bims-glucam Biomed News
on Glutamine cancer metabolism
Issue of 2022‒07‒03
eleven papers selected by
Sreeparna Banerjee
Middle East Technical University


  1. mBio. 2022 Jun 28. e0127422
      In response to Mycobacterium tuberculosis infection, macrophages mount proinflammatory and antimicrobial responses similar to those observed in M1 macrophages activated by lipopolysaccharide (LPS) and interferon gamma (IFN-γ). A metabolic reprogramming to hypoxia-inducible-factor 1 (HIF-1)-mediated uptake of glucose and its metabolism by glycolysis is required for M1-like polarization, but little is known about other metabolic programs driving the M1-like polarization during infection. We report that glutamine serves as a carbon and nitrogen source for the metabolic reprogramming to M1-like macrophages. Widely targeted metabolite screening identified an association of glutamine and/or glutamate with highly affected metabolic pathways of M1-like macrophages. Moreover, stable isotope-assisted metabolomics of U13C glutamine and U13C glucose revealed that glutamine, rather than glucose, is catabolized in both the oxidative and reductive tricarboxylic acid (TCA) cycles of M1-like macrophages, thereby generating signaling molecules that include succinate, biosynthetic precursors such as aspartate, and itaconate. U15N glutamine-tracing metabolomics further revealed participation of glutamine nitrogen in synthesis of intermediates of purine and pyrimidine metabolism plus amino acids, including aspartate. These findings were corroborated by diminished M1 polarization from chemical inhibition of glutaminase (GLS), the key enzyme in the glutaminolysis pathway, and by genetic deletion of GLS in infected macrophages. Thus, the catabolism of glutamine is an integral component of metabolic reprogramming in activating macrophages and it coordinates with elevated cytosolic glycolysis to satisfy the cellular demand for bioenergetic and biosynthetic precursors of M1-like macrophages. Knowledge of these new immunometabolic features of M1-like macrophages should advance the development of host-directed therapies for tuberculosis. IMPORTANCE Macrophages play essential roles in determining the progression and final outcome of human infection by Mycobacterium tuberculosis. While upregulation of hypoxia-inducible-factor 1 (HIF-1) and a metabolic reprogramming to the Warburg Effect-like state are known to be critical for immune cell activation in response to M. tuberculosis infection, our overall knowledge about the immunometabolism of M1-like macrophages is poor. Using widely targeted small-metabolite screening, stable isotope tracing metabolomics, and pharmacological and genetic approaches, we report that, in addition to enhanced glucose catabolism by glycolysis, glutamine is utilized as an important carbon and nitrogen source for the generation of biosynthetic precursors, signaling molecules, and itaconate in M. tuberculosis-induced M1-like macrophages. Recognizing this novel contribution of glutamine to the immunometabolic properties of M. tuberculosis-infected macrophages may facilitate the development of treatments for tuberculosis and stimulate comparable studies with other pathogen-macrophage interactions.
    Keywords:  M1-like polarization; Mycobacterium tuberculosis; TCA cycle; glutaminolysis; immunometabolism; isotope tracing metabolomics
    DOI:  https://doi.org/10.1128/mbio.01274-22
  2. J Cell Sci. 2022 Jul 01. pii: jcs.259090. [Epub ahead of print]
      Accelerated aerobic glycolysis is a distinctive metabolic property of cancer cells that confers dependency on glucose for survival. However, the therapeutic strategies targeting this vulnerability are still inefficient and have unacceptable side effects in clinical trials. Therefore, developing biomarkers to predict therapeutic efficacy would be essential to improve the selective targeting of cancer cells. Here, we found that the cell lines sensitive to glucose deprivation have high expression of cystine/glutamate antiporter xCT. We found that cystine uptake and glutamate export through xCT contributed to rapid NADPH depletion under glucose deprivation. This collapse of the redox system oxidized and inactivated AMPK, a major regulator of metabolic adaptation, resulting in a metabolic catastrophe and cell death. While this phenomenon was prevented by pharmacological or genetic inhibition of xCT, overexpression of xCT sensitized resistant cancer cells to glucose deprivation. Taken together, these findings suggest a novel cross-talk between AMPK and xCT for the metabolism and signal transduction and reveal a metabolic vulnerability in xCT-high expressing cancer cells to glucose deprivation.
