Shao Wei-Qing, Li Yi-Tong, Zhou Xu, Zhang Sheng-Guo, Fan Ming-Hao, Zhang Dong, Chen Zhen-Mei, Yi Chen-He, Wang Sheng-Hao, Zhu Wen-Wei, Lu Ming, Chen Ji-Song, Lin Jing, Zhou Yu
Department of General Surgery Huashan Hospital & Cancer Metastasis Institute, Fudan University, Shanghai, 200040, China.
Department of Infection, The Third Affiliated Hospital of Wenzhou Medical University, Zhejiang, 325000, China.
Mol Cell Biochem. 2025 Mar;480(3):1807-1818. doi: 10.1007/s11010-024-05106-w. Epub 2024 Sep 4.
The degradation of proteasomes or lysosomes is emerging as a principal determinant of programmed death ligand 1 (PDL1) expression, which affects the efficacy of immunotherapy in various malignancies. Intracellular cholesterol plays a central role in maintaining the expression of membrane receptors; however, the specific effect of cholesterol on PDL1 expression in cancer cells remains poorly understood. Cholesterol starvation and stimulation were used to modulate the cellular cholesterol levels. Immunohistochemistry and western blotting were used to analyze the protein levels in the samples and cells. Quantitative real-time PCR, co-immunoprecipitation, and confocal co-localization assays were used for mechanistic investigation. A xenograft tumor model was constructed to verify these results in vivo. Our results showed that cholesterol suppressed the ubiquitination and degradation of PDL1 in hepatocellular carcinoma (HCC) cells. Further mechanistic studies revealed that the autocrine motility factor receptor (AMFR) is an E3 ligase that mediated the ubiquitination and degradation of PDL1, which was regulated by the cholesterol/p38 mitogenic activated protein kinase axis. Moreover, lowering cholesterol levels using statins improved the efficacy of programmed death 1 (PD1) inhibition in vivo. Our findings indicate that cholesterol serves as a signal to inhibit AMFR-mediated ubiquitination and degradation of PDL1 and suggest that lowering cholesterol by statins may be a promising combination strategy to improve the efficiency of PD1 inhibition in HCC.
蛋白酶体或溶酶体的降解正逐渐成为程序性死亡配体1(PDL1)表达的主要决定因素,而这会影响各种恶性肿瘤免疫治疗的疗效。细胞内胆固醇在维持膜受体表达方面起着核心作用;然而,胆固醇对癌细胞中PDL1表达的具体影响仍知之甚少。利用胆固醇饥饿和刺激来调节细胞胆固醇水平。采用免疫组织化学和蛋白质印迹法分析样本和细胞中的蛋白质水平。运用定量实时聚合酶链反应、免疫共沉淀和共聚焦共定位分析进行机制研究。构建异种移植肿瘤模型以在体内验证这些结果。我们的结果表明,胆固醇抑制了肝细胞癌(HCC)细胞中PDL1的泛素化和降解。进一步的机制研究表明,自分泌运动因子受体(AMFR)是一种E3连接酶,介导了PDL1的泛素化和降解,其受胆固醇/p38丝裂原活化蛋白激酶轴调控。此外,使用他汀类药物降低胆固醇水平可提高体内程序性死亡1(PD1)抑制的疗效。我们的研究结果表明,胆固醇作为一种信号抑制AMFR介导的PDL1泛素化和降解,并表明他汀类药物降低胆固醇可能是提高HCC中PD1抑制效率的一种有前景的联合策略。