抑制真核生物转录：该选择哪种化合物？如何评估其活性？
Inhibiting eukaryotic transcription: Which compound to choose? How to evaluate its activity?
作者信息
Bensaude Olivier
机构信息
IBENS; UMR CNRS 8197; UA INSERM 1024; Paris, France.
出版信息
Transcription. 2011 May;2(3):103-108. doi: 10.4161/trns.2.3.16172.
Abstract
This review first discusses ways in which we can evaluate transcription inhibition, describe changes in nuclear structure due to transcription inhibition, and report on genes that are paradoxically stimulated by transcription inhibition. Next, it summarizes the characteristics and mechanisms of commonly used inhibitors: α-amanitin is highly selective for RNAP II and RNAP III but its action is slow, actinomycin D is fast but its selectivity is poor, CDK9 inhibitors such as DRB and flavopiridol are fast and reversible but many genes escape transcription inhibition. New compounds, such as triptolide, are fast and selective and able to completely arrest transcription by triggering rapid degradation of RNAP II.
摘要
本综述首先讨论了评估转录抑制的方法，描述了转录抑制导致的核结构变化，并报告了因转录抑制而受到反常刺激的基因。接下来，总结了常用抑制剂的特性和作用机制：α-鹅膏蕈碱对RNA聚合酶II和RNA聚合酶III具有高度选择性，但其作用缓慢；放线菌素D作用迅速，但其选择性较差；CDK9抑制剂（如DRB和黄酮哌啶醇）作用迅速且可逆，但许多基因能逃避转录抑制。新化合物（如雷公藤内酯醇）作用迅速且具有选择性，能够通过触发RNA聚合酶II的快速降解来完全阻止转录。
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