    Keywords:  AMPK; Cystine; Glucose starvation; NADPH; SLC7A11; xCT
    DOI:  https://doi.org/10.1242/jcs.259090
  3. Sci Rep. 2022 Jun 30. 12(1): 11062
      Most cancer cells rely on aerobic glycolysis to support uncontrolled proliferation and evade apoptosis. However, pancreatic cancer cells switch to glutamine metabolism to survive under hypoxic conditions. Activation of the Wnt/β-catenin pathway induces aerobic glycolysis by activating enzymes required for glucose metabolism and regulating the expression of glutamate transporter and glutamine synthetase. The results demonstrate that riluzole inhibits pancreatic cancer cell growth and has no effect on human pancreatic normal ductal epithelial cells. RNA-seq experiments identified the involvement of Wnt and metabolic pathways by riluzole. Inhibition of Wnt-β-catenin/TCF-LEF pathway by riluzole suppresses the expression of PDK, MCT1, cMyc, AXIN, and CyclinD1. Riluzole inhibits glucose transporter 2 expression, glucose uptake, lactate dehydrogenase A expression, and NAD + level. Furthermore, riluzole inhibits glutamate release and glutathione levels, and elevates reactive oxygen species. Riluzole disrupts mitochondrial homeostasis by inhibiting Bcl-2 and upregulating Bax expression, resulting in a drop of mitochondrial membrane potential. Finally, riluzole inhibits pancreatic cancer growth in KPC (Pdx1-Cre, LSL-Trp53R172H, and LSL-KrasG12D) mice. In conclusion, riluzole can inhibit pancreatic cancer growth by regulating glucose and glutamine metabolisms and can be used to treat pancreatic cancer.
    DOI:  https://doi.org/10.1038/s41598-022-13472-y
  4. J Nucl Med. 2022 Jun 30. pii: jnumed.122.264152. [Epub ahead of print]
      Aggressive cancers such as triple-negative breast cancer (TNBC) avidly metabolize glutamine as a feature of their malignant phenotype. The conversion of glutamine to glutamate by the glutaminase (GLS) enzyme represents the first and rate-limiting step of this pathway, and a target for drug development. Indeed, a novel GLS inhibitor (GLSi) has been developed and tested in clinical trials, but with limited success, suggesting the potential for a biomarker to select patients that could benefit from this novel therapy. Here, we study a non-metabolized amino acid analog, 18F-Fluciclovine (Axumin®) as a PET imaging biomarker for detecting the pharmacodynamic response to GLSi. We show that glutamine transporters mediate the uptake of 18F-Fluciclovine into human breast cancer cells. To allow 18F-Fluciclovine PET to be performed in mice, citrate in the tracer formulation is replaced by PBS. Mice bearing TNBC (HCC38, HCC1806 and MBA-MD-231) and ER-positive (MCF-7) breast cancer xenografts were imaged with dynamic PET at baseline and after a 2-day treatment of GLSi (CB839 (Telaglenastat)) or vehicle. Kinetic analysis suggested reversible uptake of the tracer and the distribution volume (VD) of 18F-Fluciclovine was estimated by Logan plot analysis. A significant increase of VD was observed after CB839 treatment in TNBC models exhibiting high GLS activity (HCC38 and HCC1806), but not in TNBC or MCF-7 exhibiting low GLS. Changes of VD were corroborated with changes in GLS activity measured in CB839- versus vehicle-treated tumors, as well as with changes of VD of [18F]-(2S,R4)-fluoroglutamine, which we previously validated as a measure of cellular glutamine pool size. A moderate, albeit significant decrease of [18F]fluorodeoxyglucose (FDG) PET signal was observed in HCC1806 tumors after CB839 treatment. In conclusion, 18F-Fluciclovine PET has potential to serve as a clinical translatable, pharmacodynamic biomarker of GLSi.
    Keywords:  18F-Fluciclovine PET; Animal Imaging; CB839; Distribution volume; Glutaminase; Oncology: Breast; PET; Triple negative breast cancer
    DOI:  https://doi.org/10.2967/jnumed.122.264152
  5. Mol Metab. 2022 Jun 22. pii: S2212-8778(22)00101-6. [Epub ahead of print] 101532
      Bone marrow mesenchymal stromal cells (MSCs) have immunomodulatory and regenerative potential. However, culture conditions govern their metabolic processes and therapeutic efficacy. Here we show that culturing donor-derived MSCs in Plasmax™, a physiological medium with the concentrations of nutrients found in human plasma, supports their proliferation and stemness, and prevents the nutritional stress induced by the conventional medium DMEM. The quantification of the exchange rates of metabolites between cells and medium, untargeted metabolomics, stable isotope tracing and transcriptomic analysis, performed at physiologically relevant oxygen concentrations (1%O2), reveal that MSCs rely on high rate of glucose to lactate conversion, coupled with parallel anaplerotic fluxes from glutamine and glutamate to support citrate synthesis and secretion. These distinctive traits of MSCs shape the metabolic microenvironment of bone marrow niche and can influence nutrient cross-talks under physiological and pathological conditions.
