bims-meract Biomed News
on Metabolic reprogramming and anti-cancer therapy
Issue of 2026–03–29
fourteen papers selected by
Andrea Morandi, Università degli Studi di Firenze



  1. Leukemia. 2026 Mar 23.
      Mutations in NOTCH1, which occur in ~10% of Chronic Lymphocytic Leukemia (CLL) patients at diagnosis, are typically associated with unmutated (UM) B-cell receptor (BCR) subsets and define patients with earlier treatment need. Using primary CLL cells classified as NOTCH1 wild-type (CLL/NWT) or mutated (CLL/NM), both with UM-BCR, we show that BCR stimulation activates the NOTCH1 pathway, upregulating metabolic programs and mitochondrial biogenesis, selectively in CLL/NM. These cells display enhanced basal respiration and glycolysis, driven by higher mitochondrial mass, and further increase metabolic activity upon BCR triggering. To directly implicate NOTCH1 mutations, we engineered an MEC-1 model to generate wild-type (MEC-1/NWT) or mutated (MEC-1/NM) clones in a UM-BCR background. Here, NOTCH1 hyperactivation promoted mitochondrial metabolism through TFAM-dependent transcriptional control. Gene expression profiling, metabolic assays, and stable isotope tracing confirmed that MEC-1/NM cells rely on oxidative metabolism, with increased glutamine dependency and strengthened anabolic pathways, leading to augmented proliferation compared to MEC-1/NWT. Importantly, CLL/NM cells exhibit a marked vulnerability to glutamine deprivation. Combined inhibition of glutamine utilization and BCL2 triggered rapid apoptosis, providing a rationale for tailored therapeutic strategies in NOTCH1-mutated CLL. Representation of the molecular mechanism behind the metabolic reprogramming. BCR and NOTCH1 drive a dual metabolic reprogramming of glucose and glutamine pathways. In NOTCH1-mutated cells, both glucose and glutamine uptake are positively increased and even more upon BCR stimulation. Glucose is preferentially used to fuel the pentose phosphate pathway, and glutamine the TCA cycle. Concurrently, NICD accumulation, driven by BCR signaling, promotes TFAM expression and mitochondrial biogenesis. The resulting increase in mitochondrial mass underpins enhanced ATP production, oxygen consumption, and ROS generation, establishing a glutamine-dependent mitochondrial phenotype. This dependency sensitizes NOTCH1-mutated cells to glutamine blockade, which selectively induces apoptosis, further enhanced by combination with BCL-2 inhibition.
    DOI:  https://doi.org/10.1038/s41375-026-02912-7
  2. Proc Natl Acad Sci U S A. 2026 Mar 31. 123(13): e2525213123
      Metabolic reprogramming is a fundamental hallmark of cancer progression. However, the oncogenic mechanisms underlying serine metabolism and its impact on chemotherapeutic sensitivity in gastric cancer (GC) remain poorly defined. Here, through integrated metabolomics and 13C-labeled metabolic flux analysis, we identify marked dysregulation of serine metabolism in GC, primarily driven by increased expression of phosphoglycerate dehydrogenase (PHGDH). Mechanistically, we show that with no lysine kinase 1 (WNK1) phosphorylates PHGDH at Ser349 and Ser371, enhancing its enzymatic activity and protein stability by preventing ubiquitin-mediated degradation. In vivo, WNK1 knockout mice exhibit significantly reduced gastric tumor burden, accompanied by decreased serine levels and disrupted redox balance, supporting the protumorigenic role of the WNK1-PHGDH axis. Clinically, enhanced PHGDH activity, elevated serine levels, and increased glutathione abundance are strongly associated with poor oxaliplatin response in GC patient cohorts, suggesting PHGDH as a potential predictive biomarker for chemotherapy resistance. Together, these findings delineate a WNK1-PHGDH-driven serine metabolic reprogramming axis that promotes redox adaptation and chemoresistance in GC, highlighting its dual value as a mechanistic driver and a therapeutic vulnerability in cancer treatment.
