ReferenceID 1843
Esculetin Inhibits Cancer Cell Glycolysis by Binding Tumor PGK2, GPD2, and GPI
Front Pharmacol
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 enzym
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Record Fields
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- Reference Id
- 1843
- Evidence Id
- 18433
- Core Evidence Id
- 18433
- Source Reference Id
- 3669
- Herb2 Reference Id
- HBREF004466
- Subject Paper Key
- HBIN025796_32292350
- Pubmed Id
- 32292350
- Doi
- 10.3389/fphar.2020.00379
- Paper Title
- Esculetin Inhibits Cancer Cell Glycolysis by Binding Tumor PGK2, GPD2, and GPI
- Paper 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.
- Journal
- Front Pharmacol
- Publish Year
- 2020
- Experiment Subject
- Experiment Type
- Animal & Cell Experiment
- Phenotype Related
- Malignant Tumor; Tumor
- Paper Title Cn
- Paper Title En
- Esculetin Inhibits Cancer Cell Glycolysis by Binding Tumor PGK2, GPD2, and GPI
- Bilingual Status
- semi_complete