ArticleFrontiers in pharmacology2020
Esculetin Inhibits Cancer Cell Glycolysis by Binding Tumor PGK2, GPD2, and GPI.
Article in Frontiers in pharmacology, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 26 papers, 1 of them a synthesis that pooled it.
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Who cites it
26 citing papers in PubMed, 1 synthesis or guideline pooled it, 45 citations in OpenAlex.
- Interplay Between Glucose Metabolism and Chromatin Modifications in Cancer.Frontiers in cell and developmental biology · 2021Pooled it
- PINK1‑mediated mitophagy enhances breast cancer proliferation through metabolic reprogramming.Oncology reports · 2026Article
- Widely targeted metabolomics reveals conserved and differential metabolite patterns related to nutritional and bioactive compounds in stems and leaves of threeFood chemistry: X · 2026Article
- The Role of Exosomes in Offspring Metabolic Programming in Gestational Diabetes: Mechanisms and Potential Applications.International journal of biological sciences · 2026Review
- The Utilization Value of Condensate Water from the Drying Process ofMetabolites · 2025Article
- Beta sitosterol inhibits the proliferation and migration of synoviocytes in rheumatoid arthritis via lactylation of GPI.Scientific reports · 2025Article
- Prediction of prognosis, efficacy of lung adenocarcinoma by machine learning model based on immune and metabolic related genes.Discover oncology · 2024Article
- Esculetin unveiled: Decoding its anti-tumor potential through molecular mechanisms-A comprehensive review.Cancer reports (Hoboken, N.J.) · 2024Review
- Comprehensive analysis of the lncRNAs-related immune gene signatures and their correlation with immunotherapy in lung adenocarcinoma.British journal of cancer · 2023Article
- Synergy, Additivity and Antagonism between Esculetin and Six Commonly Used Chemotherapeutics in Various Malignant Melanoma Cell Lines-An Isobolographic Analysis.Molecules (Basel, Switzerland) · 2023Article
- The Role of Reprogrammed Glucose Metabolism in Cancer.Metabolites · 2023Review
- Identification of a hypoxia-related gene prognostic signature in colorectal cancer based on bulk and single-cell RNA-seq.Scientific reports · 2023Article
- Inhibitory Effects of Esculetin on Liver Cancer Through Triggering NCOA4 Pathway-Mediation Ferritinophagy in vivo and in vitro.Journal of hepatocellular carcinoma · 2023Article
- Non-bioenergetic roles of mitochondrial GPD2 promote tumor progression.Theranostics · 2023Article
- COVID-19 metabolism: Mechanisms and therapeutic targets.MedComm · 2022Review
- New Insights onMolecules (Basel, Switzerland) · 2022Article
- Identification of microtubule-associated biomarkers in diffuse large B-cell lymphoma and prognosis prediction.Frontiers in genetics · 2022Article
- GPI: An indicator for immune infiltrates and prognosis of human breast cancer from a comprehensive analysis.Frontiers in endocrinology · 2022Article
- Taraxasterol suppresses cell proliferation and boosts cell apoptosis via inhibiting GPD2-mediated glycolysis in gastric cancer.Cytotechnology · 2021Article
- Current Development and Application of Anaerobic Glycolytic Enzymes in Urothelial Cancer.International journal of molecular sciences · 2021Review
Corrections and comments
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Authors and funding
7 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
Glycolysis can improve the tolerance of tissue cells to hypoxia, and its intermediates provide raw materials for the synthesis and metabolism of the tumor cells. If it can inhibit the activity of glycolysis-related enzymes and control the energy metabolism of tumor, it can be targeted for the treatment of malignant tumor. The target proteins phosphoglycerate kinase 2 (PGK2), glycerol-3-phosphate dehydrogenase (GPD2), and glucose-6-phosphate isomerase (GPI) were screened by combining transcriptome, proteomics, and reverse docking. We detected the binding constant of the active compound using microscale thermophoresis (MST). It was found that esculetin bound well with three potential target proteins. Esculetin significantly inhibited the rate of glycolysis, manifested by differences of cellular lactate production and glucose consumption in HepG2 cells with or without esculetin. It was found that GPD2 bound strongly to GPI, revealing the direct interaction between the two glycolysis-related proteins. Animal tests have further demonstrated that esculetin may have anticancer effects by affecting the activity of PGK2, GPD2, and GPI. The results of this study demonstrated that esculetin can affect the glucose metabolism by binding to glycolytic proteins, thus playing an anti-tumor role, and these proteins which have direct interactions are potential novel targets for tumor treatment by esculetin.
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