    Keywords:  PHGDH; WNK1; oxaliplatin treatment; serine metabolism; therapeutic vulnerability
    DOI:  https://doi.org/10.1073/pnas.2525213123
  3. Cell Death Dis. 2026 Mar 25.
      Glioblastoma (GBM), the most common malignant brain tumor in adults, remains a highly lethal and incurable cancer, with a 5-year survival rate below 10%. Standard-of-care involves surgical resection followed by concurrent temozolomide chemotherapy and radiation treatment. While these interventions can effectively shrink tumors, they fail to eradicate all malignant cells. Small populations of GBM cells invariably survive and seed recurrent disease, leading to near-universal relapse and the formation of fatal recurrent tumors, typically within 1-2 years of treatment. Here, we investigated the metabolic features that define these surviving cell populations using ten patient-derived GBM models and matched orthotopic xenograft models exposed to a clinically relevant chemoradiotherapy regimen. By sampling living cells at defined treatment intervals and integrating 13C-glucose tracing, quantitative untargeted metabolomics, and nCounter metabolic gene expression profiling, we reconstructed the temporal evolution of glucose metabolism from therapy-naïve to post-treatment states. Across all models, GBM cells that evaded therapy-induced death exhibited a conserved and coordinated reorganization of glycolytic flux. These cells showed enhanced glucose uptake and elevated abundance of upper glycolytic enzymes such as HK1, while lower glycolytic enzymes, including ALDOA, GAPDH, ENO1, and LDHA, were suppressed, resulting in reduced lactate output. This bifurcation of glycolytic metabolism redirected carbon flux toward the pentose phosphate pathway and nucleotide biosynthesis, as well as mitochondrial metabolism, supported by the increased abundance of tricarboxylic acid cycle enzymes. Notably, these adaptations were conserved in recurrent patient-derived orthotopic xenograft tumors in vivo. Together, these findings reveal a fundamental and conserved metabolic state that defines GBM cells surviving chemoradiotherapy. This study deciphers a core metabolic architecture that enables tumor cell survival, persistence, and recurrence following therapy by shifting glycolytic flux away from lactate production to balance biosynthetic demands with mitochondrial metabolism.
    DOI:  https://doi.org/10.1038/s41419-026-08646-9
  4. Cell Death Dis. 2026 Mar 23.
      Melanoma accounts for over 85% of all skin cancer deaths. Current therapies including drugs targeting BRAF and MEK significantly improve the prognosis of metastatic melanoma patients, yet innate or acquired resistance challenges long-term responses. We have shown previously that fatty acid beta-oxidation (FAO) is up-regulated during the acquisition of BRAF-inhibitor (BRAFi) resistance and that the FDA approved drug ranolazine, by targeting FAO attenuates the development of acquired resistance. However, how ranolazine-induced metabolic rewiring increases cell death is unclear. Here we identify ranolazine as a ferroptosis inducer in BRAFi-resistant melanoma, in which FAO serves as a ferroptosis surveillance mechanism. Accordingly, in progressed tumours of BRAFi treated patients up-regulation of FAO regulators correlates with increased expression of ferroptosis markers. BRAFi resistant cells are heavily poised for execution of ferroptosis; they display reduced glutathione levels, higher levels of long-chain polyunsaturated fatty acid (PUFA) membrane-incorporation, and increased membrane-resident phospholipid oxidation, all of which is amplified by ranolazine. Counteracting ranolazine action is MBOAT1/2 mediated phospholipid remodelling, which initiates reduced PUFA membrane-incorporation as ferroptosis surveillance mechanism. We show that the androgen receptor (AR), which is a determinant of BRAFi resistance, controls MBOAT1/2 expression, thereby contributing to ferroptosis resistance. In BRAFi resistant tumours and cell lines, we confirm AR upregulation predominantly in the MITFlow/AXLhigh undifferentiated/neural-crest like state, but it also occurs in the MITFhigh/AXLlow differentiated melanocytic state. The AR antagonist enzalutamide sensitises AR expressing melanoma cells to RSL3 and erastin independent of phenotype state, but in FAOhigh BRAFi relapsed tumours AR up-regulation correlates with the undifferentiated/neural-crest like (UD/NC) state, and enzalutamide synergises with ranolazine in ferroptosis-induction in UD/NC cells. Thus, therapeutically combining ranolazine with the AR inhibitor enzalutamide to induce ferroptosis can circumvent dedifferentiation related BRAFi resistance and could increase therapeutic activity and long-term efficacy.
    DOI:  https://doi.org/10.1038/s41419-026-08578-4
  5. Cell Death Dis. 2026 Mar 24.
      Epithelial ovarian cancer (EOC) is the leading cause of death among gynecological malignancies, and the tumors with advanced-stage are frequently characterized by extensive metastasis. Although metabolic reprogramming of amino acids represents a hallmark of cancer, its specific role in the metastatic progression of EOC remains poorly understood. Here, we identified a critical metabolic vulnerability in omental metastasis of EOC. Despite defective endogenous synthesis, arginine accumulation depends on exogenous uptake. In vivo experiments demonstrated that dietary arginine deprivation suppressed tumor growth and metastasis, whereas supplementation or enhanced uptake of arginine promoted tumor cell proliferation, invasion, and migration in vitro. Mechanistically, increased arginine binds to the RNA helicase DDX3X, inducing nuclear retention of DDX3X and further promoting the transcription of DNA damage response (DDR)-related genes, thereby facilitating DDR through activating the ATM/CHK2/P53 axis to enable cancer cells to survive under metastatic stress. Notably, arginine restriction or pharmacological inhibition of DDX3X did effectively suppress both primary tumor growth and omental metastasis in mouse models. Collectively, our findings reveal that arginine is a metabolic vulnerability in omental metastasis of EOC, indicating that arginine restriction and DDX3X inhibition represent promising therapeutic strategies.
