Targeting LDHA Palmitoylation Sensitizes GBM to Chemoradiotherapy via Suppressing Palmitic Acid Induced Glycolytic Reprogramming

Glioblastoma (GBM) is a lethal malignancy characterized by therapeutic resistance and recurrence, which are driven by dynamic cellular metabolic adaptation within the tumor microenvironment. However, the precise molecular metabolic mechanisms remain poorly understood. Here, we found that palmitic acid (PA) accumulates in hypoxic pseudopalisading regions of GBM and drives the formation of mesenchymal (MES) GBM and the hypoxia myeloid-derived macrophages (MDM) subpopulation, establishing an interactive tumor-promoting niche that fuels GBM recurrence. Maechanistically, PA induces ZDHHC12-mediated palmitoylation of lactate dehydrogenase A (LDHA) at cysteine 163. This enhances LDHA enzymatic activity, promoting glycolytic reprogramming that reinforces the MES phenotype and confers resistance to chemoradiotherapy. Concurrently, palmitoylation facilitates the exosomal sorting of LDHA, which is internalized by MDMs, inducing their polarization into an immunosuppressive, glycolytic hypoxia-MDM subset, which cooperatively shapes an immunosuppressive pseudopalisading niche with MES glioma stem cells to promote GBM recurrence. Critically, we identified the small molecule Rutin as a potent inhibitor of LDHA-Cys163 palmitoylation, thereby re-sensitizing GBM to chemoradiotherapy. This study defines a metabolic circuit in recurrent GBM driven by crosstalk between PA-activated MES-GBM cells and hypoxia-MDMs. The small molecule Rutin disrupts this circuit, re-sensitizing GBM to chemoradiotherapy and offering a promising strategy to overcome post-treatment recurrence.

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Publication Details

Journal
Advanced Science
Published
2026-09-28
DOI
https://doi.org/10.1002/advs.77536
Primary Topic
Cancer, Hypoxia, and Metabolism
Type
article
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article

Targeting LDHA Palmitoylation Sensitizes GBM to Chemoradiotherapy via Suppressing Palmitic Acid Induced Glycolytic Reprogramming

Ziwen Pan, Rongrong Zhao, Hao Xue, Huize Xia et al.
Advanced Science
Cancer, Hypoxia, and Metabolism
article

Targeting LDHA Palmitoylation Sensitizes GBM to Chemoradiotherapy via Suppressing Palmitic Acid Induced Glycolytic Reprogramming

Ziwen Pan, Rongrong Zhao, Hao Xue, Huize Xia, Q. A. Wang, Shulin Zhao, Yanhua Qi, Xu Qian, Gang Li, Boyan Li, Xing Guo, Weijie Tang, Zheyuan Chen, Zijie Gao, Hongyu Zhao, Zhe Han, Ruochuan Li, Jiawei Qiu, Ping Zhang, Huanyu Yang, Jixing Zhao
article en

Abstract

Glioblastoma (GBM) is a lethal malignancy characterized by therapeutic resistance and recurrence, which are driven by dynamic cellular metabolic adaptation within the tumor microenvironment. However, the precise molecular metabolic mechanisms remain poorly understood. Here, we found that palmitic acid (PA) accumulates in hypoxic pseudopalisading regions of GBM and drives the formation of mesenchymal (MES) GBM and the hypoxia myeloid-derived macrophages (MDM) subpopulation, establishing an interactive tumor-promoting niche that fuels GBM recurrence. Maechanistically, PA induces ZDHHC12-mediated palmitoylation of lactate dehydrogenase A (LDHA) at cysteine 163. This enhances LDHA enzymatic activity, promoting glycolytic reprogramming that reinforces the MES phenotype and confers resistance to chemoradiotherapy. Concurrently, palmitoylation facilitates the exosomal sorting of LDHA, which is internalized by MDMs, inducing their polarization into an immunosuppressive, glycolytic hypoxia-MDM subset, which cooperatively shapes an immunosuppressive pseudopalisading niche with MES glioma stem cells to promote GBM recurrence. Critically, we identified the small molecule Rutin as a potent inhibitor of LDHA-Cys163 palmitoylation, thereby re-sensitizing GBM to chemoradiotherapy. This study defines a metabolic circuit in recurrent GBM driven by crosstalk between PA-activated MES-GBM cells and hypoxia-MDMs. The small molecule Rutin disrupts this circuit, re-sensitizing GBM to chemoradiotherapy and offering a promising strategy to overcome post-treatment recurrence.

Advanced Science
Shandong University (CN), Shandong Provincial Hospital (CN), Qilu Hospital of Shandong University (CN), Shandong First Medical University (CN), Nanjing Medical University (CN)
Good health and well-being
Openalex Percentile: Top 16%
Cancer, Hypoxia, and Metabolism
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