Mitochondrial translocation of MDM2 and TFAM reprograms metabolism in treatment-refractory cancers
Tyrosine kinase inhibitors (TKI) are frontline therapies for oncogene-addicted cancers, yet metabolic rewiring frequently drives acquired resistance. Here, we identify a mitochondrial trafficking mechanism that regulates oxidative phosphorylation (OXPHOS) dependence in TKI-resistant tumours. Using resistant cell models and patient-derived materials, we demonstrate that OXPHOS activation is regulated by an AKT-driven, competitive interaction between mitochondrial MDM2 and the mitochondrial transcription factor TFAM at mitochondrial DNA (mtDNA). Mechanistically, adaptive AKT activation promotes cytosolic redistribution of MDM2 with reciprocal accumulation of TFAM in mitochondrial, enhancing mtDNA transcription and OXPHOS activity. To validate this mitochondrial-cytosolic exchange, we develop a quantitative, high-resolution imaging approach to map MDM2 and TFAM localization. In a TKI-resistant clinical cohort (n = 76), we revealed a positive correlation between AKT activation, MDM2 phosphorylation and TFAM mitochondrial trafficking, defining a spatial, subcellular biomarker signature of metabolically reprogrammed TKI resistance. Pharmacologic disruption of the AKT-MDM2-TFAM signaling axis reverse TKI resistance, linking mitochondrial genome regulation to therapy resistance and suggesting a metabolic vulnerability for combinatorial targeting.
Authors
- Tuan Zea Tan (ORCID: https://orcid.org/0000-0001-6624-1593)
- Susan Swee‐Shan Hue (ORCID: https://orcid.org/0000-0003-1854-1481)
- Azhar Ali (ORCID: https://orcid.org/0000-0002-5895-9076)
- Emiri O. Takaki (ORCID: https://orcid.org/0009-0009-8255-1917)
- Regina Tong Xin Wong
- L Wang
- Jie Qing Eu (ORCID: https://orcid.org/0009-0008-4219-3513)
- Jayshree L. Hirpara (ORCID: https://orcid.org/0000-0002-1454-9163)
- Shazib Pervaiz (ORCID: https://orcid.org/0000-0002-4738-019X)
- Nur Afiqah Binte Mohamed Salleh
- Dorothy Xi Yue Lim
- Boon-Cher Goh
- Yaw Chyn Lim
- Ju Ee Seet (ORCID: https://orcid.org/0000-0002-2024-5211)
- Li Ren Kong
- Andrea LA Wong
- Naoto Ohi
- Shu Jun Chan
Institutions
- Otsuka (Japan) (JP)
- National University of Singapore (SG)
- Nanyang Technological University (SG)
- Tan Tock Seng Hospital (SG)
- National University Cancer Institute, Singapore (SG)
- Duke-NUS Medical School (SG)
- National University Hospital (SG)
- National University Health System (SG)
Publication Details
- Journal
- npj Precision Oncology
- Published
- 2026-04-16
- DOI
- https://doi.org/10.1038/s41698-025-01257-1
- Primary Topic
- Cancer-related Molecular Pathways
- Type
- article
- Field-Weighted Citation Impact
- 0.00
Funders
- Otsuka Pharmaceutical
- National Medical Research Council
- Lee Kong Chian School of Medicine, Nanyang Technological University