Williams Tobias D, Michalak Ewa M, Carey Kirstyn T, Lam Enid Y N, Anderson Ashley, Griesbach Esther, Chan Yih-Chih, Papasaikas Panagiotis, Tan Vicky W T, Ngo Linh, MacPherson Laura, Gilan Omer, Rucinski Amber, Rutkowska-Klute Anna, Zinn Nico, Grandi Paola, Bantscheff Marcus, Prinjha Rab K, Dawson Sarah-Jane, Chao Jeffrey A, Wickramasinghe Vihandha O, Dawson Mark A
Friedrich Miescher Institute for Biomedical Research, 4056 Basel, Switzerland; Cancer Research Division, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia; Sir Peter MacCallum Department of Oncology, University of Melbourne, Melbourne, VIC, Australia.
Cancer Research Division, Peter MacCallum Cancer Centre, Melbourne, VIC, Australia; Sir Peter MacCallum Department of Oncology, University of Melbourne, Melbourne, VIC, Australia.
Mol Cell. 2025 Jan 2;85(1):117-131.e7. doi: 10.1016/j.molcel.2024.12.008.
Several transcription inhibitors have been developed as cancer therapies. However, they show modest clinical activity, highlighting that our understanding of the cellular response to transcriptional inhibition remains incomplete. Here we report that potent inhibitors of transcription not only impact mRNA output but also markedly impair mRNA transcript localization and nuclear export. We demonstrate that retention of newly transcribed mRNA in nuclear speckles is an adaptive response to chemically distinct transcriptional inhibitors. Retained transcripts are fully processed and accumulate in proportion to the expression level of the genes from which they emanate. The TREX mRNA export complex plays an integral role in directing nascent transcripts to nuclear speckles where they are bound to NXF1, protected from degradation, and poised for rapid export following re-initiation of transcription. Our findings provide new insights into the crosstalk between transcription and mRNA export with important implications for drugs aiming to inhibit transcription for therapeutic gain.
几种转录抑制剂已被开发用作癌症治疗药物。然而,它们的临床活性有限,这突出表明我们对细胞对转录抑制的反应的理解仍不完整。在此,我们报告强效转录抑制剂不仅会影响mRNA的产出,还会显著损害mRNA转录本的定位和核输出。我们证明,新转录的mRNA在核斑中的滞留是对化学性质不同的转录抑制剂的一种适应性反应。滞留的转录本经过充分加工,并与其所源自基因的表达水平成比例积累。TREX mRNA输出复合体在将新生转录本导向核斑中起着不可或缺的作用,在核斑中它们与NXF1结合,受到保护不被降解,并在转录重新启动后准备好快速输出。我们的发现为转录与mRNA输出之间的相互作用提供了新的见解,对旨在抑制转录以获得治疗益处的药物具有重要意义。