    DOI:  https://doi.org/10.1038/s41419-026-08606-3
  6. Neoplasia. 2026 Mar 20. pii: S1476-5586(26)00027-8. [Epub ahead of print]75 101298
       BACKGROUND: Hepatocellular carcinoma (HCC) exhibits high recurrence rates and limited therapeutic options. Endothelial cell-specific molecule 1 (ESM1) and angiopoietin-like 4 (ANGPTL4) are implicated in tumor progression, yet their synergistic role in HCC lipid metabolism and angiogenesis remains unexplored.
    METHODS: We integrated multi-omics approaches, including RNA sequencing, metabolomics, and immunoprecipitation-mass spectrometry, in HCC cell lines and patient-derived xenograft models. Key experiments involved Co-IP, Western blotting, tube formation assays, and clinical tissue microarray analysis to validate the ESM1-ANGPTL4-FASN-trioleate axis.
    RESULTS: ESM1 and ANGPTL4 formed a positive feedback loop, stabilizing fatty acid synthase (FASN) to promote trioleate synthesis. Trioleate activated the NF-κB/IL-17 pathway in HCC cells and upregulated CD99 in endothelial cells, driving angiogenesis. In vivo, ESM1/ANGPTL4 knockdown suppressed tumor growth, which was rescued by trioleate supplementation. Clinical data revealed elevated ESM1/ANGPTL4 expression in bevacizumab-resistant HCC, correlating with poor prognosis.
    CONCLUSIONS: The ESM1-ANGPTL4-FASN-trioleate axis orchestrates metabolic reprogramming and endothelial activation, representing a promising therapeutic target. Future studies should explore combination therapies targeting this axis and overcoming bevacizumab resistance in HCC.
    Keywords:  Cancer angiogenesis; ESM1-ANGPTL4 feedback; FASN; Metabolic reprogramming; Trioleate synthesis
    DOI:  https://doi.org/10.1016/j.neo.2026.101298
  7. Cell Rep. 2026 Mar 26. pii: S2211-1247(26)00235-4. [Epub ahead of print]45(4): 117157
      Ferroptosis is a lipid peroxidation-induced cell death mechanism that is regulated by amino acid metabolism. Cystine deprivation induces ferroptosis, but ferroptosis execution requires other amino acids. While methionine contributes to several metabolic pathways, including transsulfuration (TS), its role in ferroptosis remains controversial. Here, we report that methionine is required for ferroptosis triggered by cysteine deprivation. Notably, the TS pathway and methionine cycle in lung cancer cells are largely inactive, and methionine is instead funneled into polyamine synthesis via the methionine salvage route. Methionine depletion provokes metabolic shifts that dampen glutamine catabolism via the glutamine-methionine bi-cycle. Furthermore, methionine depletion alters phospholipid metabolism by promoting ACSL4 degradation, limiting polyunsaturated fatty acid (PUFA) incorporation into phospholipids. The methionine cycle intermediate S-adenosylmethionine (SAM) supplementation is sufficient to restore the perturbed metabolic state and ferroptosis sensitivity. Taken together, the results of this study highlight methionine as a key coordinator of ferroptosis through dynamic metabolic remodeling.
    Keywords:  ACSL4; CP: metabolism; CP: molecular biology; ferroptosis; glutaminolysis; methionine; methionine salvage pathway; phospholipid metabolism; transsulfuration pathway
    DOI:  https://doi.org/10.1016/j.celrep.2026.117157
  8. Sci Immunol. 2026 Mar 27. 11(117): eaeb1459
      Lipid accumulation in the tumor microenvironment is a hallmark of solid tumors, with increased palmitate (PA) availability fostering tumor progression. Although PA's direct effects on cancer cells are well described, its impact on CD8 T cells [cytotoxic T lymphocytes (CTLs)] remains unclear. Here, we show that PA irreversibly impairs CTL mitochondrial metabolism, leading to the loss of effector functions and compromised antitumor immunity. PA-induced mitochondrial dysfunction reduced histone acetylation and chromatin accessibility, suppressing transcription of genes involved in T cell replication and effector programs. We identified sphingosine kinase 2 (SPHK2) as a key mediator of PA-induced dysfunction, with pharmacological inhibition of SPHK2 restoring mitochondrial fitness, rescuing CTL effector function, and promoting antitumor activity. These findings uncover a distinct mechanism by which PA drives immune evasion in tumors and highlight SPHK2 as a potential therapeutic target to enhance T cell-based immunotherapies.
