Lysine-specifiic histone demethylase 1 (LSD1): A potential molecular target for tumor therapy
Lysine-specifiic histone demethylase 1 (LSD1): A potential molecular target for tumor therapy
复制标题
DOI：
10.1615/critreveukargeneexpr.v22.i1.40
复制
发表时间：
2012-01-01
影响因子：
1.6
通讯作者：
Xiao, Yongtao
中科院分区：
文献类型：
--
作者：
Chen, Yingwei;Jie, Wen;Xiao, Yongtao
赖氨酸特异性脱甲基酶1（LSD I）是第一个被发现的组蛋白脱甲基酶，属于黄素腺嘌呤二核苷酸（FAD）依赖性胺氧化酶超家族。LSD 1通过氧化还原过程特异性地使单甲基或二甲基化的二甲基化组蛋白H3赖氨酸4（H3 K4）和H3赖氨酸9（H3 K9）去甲基化。最近的研究表明，LSDI在细胞增殖、脂肪形成、精子发生、染色体分离和胚胎发育等多种生物学过程中发挥着重要作用。此外，LSD 1还可通过抑制p53的抑癌活性而促进肿瘤的进展。迄今为止，作为发现抗肿瘤药物的潜在药物，LSD 1抑制剂的医学意义已受到极大的重视。本文就LSDI的结构、基本功能及其在肿瘤治疗中的应用等方面的研究进展作一综述。
Lysine-specific demethylase 1 (LSD I), the first identified histone demethylase, was belonged to the superfamily of the flavin adenine dinucleotide (FAD)-dependent amine oxidases. LSD1 specifically demethylates mono- or dimethylated dimethylated histone H3 lysine4 (H3K4) and H3 lysine 9 (H3K9) via a redox process. Recently evidences showed that LSDI played an important role in a broad spectrum of biological processes, including cell proliferation, adipogenesis, spermatogenesis, chromosome segregation and embryonic development. Furthermore, LSD1 also could promote progress of tumor by inhibiting the tumor suppressor activity of p53. To date, as a potential drug for discovering anti-tumor drugs, the medical significance of LSD1 inhibitors have been greatly appreciated. Here, we reviewed the remarkable progress being made in understanding of LSDI, mainly on its structure, basic function and medical application in tumor therapy..