用。蛋白质甲基转移酶在多种人类癌症中发生基因改变。去除组蛋白甲基化的酶使得人们愈发意识到蛋白质相互作用作为潜在药物靶点的重要性。具体而言，赖氨酸特异性去甲基化酶（LSD）通过产生甲醛的氧化反应去除甲基化的组蛋白H3赖氨酸4（H3K4）和H3赖氨酸9（H3K9）。据报道，LSD1及其下游靶点参与肿瘤细胞的生长和转移。LSD1的功能研究表明，它在细胞核中调节基因转录的激活和抑制。在此，我们对组蛋白赖氨酸去甲基化酶及其在各种人类癌症中的功能进行了综述。
