摘要
背景:在过去的几年里，对首次鉴定的histone demethylase LSD1的鉴定和鉴定有了很大的关注，它可以抹去单 - 和二 - 甲基化组蛋白3赖氨酸4和9。由于LSD1的异常过表达参与了各种病理过程，尤其是癌症，获得选择性和有效的LSD1抑制剂已成为药物化学研究中的一个关键问题。 方法:目前已经建立了几种LSD1抑制剂筛选模型，包括酶偶联试验、基于lc - ms的分析和基于焦虑的分析。然而，由于某些特殊仪器的要求以及lc - ms和烦恼的额外费用，酶耦合试验是LSD1抑制剂筛选最广泛应用的方法。 结果:我们总结并比较了几种体外LSD1抑制剂筛选模型。每一种方法都有各自的优点和缺点，这些方法都不完美。为了排除错误的阳性结果，至少应该应用一个额外的方法来筛选LSD1抑制剂。
关键词: LSD1，抑制剂，筛选模型，酶耦合分析，lc - ms，FRET
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