    Keywords:  Citrate; Glutamate; Glutamine; Hypoxia; Mesenchymal stromal cells; Metabolism; Physiological medium; Plasmax; Primary cells; Stable isotope tracing
    DOI:  https://doi.org/10.1016/j.molmet.2022.101532
  6. Klin Onkol. 2022 ;35(3): 195-207
      BACKGROUND: A general characteristic of cancer metabolism is the skill to gain the essential nutrients from a relatively poor environment and use them effectively to maintain viability and create new bio-mass. The changes in intracellular and extracellular metabolites that accompany metabolic reprogramming associated with tumor growth subsequently affect gene expression, cell differentiation, and tumor microenvironment. During carcinogenesis, cancer cells face huge selection pressures that force them to constantly optimize dominant metabolic pathways and undergo major metabolic reorganizations. In general, greater flexibility of metabolic pathways increases the ability of tumor cells to satisfy their metabolic needs in a changing environment.PURPOSE: In this review, we discuss the metabolic properties of cancer cells and describe the tumor promoting effect of the transformed metabolism. We assume that changes in metabolism are significant enough to facilitate tumorigenesis and may provide interesting targets for cancer therapy.
    Keywords:  Krebs cycle; Metabolism; Warburg effect; anaplerosis; cancer; glutaminolysis; malignancy; oncogenesis; oncometabolite
    DOI:  https://doi.org/10.48095/ccko2022195
  7. Cancer Med. 2022 Jun 27.
      BACKGROUND: Tumor cells may aberrantly express metabolic enzymes to adapt to their environment for survival and growth. Targeting cancer-specific metabolic enzymes is a potential therapeutic strategy. Phosphoenolpyruvate carboxykinase (PEPCK) catalyzes the conversion of oxaloacetate to phosphoenolpyruvate and links the tricarboxylic acid cycle and glycolysis/gluconeogenesis. Mitochondrial PEPCK (PEPCK-M), encoded by PCK2, is an isozyme of PEPCK and is distributed in mitochondria. Overexpression of PCK2 has been identified in many human cancers and demonstrated to be important for the survival program initiated upon metabolic stress in cancer cells. We evaluated the expression status of PEPCK-M and investigated the function of PEPCK-M in breast cancer.METHODS: We checked the expression status of PEPCK-M in breast cancer samples by immunohistochemical staining. We knocked down or overexpressed PCK2 in breast cancer cell lines to investigate the function of PEPCK-M in breast cancer.
    RESULTS: PEPCK-M was highly expressed in estrogen receptor-positive (ER+ ) breast cancers. Decreased cell proliferation and G0 /G1 arrest were induced in ER+ breast cancer cell lines by knockdown of PCK2. PEPCK-M promoted the activation of mTORC1 downstream signaling molecules and the E2F1 pathways in ER+ breast cancer. In addition, glucose uptake, intracellular glutamine levels, and mTORC1 pathways activation by glucose and glutamine in ER+ breast cancer were attenuated by PCK2 knockdown.
    CONCLUSION: PEPCK-M promotes proliferation and cell cycle progression in ER+ breast cancer via upregulation of the mTORC1 and E2F1 pathways. PCK2 also regulates nutrient status-dependent mTORC1 pathway activation in ER+ breast cancer. Further studies are warranted to understand whether PEPCK-M is a potential therapeutic target for ER+ breast cancer.
    Keywords:  E2F1; PCK2; estrogen receptor positive (ER+) breast cancer; mTORC1; mitochondrial phosphoenolpyruvate carboxykinase (PEPCK-M)
    DOI:  https://doi.org/10.1002/cam4.4969
  8. Nat Commun. 2022 Jun 28. 13(1): 3706
      Ribosome biogenesis is an energetically expensive program that is dictated by nutrient availability. Here we report that nutrient deprivation severely impairs precursor ribosomal RNA (pre-rRNA) processing and leads to the accumulation of unprocessed rRNAs. Upon nutrient restoration, pre-rRNAs stored under starvation are processed into mature rRNAs that are utilized for ribosome biogenesis. Failure to accumulate pre-rRNAs under nutrient stress leads to perturbed ribosome assembly upon nutrient restoration and subsequent apoptosis via uL5/uL18-mediated activation of p53. Restoration of glutamine alone activates p53 by triggering uL5/uL18 translation. Induction of uL5/uL18 protein synthesis by glutamine is dependent on the translation factor eukaryotic elongation factor 2 (eEF2), which is in turn dependent on Raf/MEK/ERK signaling. Depriving cells of glutamine prevents the activation of p53 by rRNA synthesis inhibitors. Our data reveals a mechanism that tumor cells can exploit to suppress p53-mediated apoptosis during fluctuations in environmental nutrient availability.
