Yue Xin, Xiang Zhen, Yi Yang, Wang Xuecen, Zhou Weilin, Wu Weijian, Qin Wenjing, Zhao Yuxuan, Bu Xianzhang, Peng Zhenwei
Department of Radiation Oncology, The First Affiliated Hospital, Sun Yat-sen University, Guangzhou, China.
State Key Laboratory of Bioactive Molecules and Druggability Assessment, The First Affiliated Hospital of Jinan University, Guangzhou, China.
Cell Death Dis. 2025 Jul 1;16(1):481. doi: 10.1038/s41419-025-07807-6.
Radiation resistance constitutes a formidable impediment in the treatment paradigm for hepatocellular carcinoma (HCC). Deubiquitinases (DUBs) exhibit notable efficacy in modulating cellular responses to stress and exogenous interventions, endowed with the critical trait of being targetable, thus facilitating the execution of precise therapeutic strategies. Here, we demonstrate that broad-spectrum inhibition of thiol hydrolase-type DUBs markedly augments radiotherapy sensitivity in HCC cells. Based on this, via CRISPR-based screening, we identified USP14 as the principal DUB orchestrating radioresistance. Ferroptosis emerged as a pivotal form of radiation-induced cell death, with our study singularly illustrating that USP14 is instrumental in directing cellular defenses against ferroptosis via the targeting and stabilization of glutathione peroxidase (GPX4). Mechanistically, we found that radiation triggers the assembly of Tripartite motif-containing protein 14 (TRIM14) at the GPX4 locus, subsequently recruiting USP14. The TRIM14/USP14 complex facilitates the excision of pronounced K48-linked polyubiquitination at lysine residues 48 or 118 on GPX4, thereby preserving GPX4's structural integrity and antioxidative function to counteract ferroptosis. Intriguingly, TRIM14-mediated GPX4 stabilization is further amplified in radioresistant HCC, and subsequent radiation enables USP14-dependent blockade of GPX4 degradation. Consequently, pharmacological inhibition of USP14 substantially increases the susceptibility of HCC cells, thereby sensitizing patient-derived xenograft (PDX) tumors to radiotherapy. Concurrently, we explored the abscopal effect of radiotherapy and revealed that targeting USP14-enhanced ferroptosis augments antitumor immune responses post-radiation, suggesting a strategy to sustain therapeutic efficacy. In conclusion, our study uncovers the TRIM14/USP14 axis as a critical suppressor of radiation-induced ferroptosis and an actionable target to overcome radioresistance in HCC. These findings provide mechanistic insights and a translational framework for improving radiotherapy outcomes.
辐射抗性是肝细胞癌(HCC)治疗模式中的一个巨大障碍。去泛素化酶(DUBs)在调节细胞对应激和外源性干预的反应方面表现出显著功效,具有可靶向的关键特性,从而有助于实施精确的治疗策略。在此,我们证明对硫醇水解酶型DUBs的广谱抑制显著增强了HCC细胞的放射敏感性。基于此,通过基于CRISPR的筛选,我们确定USP14是协调放射抗性的主要DUB。铁死亡成为辐射诱导细胞死亡的一种关键形式,我们的研究独特地表明USP14通过靶向和稳定谷胱甘肽过氧化物酶(GPX4)在指导细胞对抗铁死亡防御中发挥作用。从机制上讲,我们发现辐射触发含三联基序蛋白14(TRIM14)在GPX4基因座处组装,随后招募USP14。TRIM14/USP14复合物促进在GPX4上赖氨酸残基48或118处显著的K48连接多聚泛素化的切除,从而保持GPX4的结构完整性和抗氧化功能以对抗铁死亡。有趣的是,TRIM14介导的GPX4稳定在放射抗性HCC中进一步增强,随后的辐射使USP14依赖的GPX4降解受阻。因此,对USP14的药理学抑制显著增加了HCC细胞的敏感性,从而使患者来源的异种移植(PDX)肿瘤对放疗敏感。同时,我们探索了放疗的远隔效应,发现靶向USP14增强的铁死亡增强了放疗后的抗肿瘤免疫反应,提示了一种维持治疗效果的策略。总之,我们的研究揭示了TRIM14/USP14轴是辐射诱导铁死亡的关键抑制因子,也是克服HCC放射抗性的一个可操作靶点。这些发现为改善放疗结果提供了机制见解和转化框架。