Targets of 3-Bromopyruvate, A New, Energy Depleting, Anticancer Agent

Author(s): P. Dell'Antone

Journal Name: Medicinal Chemistry

Volume 5 , Issue 6 , 2009

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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

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Article Details

Year: 2009
Page: [491 - 496]
Pages: 6
DOI: 10.2174/157340609790170551
Price: $65

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