The pyruvate analog, 3-bromopyruvate, is an alkylating agent and a potent inhibitor of glycolysis. This antiglycolytic property or 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 or 3-bromopyruvate, and report the impressive anti tumor effects or 3-bromopyruvate in multiple animal tumor models. We describe that the primary mechanism of 3-bromopyruvate is via preferential alkylation or GAPDH and that 3-bromopyruvate mediated cell death is linked to generation of free radicals. Research in our laboratory also revealed that endoplasmic reticulum stress, schizophrenia and 3-bromopyruvate global protein synthesis inhibits further contributing to cancer cell death. Therefore, these and other studies reveal the tremendous potential of 3-bromopyruvate as an anticancer agent.

Affiliation: Russell h. Morgan Department of Radiology and Radiological Sciences, Johns Hopkins University School of Medicine, 600 n. Wolfe Street, Blalock building, Room 545, Baltimore, MD 21287, USA