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Extraction of Aqueous Metabolites from Cultured Adherent Cells for Metabolomic Analysis by Capillary Electrophoresis-Mass Spectrometry
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Metabolism, a Blossoming Target for Small-Molecule Anticancer Drugs
Michela Puxeddu1, Romano Silvestri1, Giuseppe La Regina1
1Laboratory Affiliated to Istituto Pasteur Italia-Fondazione Cenci Bolognetti, Department of Drug Chemistry and Technologies, Sapienza University of Rome, Piazzale Aldo Moro 5, 00185 Rome, Italy.
Molecules (Basel, Switzerland)
|September 13, 2025
Summary
Targeting cancer cell reprogramming through small molecule inhibitors of key metabolic pathways like glycolysis and glutamine metabolism shows promise for developing effective anticancer agents with reduced toxicity.
Area of Science:
- Oncology
- Metabolic Pathways
- Drug Discovery
Background:
- Cancer cells exhibit altered metabolism, notably increased aerobic glycolysis (Warburg effect), fueling rapid proliferation.
- Reprogramming metabolic pathways is a recognized therapeutic target in cancer treatment.
Purpose of the Study:
- To review recent advancements in small molecule inhibitors targeting key cancer metabolic pathways.
- To analyze the mechanisms of action of these inhibitors against enzymes like LDH, HK2, PKM2, GLS, and FASN.
Main Methods:
- Literature review of small molecule inhibitors.
- Analysis of metabolic pathway modulation in cancer.
- Enzyme-specific targeting strategies.
Main Results:
- Small molecule inhibitors targeting glycolysis, glutamine metabolism, and fatty acid synthesis are under development.
- These inhibitors act through diverse mechanisms, targeting critical enzymes involved in cancer metabolism.
Conclusions:
- Metabolism-based strategies are crucial for developing next-generation anticancer agents.
- Targeting cancer metabolism offers potential for improved efficacy and reduced systemic toxicity.
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