    DOI:  https://doi.org/10.1126/sciimmunol.aeb1459
  9. Cell Death Discov. 2026 Mar 26.
      Microplastics and nanoplastics are commonly found in our everyday environments. So far, microplastics and nanoplastics have been detected in various tissues and bodily fluids, including hair, sputum, digestive tissue, lungs, blood, placental and endometrial tissue. Although some studies indicate that microplastics and nanoplastics can promote tumor development, their impact on endometrial cancer (EC) remains unclear. In this study, we examined the effect of polystyrene nanoplastics (PS-NPs) on EC development and explored the underlying pathogenic mechanisms. We observed the uptake and accumulation of PS-NPs in HEC-1B cells and EC organoids. Through cell and organoid experiments as well as mouse models, we demonstrated that PS-NP exposure can accelerate EC progression in vitro and in vivo. Next, through transcriptomic sequencing and targeted metabolomic sequencing, We found that adenosine 5'-monophosphate-activated protein kinase (AMPK) can activate ACSS2 and promote its nuclear translocation. The nuclear entry of ACSS2 is associated with increased levels of H3K9 acetylation, which may be a potential mechanism through which it regulates PLA2G3 expression. PLA2G3 mRNA levels are upregulated, increasing the production of arachidonic acid (AA), and ultimately leads to the epithelial-mesenchymal transition (EMT) in EC cells. The relevant molecular markers in this study can provide new strategies for early warning and targeted intervention, reducing the potential impact of PS-NPs on EC.
    DOI:  https://doi.org/10.1038/s41420-026-03071-5
  10. Cell Death Dis. 2026 Mar 25.
      Hepatocellular carcinoma (HCC) is the most prevalent hepatic malignancy worldwide, accounting for approximately 90% of all primary liver cancer cases. However, the mechanisms involving in liver tumorigenesis and drug resistance remain unclear, largely restricting the clinical management of HCC. Here, we first evaluated the clinical significance of malic enzyme 1 (ME1) in HCC patients and revealed that ME1 was significantly upregulated in tumor tissues and positively correlated with poor prognosis. Gain- and loss-of-function experiments suggested that ME1 promoted HCC cell viability in vitro. Consistently, hepatocyte-specific Me1 knockout (Me1HKO) mice treated with diethylnitrosamine (DEN) showed reduced tumor burden as compared to Me1Flox mice. In addition, ME1 overexpression conferred resistance to the first-line therapeutic drug lenvatinib, while knockout of ME1 restored drug sensitivity in lenvatinib-resistant HCC cells. Mechanistically, we showed that ME1 could regulate ferroptosis of HCC cells through its function on NADPH production. We further identified ferroptosis suppressor protein 1 (FSP1) as a key downstream effector, which utilized ubiquinol (CoQH2) as a lipophilic radical-trapping antioxidant to block the accumulation of lipid peroxides to pro-ferroptotic levels. In summary, our findings demonstrated that ME1 promotes HCC progression by activating the NADPH-FSP1-CoQH2 axis and thereby inhibiting ferroptosis, suggesting a promising therapeutic strategy for HCC treatment.
    DOI:  https://doi.org/10.1038/s41419-026-08572-w
  11. J Exp Clin Cancer Res. 2026 Mar 26.
      
    Keywords:  Chemosensitivity; Combination therapy; Complex I; ETC; Melanoma; Metabolic reprogramming; Mitochondria; OXPHOS; TCA cycle
    DOI:  https://doi.org/10.1186/s13046-026-03685-8
  12. Front Immunol. 2026 ;17 1782047
       Background: Chemotherapy resistance is the main obstacle to breast cancer recurrence, metastasis, and mortality. Drug-tolerant persister (DTP) cells are a novel type of target cell associated with tumor resistance, and autophagy is a key factor in maintaining the survival of tumor DTP cells. However, it is unclear whether the activation of autophagy in breast cancer DTP cells is related to their overexpression of the transcriptional regulatory factor CDCA7.
