Department of Urology, Shenzhen Institute of Translational Medicine, Medical Innovation Technology Transformation Center, Shenzhen Second People's Hospital, The First Affiliated Hospital of Shenzhen University, International Cancer Center of Shenzhen University, Shenzhen, China.
Molecular Cancer Research Center, School of Medicine, Shenzhen Campus of Sun Yat-sen University, Sun Yat-sen University, Shenzhen, China.
Oncogene. 2024 Sep;43(38):2850-2867. doi: 10.1038/s41388-024-03136-8. Epub 2024 Aug 18.
Chemoresistance is an important cause of treatment failure in bladder cancer, and identifying genes that confer drug resistance is an important step toward developing new therapeutic strategies to improve treatment outcomes. In the present study, we show that gemcitabine plus cisplatin (GEM/DDP) therapy induces NF-κB signaling, which promotes p65-mediated transcriptional activation of OIP5. OIP5 recruits the E3 ubiquitin ligase TRIP12 to bind to and degrade the phosphatase PPP1CB, thereby enhancing the transcription factor activity of YBX1. This in turn upregulates drug-resistance-related genes under the transcriptional control of YBX1, leading to chemoresistance. Moreover, PPP1CB degradation can enhance the phosphorylation activity of IKKβ, triggering the NF-κB signaling cascade, which further stimulates OIP5 gene expression, thus forming a negative feedback regulatory loop. Consistently, elevated OIP5 expression was associated with chemoresistance and poor prognosis in patients with bladder cancer. Furthermore, we used a CRISPR/Cas9-based engineered gene circuit, which can monitor the progression of chemoresistance in real-time, to induce OIP5 knockout upon detection of increased NF-κB signaling. The gene circuit significantly inhibited tumor cell growth in vivo, underscoring the potential for synergy between gene therapy and chemotherapy in the treatment of cancer.
化疗耐药是膀胱癌治疗失败的一个重要原因,鉴定赋予药物耐药性的基因是开发新的治疗策略以改善治疗效果的重要步骤。在本研究中,我们表明,吉西他滨联合顺铂(GEM/DDP)治疗诱导 NF-κB 信号通路,从而促进 p65 介导的 OIP5 的转录激活。OIP5 招募 E3 泛素连接酶 TRIP12 与其结合并降解磷酸酶 PPP1CB,从而增强 YBX1 的转录因子活性。这反过来又在上调 YBX1 转录控制下的药物耐药相关基因的表达,导致化疗耐药。此外,PPP1CB 的降解可以增强 IKKβ 的磷酸化活性,触发 NF-κB 信号级联反应,从而进一步刺激 OIP5 基因的表达,从而形成负反馈调节环。一致地,膀胱癌患者中 OIP5 表达升高与化疗耐药和预后不良相关。此外,我们使用基于 CRISPR/Cas9 的工程基因电路,该电路可以实时监测化疗耐药的进展,在检测到 NF-κB 信号增加时诱导 OIP5 敲除。该基因电路显著抑制了体内肿瘤细胞的生长,突出了基因治疗和化疗在癌症治疗中的协同作用的潜力。