A translational study "case report" on the small molecule "energy blocker" 3-bromopyruvate (3BP) as a potent anticancer agent: From bench side to bedside

Y. H. Ko, H. A. Verhoeven, M. J. Lee, D. J. Corbin, T. J. Vogl, P. L. Pedersen

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135 Scopus citations


The small alkylating molecule, 3-bromopyruvate (3BP), is a potent and specific anticancer agent. 3BP is different in its action from most currently available chemo-drugs. Thus, 3BP targets cancer cells' energy metabolism, both its high glycolysis ("Warburg Effect") and mitochondrial oxidative phosphorylation. This inhibits/ blocks total energy production leading to a depletion of energy reserves. Moreover, 3BP as an "Energy Blocker", is very rapid in killing such cells. This is in sharp contrast to most commonly used anticancer agents that usually take longer to show a noticeable effect. In addition, 3BP at its effective concentrations that kill cancer cells has little or no effect on normal cells. Therefore, 3BP can be considered a member, perhaps one of the first, of a new class of anticancer agents. Following 3BP's discovery as a novel anticancer agent in vitro in the Year 2000 (Published in Ko et al. Can Lett 173:83-91, 2001), and also as a highly effective and rapid anticancer agent in vivo shortly thereafter (Ko et al. Biochem Biophys Res Commun 324:269-275, 2004), its efficacy as a potent anticancer agent in humans was demonstrated. Here, based on translational research, we report results of a case study in a young adult cancer patient with fibrolamellar hepatocellular carcinoma. Thus, a bench side discovery in the Department of Biological Chemistry at Johns Hopkins University, School of Medicine was taken effectively to bedside treatment at Johann Wolfgang Goethe University Frankfurt/Main Hospital, Germany. The results obtained hold promise for 3BP as a future cancer therapeutic without apparent cyto-toxicity when formulated properly.

Original languageEnglish
Pages (from-to)163-170
Number of pages8
JournalJournal of Bioenergetics and Biomembranes
Issue number1
StatePublished - Feb 2012

Bibliographical note

Funding Information:
Acknowledgements Work reported here was supported in part by NIH grants CA 10951 and CA 08018 to PLP. YHK is very grateful to PLP’s lab members, her Ph.D. thesis advisor, Dr. Bruce McFadden (Washington State University, Pullman, WA), Dr. André Goffeau (Université Catholique de Louvain, Louvain-la-Neuve, Belgium), Dr. Scott Mogel (Aalto Scientific, Ltd., Carlsbad, CA), Dr. Pam Meyer (Marbella, Spain), the honorable Judge Gregory Hopkins (Aurora, CO), Moshe Rogosnitzky (Adjuvant Medical Solutions, Telz Stone, Israel), Ilona McClintick (Baltimore, MD), and the Grow family (Murray, UT) who have been very supportive of her efforts to fight cancer. The authors are very grateful also to David Blum (JHU, Baltimore, MD) for his assistance with the artwork, Jos Kaldenhoven (Schijndel, the Netherlands) for photography and his expertise as a nurse, Dr. Dwight McKee (Life Plus International in Batesville, AR) and Dr. George Sack (JHU, Baltimore, MD) for carefully reading the Case Report and for helpful comments.


  • 3-bromopyruvate
  • Cancer
  • Fibrolamellar carcinoma
  • Hexokinase 2
  • Liver cancer
  • Mitochondria
  • Positron Emission Tomography (PET)
  • Warburg Effect


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