Yang Jianqiang, Chen Fanghui, Fu Zhenzhen, Yang Fan, Saba Nabil F, Teng Yong
Department of Hematology and Medical Oncology, Emory University, Atlanta, Georgia.
Winship Cancer Institute of Emory University, Atlanta, Georgia.
Cancer Res. 2025 Jun 2;85(11):2014-2026. doi: 10.1158/0008-5472.CAN-24-3477.
The tricarboxylic acid (TCA) cycle is often rewired or dysregulated to meet the increased energy and biosynthetic demands of rapidly dividing cancer cells, and targeting the TCA cycle is a potential therapeutic strategy for treating cancer. However, tumor cell metabolism can impact other cells in the tumor microenvironment, and disrupting the TCA cycle in cancer cells could impact the antitumor immune response. In this study, using CPI-613 as a model drug for TCA cycle inhibition, we identified a molecular mechanism by which blocking the TCA cycle enhances T-cell-mediated antitumor immunity in the context of head and neck squamous cell carcinoma (HNSCC). Impairment of mitochondrial metabolism by CPI-613 induced endoplasmic reticulum stress in HNSCC cells, leading to increased expression of spliced X-box-binding protein 1. This, in turn, directly suppressed the transcriptional activity of the thrombospondin-2 gene. Correspondingly, CPI-613 reduced the secretion of thrombospondin-2 from HNSCC cells, enhancing the proliferation and cytotoxic potential of tumor-infiltrating CD36+CD8+ T cells by upregulating AKT-mTOR signaling. This mechanism ultimately enhanced antitumor immunity in a syngeneic mouse model of orthotopic HNSCC following CPI-613 treatment. These findings uncover the immunomodulatory role of the TCA cycle in cancer cells and suggest that targeting it is a promising approach to harness tumor-reactive immune cells. Significance: The immunomodulatory role of the TCA cycle in cancer cells provides a therapeutic opportunity to enhance antitumor immunity by targeting tumor cell metabolism.
三羧酸(TCA)循环常常被重新布线或失调,以满足快速分裂的癌细胞对能量和生物合成的增加需求,靶向TCA循环是治疗癌症的一种潜在治疗策略。然而,肿瘤细胞代谢会影响肿瘤微环境中的其他细胞,破坏癌细胞中的TCA循环可能会影响抗肿瘤免疫反应。在本研究中,我们使用CPI-613作为抑制TCA循环的模型药物,确定了一种分子机制,即阻断TCA循环可在头颈部鳞状细胞癌(HNSCC)背景下增强T细胞介导的抗肿瘤免疫。CPI-613对线粒体代谢的损害诱导了HNSCC细胞中的内质网应激,导致剪接的X盒结合蛋白1表达增加。这反过来又直接抑制了血小板反应蛋白-2基因的转录活性。相应地,CPI-613减少了HNSCC细胞中血小板反应蛋白-2的分泌,通过上调AKT-mTOR信号增强了肿瘤浸润性CD36+CD8+T细胞的增殖和细胞毒性潜力。该机制最终在CPI-613治疗后的原位HNSCC同基因小鼠模型中增强了抗肿瘤免疫。这些发现揭示了TCA循环在癌细胞中的免疫调节作用,并表明靶向它是利用肿瘤反应性免疫细胞的一种有前景的方法。意义:TCA循环在癌细胞中的免疫调节作用为通过靶向肿瘤细胞代谢增强抗肿瘤免疫提供了治疗机会。