ArticlePloS one2018
Lapachol inhibits glycolysis in cancer cells by targeting pyruvate kinase M2.
Article in PloS one, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 33 papers, 1 of them a synthesis that pooled it.
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The trial behind it
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Who cites it
33 citing papers in PubMed, 1 synthesis or guideline pooled it, 74 citations in OpenAlex.
- Natural products targeting glycolysis in cancer.Frontiers in pharmacology · 2022Pooled it
- Benzyl-Naphthoquinones as Selective Anticancer Agents for Oral Squamous Cell Carcinoma via Apoptosis Induction.Biomedicines · 2026Article
- In Vitro Evaluation of Natural Sesquiterpene Lactones and Naphthoquinones Against Pancreatic Ductal Adenocarcinoma Cells.Molecules (Basel, Switzerland) · 2026Article
- Silk Fibroin-Stabilized Lapachol Microemulsion Enhances Antiglioma Activity In Vitro.Chemistry & biodiversity · 2026Article
- Article
- Lapachol interferes with the cell cycle and inhibits proliferation and migration of bladder tumor cells with effects on ncRNA expression.Scientific reports · 2025Article
- Mannich Base Derived from Lawsone Inhibits PKM2 and Induces Neoplastic Cell Death.Biomedicines · 2024Article
- Effects of phosphoglycerate kinase 1 and pyruvate kinase M2 on metabolism and physiochemical changes in postmortem muscle.Food chemistry: X · 2024Article
- Inhibition of Pyruvate kinase M2 (PKM2) by shikonin attenuates isoproterenol-induced acute myocardial infarction via reduction in inflammation, hypoxia, apoptosis, and fibrosis.Naunyn-Schmiedeberg's archives of pharmacology · 2024Article
- Preclinical evaluation of L-fucoside from lapachol-loaded nanoemulsion as a strategy to breast cancer treatment.Biomedicine & pharmacotherapy = Biomedecine & pharmacotherapie · 2024Article
- A Novel Phytocolorant, Neoxanthin, as a Potent Chemopreventive: Current Progress and Future Prospects.Current medicinal chemistry · 2024Review
- Role of Pyruvate Kinase M2 (PKM2) in Cardiovascular Diseases.Journal of cardiovascular translational research · 2023Review
- Chemoselective Synthesis of Mannich Adducts from 1,4-Naphthoquinones and Profile as Autophagic Inducers in Oral Squamous Cell Carcinoma.Molecules (Basel, Switzerland) · 2022Article
- Design of Conjugates Based on Sesquiterpene Lactones with Polyalkoxybenzenes by "Click" Chemistry to Create Potential Anticancer Agents.Molecules (Basel, Switzerland) · 2022Article
- Identification of Natural Compounds as Inhibitors of Pyruvate Kinase M2 for Cancer Treatment.Molecules (Basel, Switzerland) · 2022Article
- Targeting Glucose Metabolism Enzymes in Cancer Treatment: Current and Emerging Strategies.Cancers · 2022Review
- TGF-β signaling in the tumor metabolic microenvironment and targeted therapies.Journal of hematology & oncology · 2022Review
- Pro-Apoptotic Antitumoral Effect of Novel Acridine-Core Naphthoquinone Compounds against Oral Squamous Cell Carcinoma.Molecules (Basel, Switzerland) · 2022Article
- How Should the Worldwide Knowledge of Traditional Cancer Healing Be Integrated with Herbs and Mushrooms into Modern Molecular Pharmacology?Pharmaceuticals (Basel, Switzerland) · 2022Review
- Metabolism heterogeneity in melanoma fuels deactivation of immunotherapy: Predict before protect.Frontiers in oncology · 2022Review
Corrections and comments
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Authors and funding
6 authors at 2 institutions in 2 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Reliance on aerobic glycolysis is one of the hallmarks of cancer. Although pyruvate kinase M2 (PKM2) is a key mediator of glycolysis in cancer cells, lack of selective agents that target PKM2 remains a challenge in exploiting metabolic pathways for cancer therapy. We report that unlike its structural analog shikonin, a known inhibitor of PKM2, lapachol failed to induce non-apoptotic cell death ferroxitosis in hypoxia. However, melanoma cells treated with lapachol showed a dose-dependent inhibition of glycolysis and a corresponding increase in oxygen consumption. Accordingly, in silico studies revealed a high affinity-binding pocket for lapachol on PKM2 structure. Lapachol inhibited PKM2 activity of purified enzyme as well as in melanoma cell extracts. Blockade of glycolysis by lapachol in melanoma cells led to decreased ATP levels and inhibition of cell proliferation. Furthermore, perturbation of glycolysis in melanoma cells with lapachol sensitized cells to mitochondrial protonophore and promoted apoptosis. These results present lapachol as an inhibitor of PKM2 to interrogate metabolic plasticity in tumor cells.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.