ArticleCancer & metabolism2021
Pharmacological activation of pyruvate kinase M2 reprograms glycolysis leading to TXNIP depletion and AMPK activation in breast cancer cells.
Article in Cancer & metabolism, 2021. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 19 papers.
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Who cites it
19 citing papers in PubMed, 35 citations in OpenAlex.
- Promising Role of PKM2 in the Diagnosis and Prognosis of Ovarian Cancer.Anti-cancer agents in medicinal chemistry · 2026Review
- Integrated screening for small molecules interfering with PKM2: a drug repurposing strategy against glioblastoma.Journal of translational medicine · 2025Article
- Deletion of PTP1B in cardiomyocytes alters cardiac metabolic signaling to protect against cardiomyopathy induced by a high-fat diet.Science signaling · 2025Article
- Metabolic Adaptations in Cancer Progression: Optimization Strategies and Therapeutic Targets.Cancers · 2025Review
- Differential Regulation of PKM2, AMPK, and mTOR in Response to Insulin and Dietary Management.Cells · 2025Article
- Novel sulfonamides unveiled as potent anti-lung cancer agentsRSC medicinal chemistry · 2024Article
- Targeted suppression of oral squamous cell carcinoma by pyrimidine-tethered quinoxaline derivatives.RSC medicinal chemistry · 2024Article
- N6-isopentenyladenosine inhibits aerobic glycolysis in glioblastoma cells by targeting PKM2 expression and activity.FEBS open bio · 2024Article
- Non-metabolic enzyme function of pyruvate kinase M2 in breast cancer.Frontiers in oncology · 2024Review
- Chlorpromazine affects glioblastoma bioenergetics by interfering with pyruvate kinase M2.Cell death & disease · 2023Article
- Modulating Glycolysis to Improve Cancer Therapy.International journal of molecular sciences · 2023Review
- Docetaxel suppressed cell proliferation through Smad3/HIF-1α-mediated glycolysis in prostate cancer cells.Cell communication and signaling : CCS · 2022Article
- Article
- Immunomodulatory Role of Thioredoxin Interacting Protein in Cancer's Impediments: Current Understanding and Therapeutic Implications.Vaccines · 2022Review
- Cinnamon extract improves abnormalities in glucose tolerance by decreasing Acyl-CoA synthetase long-chain family 1 expression in adipocytes.Scientific reports · 2022Article
- PKM2 Modulation in Head and Neck Squamous Cell Carcinoma.International journal of molecular sciences · 2022Article
- Article
- Multifaceted Role of AMPK in Viral Infections.Cells · 2021Review
- Combination Treatment Using Pyruvate Kinase M2 Inhibitors for the Sensitization of High Density Triple-negative Breast Cancer Cells.In vivo (Athens, Greece)Article
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Authors and funding
5 authors at 1 institution in 1 country.
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Abstract
backgroundAerobic glycolysis, discovered by Otto Warburg, is a hallmark of cancer metabolism even though not yet fully understood. The low activity of the cancerous pyruvate kinase isozyme (M2) is thought to play an important role by facilitating the conversion of glycolytic intermediates to other anabolic pathways to support tumors' high proliferation rate.
methodsFive breast cancer cell lines representing different molecular subtypes were used in this study where real time measurements of cellular bioenergetics and immunoblotting analysis of energy- and nutrient-sensing pathways were employed to investigate the potential effects of PKM2 allosteric activator (DASA-58) in glucose rewiring.
resultsIn this study, we show that DASA-58 can induce pyruvate kinase activity in breast cancer cells without affecting the overall cell survival. The drug is also able to reduce TXNIP levels (an intracellular glucose sensor) probably through depletion of upstream glycolytic metabolites and independent of AMPK and ER signaling. AMPK shows an induction in phosphorylation (T172) in response to treatment an effect that can be potentiated by combining DASA-58 with other metabolic inhibitors.
conclusionsAltogether, the multifaceted metabolic reprogramming induced by DASA-58 in breast cancer cells increases their susceptibility to other therapeutics suggesting the suitability of the intracellular glucose sensor TXNIP as a marker of PK activity.
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