    DOI:  https://doi.org/10.1038/s41467-022-31418-w
  9. J Biol Chem. 2022 Jun 22. pii: S0021-9258(22)00620-2. [Epub ahead of print] 102178
      The Solute Carrier 1A (SLC1A) family comprises a group of membrane proteins that act as dual-function amino acid transporters and chloride channels and includes the alanine serine cysteine transporters (ASCTs) as well as the excitatory amino acid transporters (EAATs). ASCT2 is regarded as a promising target for cancer therapy, as it can transport glutamine and other neutral amino acids into cells and is upregulated in a range of solid tumors. The compound L-γ-glutamyl-p-nitroanilide (GPNA) is widely used in studies probing the role of ASCT2 in cancer biology; however, the mechanism by which GPNA inhibits ASCT2 is not entirely clear. Here, we used electrophysiology and radiolabelled flux assays to demonstrate that GPNA activates the chloride conductance of ASCT2 to the same extent as a transported substrate, whilst not undergoing the full transport cycle. This is a previously unreported phenomenon for inhibitors of the SLC1A family but corroborates a body of literature suggesting that the structural requirements for transport are distinct from those for chloride channel formation. We also show that in addition to its currently known targets, GPNA inhibits several of the EAATs. Together, these findings raise questions about the true mechanisms of its anticancer effects.
    Keywords:  ASCT; Amino acid transport; EAAT; GPNA; SLC1A; cancer biology; chloride channel; glutamate; glutamine; inhibition mechanism
    DOI:  https://doi.org/10.1016/j.jbc.2022.102178
  10. Cancer Res. 2022 Jun 30. pii: can.22.0917. [Epub ahead of print]
      Metabolic reprogramming is a hallmark of cancer progression. Metabolic activity supports tumorigenesis and tumor progression, allowing cells to uptake essential nutrients from the environment and use the nutrients to maintain viability and support proliferation. The metabolic pathways of malignant cells are altered to accommodate increased demand for energy, reducing equivalents, and biosynthetic precursors. Activated oncogenes coordinate with altered metabolism to control cell-autonomous pathways, which can lead to tumorigenesis when abnormalities accumulate. Clinical and preclinical studies have shown that targeting metabolic features of hematological malignancies is an appealing therapeutic approach. This review provides a comprehensive overview of the mechanisms of metabolic reprogramming in hematologic malignancies and potential therapeutic strategies to target cancer metabolism.
    DOI:  https://doi.org/10.1158/0008-5472.CAN-22-0917
  11. Front Oncol. 2022 ;12 816504
      Therapeutic targeting of tumor vulnerabilities is emerging as a key area of research. This review is focused on exploiting the vulnerabilities of tumor cells and the immune cells in the tumor immune microenvironment (TIME), including tumor hypoxia, tumor acidity, the bidirectional proton-coupled monocarboxylate transporters (MCTs) of lactate, mitochondrial oxidative phosphorylation (OXPHOS), and redox enzymes in the tricarboxylic acid cycle. Cancer cells use glucose for energy even under normoxic conditions. Although cancer cells predominantly rely on glycolysis, many have fully functional mitochondria, suggesting that mitochondria are a vulnerable target organelle in cancer cells. Thus, one key distinction between cancer and normal cell metabolism is metabolic reprogramming. Mitochondria-targeted small molecule inhibitors of OXPHOS inhibit tumor proliferation and growth. Another hallmark of cancer is extracellular acidification due lactate accumulation. Emerging results show that lactate acts as a fuel for mitochondrial metabolism and supports tumor proliferation and growth. Metabolic reprogramming occurs in glycolysis-deficient tumor phenotypes and in kinase-targeted, drug-resistant cancers overexpressing OXPHOS genes. Glycolytic cancer cells located away from the vasculature overexpress MCT4 transporter to prevent overacidification by exporting lactate, and the oxidative cancer cells located near the vasculature express MCT1 transporter to provide energy through incorporation of lactate into the tricarboxylic acid cycle. MCTs are, therefore, a vulnerable target in cancer metabolism. MCT inhibitors exert synthetic lethality in combination with metformin, a weak inhibitor of OXPHOS, in cancer cells. Simultaneously targeting multiple vulnerabilities within mitochondria shows synergistic antiproliferative and antitumor effects. Developing tumor-selective, small molecule inhibitors of OXPHOS with a high therapeutic index is critical to fully exploiting the mitochondrial vulnerabilities. We and others developed small-molecule inhibitors containing triphenylphosphonium cation that potently inhibit OXPHOS in tumor cells and tissues. Factors affecting tumor cell vulnerabilities also impact immune cells in the TIME. Glycolytic tumor cells supply lactate to the tumor-suppressing regulatory T cells overexpressing MCTs. Therapeutic opportunities for targeting vulnerabilities in tumor cells and the TIME, as well as the implications on cancer health disparities and cancer treatment, are addressed.
    Keywords:  Mitochondrial drugs; metabolic reprogramming; monocarboxylate transporters; oxidative phosphorylation (OXPHOS); tumor microenvironment
    DOI:  https://doi.org/10.3389/fonc.2022.816504