bims-medica Biomed News
on Metabolism and diet in cancer
Issue of 2026–03–29
ten papers selected by
Brett Chrest, Wake Forest University



  1. Cell Metab. 2026 Mar 24. pii: S1550-4131(26)00093-8. [Epub ahead of print]
      Lactate has been proposed to enter mitochondria and fuel respiration, but this "intracellular lactate shuttle" remains controversial. Using genetically encoded lactate and redox sensors in cultured cells and neurons in vivo, we identify a dynamic lactate pool within the mitochondrial matrix that tracks extracellular and blood lactate and promotes lactylation of mitochondrial proteins. Lactate crosses the inner mitochondrial membrane through a saturable pathway that is partly sensitive to pharmacologic and genetic inhibition of the mitochondrial pyruvate carrier (MPC). Despite transport and matrix lactate dehydrogenase activity, lactate does not measurably energize the electron transport chain under the conditions tested. Instead, energized mitochondria can produce lactate from pyruvate, a response enhanced by hypoxia. Blocking MPC causes matrix lactate and H₂O₂ accumulation, revealing a rapid lactate-based "vent" that modulates matrix energy and reactive oxygen species.
    Keywords:  genetically encoded fluorescent indicator; hypoxia; lactate; lactate dehydrogenase; membrane transport; metabolism; mitochondrial pyruvate carrier; monocarboxylate transporter; pyruvate; reactive oxygen species
    DOI:  https://doi.org/10.1016/j.cmet.2026.02.020
  2. 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
  3. Biomedicines. 2026 Mar 14. pii: 667. [Epub ahead of print]14(3):
      Background/Objectives: Acute myeloid leukemia (AML) remains a hematologic malignancy with poor prognosis. The neddylation inhibitor MLN4924 has demonstrated potent anti-leukemic activity in preclinical models, yet its clinical translation faces significant challenges. The aim of this study was to explore combination therapy strategies that could further enhance MLN4924's anti-leukemia potential. Methods: AML cell lines used in this study were Kasumi-1 and MOLM-13. Cell viability was assessed using CCK-8 assays. mRNA and protein expression levels were determined through RT-qPCR and Western blot, respectively. Flow cytometry was employed to analyze surface markers (SLC1A5, CD11b, CD14, CD16), mitochondrial membrane potential (JC-1), and apoptosis (Annexin V-FITC/PI). In vivo efficacy was validated using an NCG mouse xenograft model. Transcriptomic profiling was performed to explore the potential mechanism by which MLN4924 in combination with V9302 inhibits leukemia. Results: Treatment with MLN4924 significantly upregulated key glutamine metabolic proteins, GLUL and the glutamine transporter SLC1A5, in AML cells. Knockdown of SLC1A5 significantly enhanced AML cell sensitivity to MLN4924. The combination of MLN4924 and the SLC1A5 inhibitor V9302 synergistically inhibited AML cell proliferation, induced monocytic differentiation, and promoted apoptosis. Transcriptomic analysis revealed that this combination therapy prominently suppressed the tricarboxylic acid (TCA) cycle. Conclusions: Neddylation inhibition induces compensatory upregulation of glutamine metabolism in AML. Co-targeting neddylation and glutamine transporter SLC1A5 synergistically exerts anti-leukemic effects, at least in part through disruption of the TCA cycle. This combination represents a novel and effective therapeutic strategy against AML.
    Keywords:  GLUL; MLN4924; SLC1A5; V9302; acute myeloid leukemia; glutamine metabolism; neddylation
    DOI:  https://doi.org/10.3390/biomedicines14030667
  4. Anticancer Res. 2026 Apr;46(4): 1875-1882
       BACKGROUND/AIM: In the present study we compared the glucose and glutamine requirements of cancer and normal cells to determine if the Warburg effect is cancer specific.
    MATERIALS AND METHODS: 143B human osteosarcoma, HT1080 human fibrosarcoma, HCT116 human colon cancer and normal Hs27 human fibroblasts were cultured in Dulbecco's modified Eagle's medium (DMEM) with and without glucose; with and without glutamine; or with and without methionine. The EC50 of glucose, glutamine and methionine was compared in cancer and normal cells. Co-culture of Hs27 normal fibroblast with each cancer cell line was performed by using 12-well plates with and without glucose or methionine. Cell viability was determined with the WST-8 viability reagent, by phase-contrast microscopy or fluorescence microscopy.
    RESULTS: The EC50 of glucose for the three cancer cell lines ranged from 0.54 to 4.88 mM. The EC50 of glucose for Hs27 normal fibroblasts was 0.35 mM, which was not significantly lower than in HCT116 cells (p=0.2225). The EC50 for glutamine ranged from 0.15 to 0.54 mM for the cancer-cell lines and 0.24 mM for normal fibroblasts, which did not distinguish normal from cancer cells. For comparison the EC50 of cancer cells for methionine ranged from 3.8 μM to 21.4 μM while for normal fibroblasts the EC50 for methionine was 2.3 μM, which was significantly lower than in all the cancer cell lines (p<0.0167). In co-culture of cancer and normal fibroblasts, glucose-free or glutamine-free medium resulted in loss of cell viability by day 7 for both the cancer and normal cells. In contrast, in methionine-free medium, the normal fibroblasts were alive and healthy at day 7.
