LSD1 Inhibitor Screening Assay

LSD1是一种组蛋白去甲基化酶，其作用于特定赖氨酸残基会改变染色体DNA的转录。它还通过去甲基化特定赖氨酸残基来抑制p53的肿瘤抑制活性。LSD1抑制剂是阐明转录和细胞周期进展机制的重要工具，具有治疗癌症的潜力。Cayman的LSD1抑制剂筛选检测法提供了一种方便的荧光法来筛选LSD1特异性抑制剂。该检测法基于多步酶促反应，其中LSD1首先在组蛋白H3N端尾部前21个氨基酸对应的肽上的赖氨酸4去甲基化过程中产生H2O2。在辣根过氧化物酶存在下，H2O2与ADHP反应生成强荧光化合物试卤灵，可以用530-540nm之间的激发波长和585-595nm之间的发射波长进行分析。LSD1 is a histone demethylase whose actions on specific lysine residues alter transcription of chromosomal DNA. It also inhibits the tumor suppressor activity of p53 by demethylating a specific lysine residue. Inhibitors of LSD1 are important tools used to elucidate mechanisms of transcription and cell cycle progression and have therapeutic potential for treating cancer. Cayman's LSD1 Inhibitor Screening Assay provides a convenient fluorescence-based method for screening LSD1-specific inhibitors. The assay is based on the multistep enzymatic reaction in which LSD1 first produces H2O2 during the demethylation of lysine 4 on a peptide corresponding to the first 21 amino acids of the N-terminal tail of histone H3. In the presence of horseradish peroxidase, H2O2 reacts with ADHP to produce the highly fluorescent compound resorufin that can be analyzed with an excitation wavelength between 530-540 nm and an emission wavelength between 585-595 nm.分子式分子量