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Published on: May 12, 2020
Targeting aerobic glycolysis: 3-bromopyruvate as a promising anticancer drug
Simone Cardaci1, Enrico Desideri, Maria Rosa Ciriolo
1Department of Biology, University of Rome Tor Vergata, Via della Ricerca Scientifica, 00133 Rome, Italy.
Abstract:
The Warburg effect refers to the phenomenon whereby cancer cells avidly take up glucose and produce lactic acid under aerobic conditions. Although the molecular mechanisms underlying tumor reliance on glycolysis remains not completely clear, its inhibition opens feasible therapeutic windows for cancer treatment. Indeed, several small molecules have emerged by combinatorial studies exhibiting promising anticancer activity both in vitro and in vivo, as a single agent or in combination with other therapeutic modalities. Therefore, besides reviewing the alterations of glycolysis that occur with malignant transformation, this manuscript aims at recapitulating the most effective pharmacological therapeutics of its targeting. In particular, we describe the principal mechanisms of action and the main targets of 3-bromopyruvate, an alkylating agent with impressive antitumor effects in several models of animal tumors. Moreover, we discuss the chemo-potentiating strategies that would make unparalleled the putative therapeutic efficacy of its use in clinical settings.
Insights
Cancer cells utilize glucose excessively via the Warburg effect. Targeting this glycolysis pathway with drugs like 3-bromopyruvate offers promising cancer treatment strategies, enhancing therapeutic efficacy.
Area of Science:
- Biochemistry
- Oncology
- Pharmacology
Background:
- The Warburg effect describes increased glucose uptake and lactate production in cancer cells under aerobic conditions.
- While the exact mechanisms are unclear, targeting tumor glycolysis presents therapeutic opportunities.
- Several small molecules show anticancer potential in vitro and in vivo.
Purpose of the Study:
- To review metabolic alterations in malignant transformation.
- To summarize effective pharmacological therapies targeting glycolysis.
- To detail the mechanism of action and targets of 3-bromopyruvate.
Main Methods:
- Review of scientific literature on glycolysis and cancer.
- Analysis of small molecules targeting cancer metabolism.
- Focus on 3-bromopyruvate's antitumor effects and mechanisms.
Main Results:
- 3-bromopyruvate, an alkylating agent, demonstrates significant antitumor activity in animal models.
- Discussion of strategies to potentiate 3-bromopyruvate's efficacy.
Conclusions:
- Targeting the Warburg effect is a viable cancer treatment strategy.
- 3-bromopyruvate shows promise as an anticancer agent.
- Combination therapies may enhance clinical efficacy.
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