Kalyoncu Minenur, Demirci Dilara, Eris Sude, Dayanc Bengisu, Cakiroglu Ece, Basol Merve, Uysal Merve, Cakan-Akdogan Gulcin, Liu Fang, Ozturk Mehmet, Karakülah Gökhan, Senturk Serif
Izmir Biomedicine and Genome Center, Turkey.
Department of Genomics and Molecular Biotechnology, Izmir International Biomedicine and Genome Institute, Dokuz Eylul University, Izmir, Turkey.
Mol Oncol. 2025 Sep;19(9):2594-2618. doi: 10.1002/1878-0261.70021. Epub 2025 Mar 14.
Transforming growth factor-β (TGF-β) signaling and cellular senescence are key hallmarks of hepatocellular carcinoma (HCC) pathogenesis. Despite provoking senescence-associated growth arrest in epithelial HCC cells, elevated TGF-β activity paradoxically correlates with increased aggressiveness and poor prognosis in advanced tumors. Whether the transition between these dichotomous functions involves modulation of the senescence phenotype during disease progression remains elusive. Exploiting the epithelial HCC cell line Huh7 as a robust model, we demonstrate that chronic exposure to TGF-β prompts escape from Smad3-mediated senescence, leading to the development of TGF-β resistance. This altered state is characterized by an optimal proliferation rate and the acquisition of molecular and functional traits of less-differentiated mesenchymal cells, coinciding with differential growth capacity in 2D and 3D culture conditions, epithelial-to-mesenchymal transition (EMT), and increased invasiveness in vitro, and metastasis in vivo. Mechanistically, resistant cells exhibit defective activation and nuclear trafficking of Smad molecules, particularly Smad3, as ectopic activation of the TGF-β/Smad3 axis is able to reinstate TGF-β sensitivity. An integrated transcriptomic landscape reveals both shared and distinct gene signatures associated with senescent and TGF-β resistant states. Importantly, genetic ablation and molecular studies identify microtubule affinity regulating kinase 1 (MARK1) and glutamate metabotropic receptor 8 (GRM8) as critical modulators of the resistance phenomenon, potentially by impairing spatiotemporal signaling dynamics of Smad activity. Our findings unveil a novel phenomenon wherein epithelial HCC cells may exploit senescence plasticity as a mechanism to oppose TGF-β anti-tumor responses and progress towards more aggressive HCC phenotypes.
转化生长因子-β(TGF-β)信号传导和细胞衰老 是肝细胞癌(HCC)发病机制的关键标志。尽管TGF-β活性升高会引发上皮性HCC细胞的衰老相关生长停滞,但矛盾的是,在晚期肿瘤中,其活性升高与侵袭性增加和预后不良相关。在疾病进展过程中,这些二分功能之间的转变是否涉及衰老表型的调节仍不清楚。利用上皮性HCC细胞系Huh7作为一个强大的模型,我们证明长期暴露于TGF-β会促使细胞逃离Smad3介导的衰老,导致TGF-β抗性的产生。这种改变的状态的特征是最佳增殖率以及获得低分化间充质细胞的分子和功能特性,这与二维和三维培养条件下的不同生长能力、上皮-间充质转化(EMT)以及体外侵袭性增加和体内转移相吻合。从机制上讲,抗性细胞表现出Smad分子,特别是Smad3的激活和核转运缺陷,因为TGF-β/Smad3轴的异位激活能够恢复TGF-β敏感性。一个综合的转录组图谱揭示了与衰老和TGF-β抗性状态相关的共同和独特的基因特征。重要的是,基因敲除和分子研究确定微管亲和力调节激酶1(MARK1)和谷氨酸代谢型受体8(GRM8)是抗性现象的关键调节因子,可能是通过损害Smad活性 的时空信号动态。我们的研究结果揭示了一种新现象,即上皮性HCC细胞可能利用衰老可塑性作为一种机制来对抗TGF-β的抗肿瘤反应,并向更具侵袭性的HCC表型发展。