Unmasking the Warburg Effect: Unleashing the Power of Enzyme Inhibitors for Cancer Therapy
The Warburg effect (or aerobic glycolysis), which was first described in 1926 by Otto Heinrich Warburg, consists of the change in glucose metabolism in cancer cells. In normal cells, glucose metabolism finalizes in the mitochondria through oxidative phosphorylation (OXPHOS) in the presence of oxygen...
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MDPI AG
2023-09-01
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| Series: | Drugs and Drug Candidates |
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| Online Access: | https://www.mdpi.com/2813-2998/2/3/37 |
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| author | Eduardo Angulo-Elizari Leire Gaviria-Soteras Irati Zubiri Sandra Ramos-Inza Carmen Sanmartin Daniel Plano |
| author_facet | Eduardo Angulo-Elizari Leire Gaviria-Soteras Irati Zubiri Sandra Ramos-Inza Carmen Sanmartin Daniel Plano |
| author_sort | Eduardo Angulo-Elizari |
| collection | DOAJ |
| description | The Warburg effect (or aerobic glycolysis), which was first described in 1926 by Otto Heinrich Warburg, consists of the change in glucose metabolism in cancer cells. In normal cells, glucose metabolism finalizes in the mitochondria through oxidative phosphorylation (OXPHOS) in the presence of oxygen. However, the Warburg effect describes a change in the glucose metabolism in cancer cells, consuming excess glucose and converting it into lactate independently of the presence of oxygen. During this process, a wide variety of enzymes can modify their expression and activity to contribute to the mechanism of deregulated cancer metabolism. Therefore, the modulation of enzymes regulating aerobic glycolysis is a strategy for cancer treatment. Although numerous enzymes play a role in regulating aerobic glycolysis, hexokinase 2 (HK2), pyruvate dehydrogenase kinase (PDK), pyruvate kinase (PK), and lactate dehydrogenase (LDH) are worth mentioning. Numerous modulators of these enzymes have been described in recent years. This review aims to present and group, according to their chemical structure, the most recent emerging molecules targeting the above-mentioned enzymes involved in the Warburg effect in view of the future development of cancer treatments. |
| first_indexed | 2024-03-10T22:52:52Z |
| format | Article |
| id | doaj.art-0b5d1e732c504531b09a1f8b8df39019 |
| institution | Directory Open Access Journal |
| issn | 2813-2998 |
| language | English |
| last_indexed | 2024-03-10T22:52:52Z |
| publishDate | 2023-09-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Drugs and Drug Candidates |
| spelling | doaj.art-0b5d1e732c504531b09a1f8b8df390192023-11-19T10:11:51ZengMDPI AGDrugs and Drug Candidates2813-29982023-09-012372876910.3390/ddc2030037Unmasking the Warburg Effect: Unleashing the Power of Enzyme Inhibitors for Cancer TherapyEduardo Angulo-Elizari0Leire Gaviria-Soteras1Irati Zubiri2Sandra Ramos-Inza3Carmen Sanmartin4Daniel Plano5Department of Pharmaceutical Technology and Chemistry, School of Pharmacy and Nutrition, University of Navarra, Irunlarrea 1, E-31008 Pamplona, SpainDepartment of Pharmaceutical Technology and Chemistry, School of Pharmacy and Nutrition, University of Navarra, Irunlarrea 1, E-31008 Pamplona, SpainDepartment of Pharmaceutical Technology and Chemistry, School of Pharmacy and Nutrition, University of Navarra, Irunlarrea 1, E-31008 Pamplona, SpainDepartment of Pharmaceutical Technology and Chemistry, School of Pharmacy and Nutrition, University of Navarra, Irunlarrea 1, E-31008 Pamplona, SpainDepartment of Pharmaceutical Technology and Chemistry, School of Pharmacy and Nutrition, University of Navarra, Irunlarrea 1, E-31008 Pamplona, SpainDepartment of Pharmaceutical Technology and Chemistry, School of Pharmacy and Nutrition, University of Navarra, Irunlarrea 1, E-31008 Pamplona, SpainThe Warburg effect (or aerobic glycolysis), which was first described in 1926 by Otto Heinrich Warburg, consists of the change in glucose metabolism in cancer cells. In normal cells, glucose metabolism finalizes in the mitochondria through oxidative phosphorylation (OXPHOS) in the presence of oxygen. However, the Warburg effect describes a change in the glucose metabolism in cancer cells, consuming excess glucose and converting it into lactate independently of the presence of oxygen. During this process, a wide variety of enzymes can modify their expression and activity to contribute to the mechanism of deregulated cancer metabolism. Therefore, the modulation of enzymes regulating aerobic glycolysis is a strategy for cancer treatment. Although numerous enzymes play a role in regulating aerobic glycolysis, hexokinase 2 (HK2), pyruvate dehydrogenase kinase (PDK), pyruvate kinase (PK), and lactate dehydrogenase (LDH) are worth mentioning. Numerous modulators of these enzymes have been described in recent years. This review aims to present and group, according to their chemical structure, the most recent emerging molecules targeting the above-mentioned enzymes involved in the Warburg effect in view of the future development of cancer treatments.https://www.mdpi.com/2813-2998/2/3/37Warburg effectaerobic glycolysisdrug discoverycancerhexokinasepyruvate kinase |
| spellingShingle | Eduardo Angulo-Elizari Leire Gaviria-Soteras Irati Zubiri Sandra Ramos-Inza Carmen Sanmartin Daniel Plano Unmasking the Warburg Effect: Unleashing the Power of Enzyme Inhibitors for Cancer Therapy Drugs and Drug Candidates Warburg effect aerobic glycolysis drug discovery cancer hexokinase pyruvate kinase |
| title | Unmasking the Warburg Effect: Unleashing the Power of Enzyme Inhibitors for Cancer Therapy |
| title_full | Unmasking the Warburg Effect: Unleashing the Power of Enzyme Inhibitors for Cancer Therapy |
| title_fullStr | Unmasking the Warburg Effect: Unleashing the Power of Enzyme Inhibitors for Cancer Therapy |
| title_full_unstemmed | Unmasking the Warburg Effect: Unleashing the Power of Enzyme Inhibitors for Cancer Therapy |
| title_short | Unmasking the Warburg Effect: Unleashing the Power of Enzyme Inhibitors for Cancer Therapy |
| title_sort | unmasking the warburg effect unleashing the power of enzyme inhibitors for cancer therapy |
| topic | Warburg effect aerobic glycolysis drug discovery cancer hexokinase pyruvate kinase |
| url | https://www.mdpi.com/2813-2998/2/3/37 |
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