Glycolysis inhibitors for anticancer therapy: A review of recent patents
Abstract
BACKGROUND: The aerobic glycolysis in tumor cells known as Warburg effect is one of the most important hallmarks of cancer. It is proposed that the upregulation of the series of metabolic enzymes along the glycolytic pathway may contribute to the Warburg effect. OBJECTIVES: The inhibition of these glycolytic enzymes has been found to be a novel strategy for anticancer treatment. This review summaries recent patents in the development of small molecule inhibitors for the key enzymes in tumor glycolysis. The targeted enzymes are GLUTs, HKs, PFK, PGAM1, PKM2, LDHA, MCTs and PDK. CONCLUSION: Although most inhibitors are still in the preclinical phase, the inhibition of glycolytic enzymes represents a very promising approach for anticancer treatment. The future development could be more focused on the discovery of new metabolic enzyme that is specifically expressed in tumor cells.
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A number of glycolytic and OxPHOS inhibitors are currently being investigated in preclinical and clinical studies.
“A number of glycolytic and OxPHOS inhibitors are currently being investigated in preclinical and clinical studies [20,77].”
From 20-Hydroxyecdysone Confers Antioxidant and Antineoplastic Properties in Human Non-Small Cell Lung Cancer Cells (2023) · cites this paper as [77]
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- Authors
- Sheng, H., & Tang, W.
- Affiliations
- Purdue University West Lafayette (US)
- Venue
- Recent Patents on Anti-Cancer Drug Discovery
- Publisher
- Bentham Science Publishers Ltd.
- Published
- 2016-08-09
- Volume
- 11
- Issue
- 3
- Pages
- 297-308
- ISSN
- 1574-8928 (ISSN-L)
- OpenAlex
- W2337401400
- Cited by
- 71
- References
- 0
- Citations by year
- 2026: 2 · 2025: 4 · 2024: 6 · 2023: 11 · 2022: 8 · 2021: 5 · 2020: 15 · 2019: 9 · 2018: 7 · 2017: 2 · 2016: 2
- FWCI
- 2.78
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Recent Patents on Anti-Cancer Drug Discovery (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Cancer Research › Cancer, Hypoxia, and Metabolism
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Metabolism, Diabetes, and Cancer
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Biochemical and Molecular Research
- Keywords
- glycolysis inhibitors, Warburg effect, aerobic glycolysis, cancer metabolism, glycolytic enzymes, glucose transporters, hexokinase, phosphoglycerate mutase 1, PKM2, LDHA, monocarboxylate transporters, pyruvate dehydrogenase kinase, small molecule inhibitors, anticancer drug discovery, patents
- MeSH terms
- Pyruvate Dehydrogenase Acetyl-Transferring Kinase, Animals, Antineoplastic Agents, Enzyme Inhibitors, Glycolysis, Hexokinase, Humans, Neoplasms, Patents as Topic, Pyruvate Kinase, Structure-Activity Relationship, Molecular Structure, Protein Serine-Threonine Kinases, Phosphofructokinases, Glucose Transport Proteins, Facilitative, Drug Discovery, Molecular Targeted Therapy
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