    CONCLUSION: The Warburg effect of glucose and glutamine addiction is not cancer specific in comparison to methionine addiction (Hoffman effect), which is cancer specific, suggesting the Warburg effect is not a cancer paradigm.
    Keywords:  Glucose; Hoffman effect; Warburg effect; cancer cells; cancer-specific; co-culture; glutamine; methionine; normal fibroblasts; paradigm; requirement; vulnerability
    DOI:  https://doi.org/10.21873/anticanres.18080
  5. Cell Death Discov. 2026 Mar 24.
      Autophagy induction has recently emerged as a mechanism of resistance to FLT3 inhibitors (FLT3i) in patients with FLT3-ITD mutant acute myeloid leukemia (AML). Here, we assessed the molecular mechanisms of autophagy inhibition associated with FLT3i and its impact on cell survival and pharmacological resistance. In FLT3-ITD AML cell lines (MOLM13 and MV4-11), treatment with first- and second-generation FLT3i (midostaurin and quizartinib, respectively) induced autophagy. Combining FLT3i with autophagy inhibitors further decreased cell viability and increased cell apoptosis in both cell lines and in primary patient samples. Label-free quantification proteomics of MOLM13 cells revealed that RFC4 (Replication Factor C Subunit 4), an autophagy regulator linked to increased chemosensitivity, and GATD3/C21orf33 (Glutamine Amidotransferase Class 1 Domain Containing 3) proteins were upregulated only in the combined group, while 11 proteins mostly associated with chemoresistance were downregulated. In vivo, the combination of midostaurin and autophagy inhibition improved overall survival in MOLM13-transplanted mice. ATG5- (Autophagy Related 5) and ATG7-knockdown (Autophagy Related 7) increased sensitivity to first- and second-generation FLT3i in MOLM13 cells. To investigate the potential of autophagy inhibition in overcoming FLT3i resistance, we generated MV4-11 cells resistant to quizartinib (MV4-11QR). The resistant cell line exhibited higher basal levels of autophagy compared to the parental cell line. The combination of quizartinib and chloroquine demonstrated a synergistic effect in MV4-11QR cells and this effect was associated with greater inhibition of the FLT3 receptor compared to the monotherapies. Therefore, combining FLT3i with autophagy inhibition enhances the FLT3i antileukemic efficacy and overcomes pharmacological resistance.
    DOI:  https://doi.org/10.1038/s41420-026-03037-7
  6. bioRxiv. 2026 Mar 18. pii: 2026.03.16.712182. [Epub ahead of print]
      Cancer cell dissemination critically determines clinical prognosis, yet metabolic dependencies and corresponding therapeutic targets during spread of lymphoid malignancies remain poorly understood. Here we show that the pyruvate branch point operates as a metabolic checkpoint for lymphoid cancer cell migration and disease dissemination through mitochondrial ROS (mROS)/HIF-1a signaling. Isolation of highly migratory mROS hi cells led us to identify selective metabolic requirements of malignant lymphocyte migration and disease dissemination. Highly migratory cells show a reprogrammed metabolic profile characterized by increased glucose uptake and reduced glucose-carbon entry into the TCA cycle. Reprogramming of the TCA cycle with downregulation of citrate synthase provide the mechanistic basis for decreased pyruvate oxidation leading to increased migration and disease dissemination through mROS/HIF-1a signaling. Our findings connect central carbon metabolism and migratory capacity of lymphoid cancer cells and identify the pyruvate branch point as a metabolic switch and potential therapeutic target in lymphoid cancer cell dissemination.
    DOI:  https://doi.org/10.64898/2026.03.16.712182
  7. Oncogenesis. 2026 Mar 26.
      Proliferating cancer cells reprogramme metabolism to secure nucleotides and other macromolecules required for biomass accumulation and genome duplication. Beyond serving as DNA/RNA precursors, nucleotides act as energy currencies, second messengers, glycosyl donors, and modulators of cytoskeletal dynamics; sustaining adequate pools is therefore indispensable for tumour growth and progression. Oncogenic lesions, such as loss of TP53 or LKB1, hyperactive PI3K-AKT-mTORC1, and MYC or RAS, coordinate transcriptional programmes, substrate transport, and post-translational control of rate-limiting enzymes to elevate de novo purine and pyrimidine synthesis and shape salvage use. These circuits integrate glycolysis, the pentose-phosphate pathway, folate-dependent one-carbon metabolism, and glutamine/aspartate provisioning to channel carbon and nitrogen into ring assembly. In this review, we organize this landscape into an environment-shaped routing model that explains when tumours favour de novo versus salvage and how therapies reroute flux. We synthesise current mechanisms by which oncogenes and tumour suppressors regulate nucleotide synthesis in cancer and outline therapeutic implications, including inhibitors of pathway enzymes (e.g., DHODH, IMPDH), strategies that restrict precursor availability, and rational combinations with targeted agents or DNA-damaging therapies to exploit replication stress and metabolic vulnerabilities. Together, these insights highlight nucleotide metabolism as a central, drug-responsive nexus linking oncogenic signalling to malignant proliferation.
