Medicinal Chemistry

Atta-ur-Rahman  
Honorary Life Fellow
Kings College
University of Cambridge
Cambridge
UK
Email: mc@benthamscience.org

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

Author(s): P. Dell'Antone

Affiliation: Dipartimento di Scienze Biomediche Sperimentali, Universita di Padova, Italy.

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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Article Details

VOLUME: 5
ISSUE: 6
Page: [491 - 496]
Pages: 6
DOI: 10.2174/157340609790170551