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RNA 聚合酶 I 催化核心的表达受 RPA12 的影响。

Expression of RNA polymerase I catalytic core is influenced by RPA12.

机构信息

Drug Research Program, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.

Department of Pharmaceutical Biosciences, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.

出版信息

PLoS One. 2023 May 11;18(5):e0285660. doi: 10.1371/journal.pone.0285660. eCollection 2023.

Abstract

RNA Polymerase I (Pol I) has recently been recognized as a cancer therapeutic target. The activity of this enzyme is essential for ribosome biogenesis and is universally activated in cancers. The enzymatic activity of this multi-subunit complex resides in its catalytic core composed of RPA194, RPA135, and RPA12, a subunit with functions in RNA cleavage, transcription initiation and elongation. Here we explore whether RPA12 influences the regulation of RPA194 in human cancer cells. We use a specific small-molecule Pol I inhibitor BMH-21 that inhibits transcription initiation, elongation and ultimately activates the degradation of Pol I catalytic subunit RPA194. We show that silencing RPA12 causes alterations in the expression and localization of Pol I subunits RPA194 and RPA135. Furthermore, we find that despite these alterations not only does the Pol I core complex between RPA194 and RPA135 remain intact upon RPA12 knockdown, but the transcription of Pol I and its engagement with chromatin remain unaffected. The BMH-21-mediated degradation of RPA194 was independent of RPA12 suggesting that RPA12 affects the basal expression, but not the drug-inducible turnover of RPA194. These studies add to knowledge defining regulatory factors for the expression of this Pol I catalytic subunit.

摘要

RNA 聚合酶 I(Pol I)最近被认为是癌症治疗的靶点。该酶的活性对于核糖体的生物发生至关重要,并且在癌症中普遍被激活。该多亚基复合物的酶活性位于其催化核心,该核心由 RPA194、RPA135 和 RPA12 组成,RPA12 具有 RNA 切割、转录起始和延伸的功能。在这里,我们探讨了 RPA12 是否影响人癌细胞中 RPA194 的调节。我们使用了一种特定的 Pol I 小分子抑制剂 BMH-21,它抑制转录起始、延伸,最终激活 Pol I 催化亚基 RPA194 的降解。我们发现,沉默 RPA12 会导致 Pol I 亚基 RPA194 和 RPA135 的表达和定位发生改变。此外,我们发现,尽管存在这些变化,RPA12 敲低后,Pol I 核心复合物(RPA194 和 RPA135 之间)不仅保持完整,而且 Pol I 的转录及其与染色质的结合仍然不受影响。BMH-21 介导的 RPA194 降解与 RPA12 无关,这表明 RPA12 影响 RPA194 的基础表达,而不是药物诱导的 RPA194 周转率。这些研究增加了对这种 Pol I 催化亚基表达的调节因子的认识。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bd69/10174586/e2690876187b/pone.0285660.g001.jpg

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