    Methods: We analyzed CDCA7 expression using public datasets and clinical samples and established breast cancer cell lines with CDCA7 overexpression and knockdown to assess the role of CDCA7 in breast cancer. Autophagy was assessed via electron microscopy, mRFP-GFP-LC3 imaging, and immunoblotting. Mechanistic studies employed ChIP-seq, dual-luciferase assays, and site-directed mutagenesis. Functional assays measured chemosensitivity (CCK-8), migration/invasion (scratch/Transwell), and in vivo tumorigenicity (mouse xenograft).
    Results: CDCA7 was significantly upregulated in breast cancer DTP cells. Overexpression of CDCA7 in breast cancer cells significantly enhanced autophagy-related biological processes and molecular functions. Through ChIP-seq and targeted knockout experiments, we identified the binding sites of CDCA7 on the autophagy-related protein genes ULK1, ATG2A, and ATG3. Using transmission electron microscopy and mRFP/mCherry-GFP-LC3B tandem fluorescent tagging, we observed that CDCA7 knockdown significantly reduced the number of autolysosomes in breast cancer DTP cells and markedly inhibited autophagic flux. Moreover, CDCA7 knockdown not only decreased drug resistance in breast cancer cells but also reduced metastasis, invasion, and tumorigenic ability in vivo, ultimately prolonging the survival of tumor-bearing mice.
    Conclusion: CDCA7 drives breast cancer chemoresistance by transcriptionally activating a pro-survival autophagy program in DTP cells, nominating it as a promising therapeutic target.
    Keywords:  CDCA7; autophagy; breast cancer; drug-tolerant persister state; transcriptional regulation
    DOI:  https://doi.org/10.3389/fimmu.2026.1782047
  13. Cell Death Discov. 2026 Mar 27.
      Mitochondria play a central role in metastatic spread and cancer progression, with the IκBα/NF-κB signaling axis acting as a key regulator of both processes. We suggest that a stable fraction of IκBα localizes to mitochondria, where it escapes proteasomal degradation and acquires oncogenic functions independent of its canonical role in NF-κB inhibition. Using engineered A549 lung cancer cells with enforced mitochondrial localization of IκBα (IκBα-MTS), we show that the IκBα mitochondrial pool promotes increased cell proliferation, enhanced migration, and resistance to chemotherapy-induced apoptosis, along with a metabolic reprogramming characterized by elevated glycolysis and lactate secretion. These changes activated endothelial cells (ECs) and triggered cancer-associated thrombosis (CAT). This prothrombotic state, marked by elevated vWF a potent trigger for platelet adhesion and activation, contributed to an environment favorable for metastatic dissemination. Our findings reveal mitochondrial IκBα as a key mediator in mitochondrial stress, endothelial activation, and thrombo-inflammatory mechanisms that drive lung cancer progression.
    DOI:  https://doi.org/10.1038/s41420-026-03022-0
  14. Eur J Pharmacol. 2026 Mar 25. pii: S0014-2999(26)00282-7. [Epub ahead of print] 178800
      In a compound screen on melanoma cells, we identified FX-11 as one of the compounds inhibiting the growth of sensitive and Encorafenib/Binimetinib-resistant 624Mel and Wm3248 melanoma cells. FX-11, reported to be a lactate dehydrogenase inhibitor (LDHi), did not decrease the NAD+/NADH ratio, glucose uptake, or lactate secretion of melanoma cells, unlike other LDH inhibitors we used as controls. Instead, FX-11 increased both the oxygen consumption and the extracellular acidification rate of cells in Seahorse assays, behaving similarly to the mitochondrial uncouplers FCCP and BAM15. FX-11 could also be used as an uncoupler in Mito Stress tests. In addition, FX-11 and BAM15 drastically decreased the mitochondrial membrane potential, in contrast to the LDH inhibitors LDH-IN-I and GNE-140. Finally, FX-11 treatment induced an increase in AMPK and acetyl-CoA carboxylase (ACC) phosphorylation and a decrease in phosphorylation of the eukaryotic initiation factor 4E-binding protein 1 (4E-BP1), indicative of AMPK activation by decreased ATP/AMP ratio. The observed AMPK activation seems to be involved in FX-11-mediated cell death since knock-down of AMPKα1 reduced cell death. Specific activation of AMPK by MK8722, on the other hand, increased cell death. Taken together, we provide evidence that FX-11 inhibits the growth of melanoma cells, including drug-resistant ones, through an AMPK-dependent mechanism by acting as a mitochondrial uncoupler. Our data do not support that FX-11 acts as an LDH inhibitor.
    Keywords:  AMPK; FX-11; lactate dehydrogenase inhibitor; mTOR; melanoma; metabolism; mitochondrial uncoupling
    DOI:  https://doi.org/10.1016/j.ejphar.2026.178800