Zhang Ning, Sun Linmao, Zhou Shuo, Ji Changyong, Cui Tianming, Chu Qi, Ye Jiareng, Liang Shuhang, Ma Kun, Liu Yufeng, Li Xianying, Guo Xinyu, Zhang Weizhi, Gu Xuetian, Cheng Cheng, Zha Qingrui, Tao Shengwei, Zhang Yunguang, Chu Junhui, Wu Chenghui, Zhang Yuchen, Wang Jiabei, Liu Yao, Liu Lianxin
Department of General Surgery, Key Laboratory of Hepatosplenic Surgery, Ministry of Education, The First Affiliated Hospital of Harbin Medical University, Harbin, China.
Department of Hepatobiliary Surgery, Centre for Leading Medicine and Advanced Technologies of IHM, The First Affiliated Hospital of USTC, Division of Life Sciences and Medicine, University of Science and Technology of China, Hefei, Anhui, China.
Nat Commun. 2025 Apr 3;16(1):3177. doi: 10.1038/s41467-025-58429-7.
Gemcitabine combined with cisplatin is the first-line chemotherapy for advanced cholangiocarcinoma, but drug resistance remains a challenge, leading to unsatisfactory therapeutic effect. Here, we elucidate the possibility of chemotherapy regimens sensitized by inhibiting succinylation in patients with cholangiocarcinoma from the perspective of post-translational modification. Our omics analysis reveals that succinylation of PDHA1 lysine 83, a key enzyme in the tricarboxylic acid cycle, alters PDH enzyme activity, modulates metabolic flux, and leads to alpha-ketoglutaric acid accumulation in the tumor microenvironment. This process activates the OXGR1 receptor on macrophages, triggering MAPK signaling and inhibiting MHC-II antigen presentation, which promotes immune escape and tumor progression. Moreover, we show that inhibiting PDHA1 succinylation with CPI-613 enhances the efficacy of gemcitabine and cisplatin. Targeting PDHA1 succinylation may be a promising strategy to improve treatment outcomes in cholangiocarcinoma and warrants further clinical exploration.
吉西他滨联合顺铂是晚期胆管癌的一线化疗方案,但耐药性仍然是一个挑战,导致治疗效果不尽人意。在此,我们从翻译后修饰的角度阐明了通过抑制琥珀酰化使胆管癌患者化疗方案敏感化的可能性。我们的组学分析表明,三羧酸循环中的关键酶PDHA1赖氨酸83的琥珀酰化改变了PDH酶活性,调节了代谢通量,并导致肿瘤微环境中α-酮戊二酸积累。这一过程激活了巨噬细胞上的OXGR1受体,触发MAPK信号传导并抑制MHC-II抗原呈递,从而促进免疫逃逸和肿瘤进展。此外,我们表明用CPI-613抑制PDHA1琥珀酰化可增强吉西他滨和顺铂的疗效。靶向PDHA1琥珀酰化可能是改善胆管癌治疗结果的一种有前景的策略,值得进一步的临床探索。