Drug Research Program, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.
Department of Pharmaceutical Biosciences, Faculty of Pharmacy, University of Helsinki, Helsinki, Finland.
PLoS One. 2023 May 11;18(5):e0285660. doi: 10.1371/journal.pone.0285660. eCollection 2023.
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.
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。