    DOI:  https://doi.org/10.1038/s41389-026-00608-2
  8. Cell Death Dis. 2026 Mar 26.
      Most tumors exhibit increased glucose uptake and reprogram metabolism to aerobic glycolysis to meet their demands for macromolecule biosynthesis and energy production. Consequently, PET/CT using 18F-2-fluoro-2-deoxy-D-glucose (18F-FDG-PET/CT) has been developed and is clinically utilized in cancer imaging diagnostics. However, numerous cancers demonstrate negative imaging during 18F-FDG-PET/CT detection, suggesting these cancers employ alternative metabolic rewiring. In this study, we discovered that 18F-FDG-PET/CT-negative gastric cancers coordinate glutamine-based gluconeogenesis and fatty acid oxidation to meet DNA and ATP demands, sustaining tumor growth despite low glucose uptake. PCK and CPT1A, the key enzymes which are responsible for remodeling the metabolism, were highly expressed in FDG-PET/CT-negative gastric cancers. Accordingly, PCK/CPT1A negatively correlated with 18F-FDG imaging levels and positively correlated with poorer clinical classifications. Mechanistically, PPARγ is highly expressed in FDG-PET/CT-negative cells and drives the transcription of the PCK and genes. Pharmacological inhibition of the PCK/CPT1A significantly suppressed tumor growth in 18F-FDG-PET/CT-negative gastric cancers, as demonstrated in both cell-derived xenograft (CDX) and patient-derived xenograft (PDX) models. Together, these results highlight the heterogeneity of tumor cells from metabolic perspective, and identify PCK/CPT1A as a target for metabolic reprogramming and precision therapy of 18F-FDG-PET/CT-negative cancers.
    DOI:  https://doi.org/10.1038/s41419-026-08662-9
  9. Mol Cancer Ther. 2026 Mar 17.
      This study tested the hypothesis that tumor cells can evade apoptosis following BH3 mimetic treatment by utilizing alternative Bim binding partners. Levels of Bim heterodimers with Mcl-1, Bcl-2 and Bcl-xL were measured in multiple hematologic cell line xenograft models (AMO-1, MV4-11, and RPMI-8226) following single-dose S63845 or venetoclax; Bak-Bax heterodimer and cleaved caspase-3 (cCasp3) levels were measured to demonstrate mitochondrial apoptosis. Anti-tumor efficacies of these agents were measured in vivo in mice bearing AMO-1 or MV4-11 xenografts and in vitro in patient-derived lymphoblastoid-like cells. Mechanism of combination activity of the CDC-like kinase (CLK) inhibitor cirtuvivint with venetoclax was determined in MV4-11 and KG-1a xenografts. S63845 decreased Mcl-1-Bim levels in AMO-1 and MV4-11 tumors by ~90% while unexpectedly decreasing Bcl-2-Bim and increasing Bcl-xL-Bim levels. Venetoclax decreased Bcl-2-Bim levels while increasing Mcl-1-Bim and Bcl-xL-Bim levels in MV4-11 tumors. The S63845+venetoclax combination decreased Mcl-1-Bim levels and demonstrated greater cell killing activity and pharmacodynamic effects than either single agent in multiple models including patient-derived lymphoblastoid-like cells. Cirtuvivint decreased Mcl-1 and Bim levels, combining with venetoclax to induce significantly greater Bak-Bax and cCasp3 responses than either single agent and induced regression of MV4-11 xenograft tumors. Our results elucidate quantitative pharmacodynamics of S63845, venetoclax, and cirtuvivint, an agent that is currently being evaluated with venetoclax to treat AML (NCT06484062). Compensatory increases in off-target Bim heterodimer levels in response to either S63845 or venetoclax offer a possible mechanism of clinical drug resistance.
    DOI:  https://doi.org/10.1158/1535-7163.MCT-25-0855
  10. Neurol Int. 2026 Feb 24. pii: 40. [Epub ahead of print]18(3):
      Purpose: Glioblastoma multiforme (GBM) is a highly aggressive cancer with limited survival despite current treatments. Rising treatment costs highlight the importance of identifying more affordable therapeutic alternatives. A body of literature has shown that metformin has the potential to act as an antineoplastic agent. Here, we examined the effects of metformin on GBM in humans. Methods: The Preferred Reporting Items for Systematic reviews and Meta-Analyses (PRISMA) guidelines were followed to perform the review. A total of 469 studies were screened using comprehensive search terms. Of these, 4 studies were compatible for the meta-analysis. Results: Data analysis demonstrated an increase in median overall survival for GBM patients up to 18 months compared to controls (p = 0.00197). Conclusions: Overall, our findings support the efficacy of metformin as an anti-neoplastic agent, and that it may grant a survival advantage for patients diagnosed with GBM. Further analyses should find dose-dependent relationships between metformin and the targeted survival outcomes in larger, rigorous clinical trials.
    Keywords:  cancer therapy; glioblastoma multiforme; metformin
    DOI:  https://doi.org/10.3390/neurolint18030040