Abstract
3-bromopyruvate (3-BrPA), a pyruvate analog recently proposed as a possible anticancer drug, was investigated in relation to its capacity to inhibit energy production in fractions obtained from normal cells (rat hepatocytes) and in isolated rat thymocytes. Findings were that main targets of the drug were glyceraldehyde 3-phosphate dehydrogenase, and not hexokinase as suggested for hepatoma cells, and succinate -driven ATP synthesis. Consistently with the above findings, in the normal cells studied (thymocytes) the drug elicited an important fall in ATP levels. The significance of the present findings in concern with a possible therapeutic usefulness of the drug is discussed.
Keywords: 3-Bromopyruvate, Warburg effect, tumor therapy, glycolysis, hexokinase, glyceraldehyde-3-phosphate dehydrogenase, oxidative phosphorylation, succinate dehydrogenase
Medicinal Chemistry
Title: Targets of 3-Bromopyruvate, A New, Energy Depleting, Anticancer Agent
Volume: 5 Issue: 6
Author(s): P. Dell'Antone
Affiliation:
Keywords: 3-Bromopyruvate, Warburg effect, tumor therapy, glycolysis, hexokinase, glyceraldehyde-3-phosphate dehydrogenase, oxidative phosphorylation, succinate dehydrogenase
Abstract: 3-bromopyruvate (3-BrPA), a pyruvate analog recently proposed as a possible anticancer drug, was investigated in relation to its capacity to inhibit energy production in fractions obtained from normal cells (rat hepatocytes) and in isolated rat thymocytes. Findings were that main targets of the drug were glyceraldehyde 3-phosphate dehydrogenase, and not hexokinase as suggested for hepatoma cells, and succinate -driven ATP synthesis. Consistently with the above findings, in the normal cells studied (thymocytes) the drug elicited an important fall in ATP levels. The significance of the present findings in concern with a possible therapeutic usefulness of the drug is discussed.
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Cite this article as:
Dell'Antone P., Targets of 3-Bromopyruvate, A New, Energy Depleting, Anticancer Agent, Medicinal Chemistry 2009; 5 (6) . https://dx.doi.org/10.2174/157340609790170551
DOI https://dx.doi.org/10.2174/157340609790170551 |
Print ISSN 1573-4064 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6638 |
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