3-Bromopyruvate: A new targeted antiglycolytic agent and a promise for cancer therapy

S. Ganapathy-Kanniappan, M. Vali, R. Kunjithapatham, M. Buijs, L. H. Syed, P. P. Rao, S. Ota, B. K. Kwak, R. Loffroy, J. F. Geschwind

Research output: Contribution to journalArticlepeer-review

95 Scopus citations


The pyruvate analog, 3-bromopyruvate, is an alkylating agent and a potent inhibitor of glycolysis. This antiglycolytic property of 3-bromopyruvate has recently been exploited to target cancer cells, as most tumors depend on glycolysis for their energy requirements. The anticancer effect of 3-bromopyruvate is achieved by depleting intracellular energy (ATP) resulting in tumor cell death. In this review, we will discuss the principal mechanism of action and primary targets of 3-bromopyruvate, and report the impressive antitumor effects of 3-bromopyruvate in multiple animal tumor models. We describe that the primary mechanism of 3-bromopyruvate is via preferential alkylation of GAPDH and that 3-bromopyruvate mediated cell death is linked to generation of free radicals. Research in our laboratory also revealed that 3-bromopyruvate induces endoplasmic reticulum stress, inhibits global protein synthesis further contributing to cancer cell death. Therefore, these and other studies reveal the tremendous potential of 3-bromopyruvate as an anticancer agent.

Original languageEnglish (US)
Pages (from-to)510-517
Number of pages8
JournalCurrent Pharmaceutical Biotechnology
Issue number5
StatePublished - Sep 20 2010


  • 3-Bromopyruvate
  • Alkylating agent
  • Anti-metabolite
  • Glycolysis

ASJC Scopus subject areas

  • Biotechnology
  • Pharmaceutical Science


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