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An Update on Patents Covering Agents That Interfere with the Cancer Glycolytic Cascade
Serena Fortunato1, Giulia Bononi1, Carlotta Granchi1
1Dipartimento di Farmacia, Università di Pisa, Via Bonanno 33, 56126, Pisa, Italy.
Abstract:
Many tumors exhibit altered metabolic characteristics relative to normal and healthy tissues. Their metabolic profile highlights a strong prevalence of glycolysis over oxidative phosphorylation, regardless of their exposure to different oxygen levels (the Warburg effect). This condition originates from a set of gene regulations, consisting of the overexpression of some enzymes or transporters involved in the glycolytic pathway. Therefore, these effectors may constitute appealing targets for the implementation of selective therapeutic interventions against cancer. Recently, significant progress has been made in the discovery of molecules that act at various levels of the glycolytic pathway of tumor cells. So far, some of the most widely explored targets of the glycolytic cascade are represented by glucose transporters, hexokinase, 6-phosphofructokinase, enolase, pyruvate kinase, lactate dehydrogenase, and monocarboxylate transporters. The purpose of this minireview is to provide an update on some of the most recently patented bioactive molecules that are able to interfere with cancer glycolysis, and on their use in specific combination therapies.
Insights
Cancer cells heavily rely on glycolysis, a metabolic process, for energy. New research highlights recently patented molecules targeting this pathway, offering potential for novel cancer therapies and combination treatments.
Area of Science:
- Biochemistry
- Oncology
- Metabolic pathways
Background:
- Tumors display altered metabolism, favoring glycolysis over oxidative phosphorylation (the Warburg effect), irrespective of oxygen availability.
- This metabolic shift is driven by gene regulation leading to overexpression of glycolytic enzymes and transporters.
- These glycolytic components represent promising targets for selective anti-cancer therapies.
Purpose of the Study:
- To review recently patented bioactive molecules targeting cancer glycolysis.
- To update on the application of these molecules in combination therapies.
Main Methods:
- Literature review of recent patents.
- Analysis of molecules interfering with key glycolytic targets.
- Examination of combination therapy strategies.
Main Results:
- Identification of novel patented molecules targeting glucose transporters, hexokinase, 6-phosphofructokinase, enolase, pyruvate kinase, lactate dehydrogenase, and monocarboxylate transporters.
- Overview of emerging combination therapies utilizing these targeted molecules.
Conclusions:
- Targeting cancer cell glycolysis with novel molecules shows therapeutic potential.
- Combination therapies involving these agents may enhance anti-cancer efficacy.
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