开发甲醛响应的小分子荧光探针用于组蛋白去甲基化酶活性检测
首发时间:2020-05-27
摘要:组蛋白去甲基化酶(HDMs)是表观遗传调控的重要参与者,也是癌症治疗的重要靶标,对维持转录状态和决定细胞命运起着至关重要的作用。然而,目前用于分析HDMs活性的有效分子工具十分有限。本文基于HDMs催化底物去甲基化的过程中会产生小分子甲醛(HCHO)这一机理,通过合成HCHO响应的高灵敏小分子荧光探针(Na-FA),实现了赖氨酸特异性去甲基化酶(LSD1)的活性分析。该探针对LSD1具有高特异性荧光响应,其检测限低至0.8 nM,还可成功检测到Hela细胞裂解液中LSD1活性,在表观遗传学研究、药物发现和临床诊断方面具有广阔的应用前景。
关键词: 分析化学 小分子荧光探针 组蛋白去甲基化酶 活性分析
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Development of Formaldehyde-responsive Small Molecule Fluorescent Probe for Detection of Histone Demethylase Activity
Abstract:Histone demethylases (HDMs) are vital players in epigenetic regulation and important targets in cancer treatment, which plays a crucial role in maintaining transcription status and determining cell fate. However, the effective molecular tools for analyzing HDMs activity are still limited. Since HDMs produce small molecule formaldehyde (HCHO) in the process of catalytic demethylation, we synthesize a highly sensitive small molecule fluorescent probe (Na-FA) that responds to HCHO, realized the in vitro activity analysis of lysine-specific demethylase (LSD1). The probe has a highly specific fluorescence response to LSD1 activity, and its detection limit is as low as 0.8 nM. What\'s more, the probe can also successfully detect the activity of LSD1 in Hela cell lysate, which has broad application prospects in epigenetics research, drug discovery and clinical diagnosis.
Keywords: Analytical chemistry Small molecule fluorescent probe Histone demethylase Activity analysiskey
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