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The anticancer agent 3-bromopyruvate: a simple but powerful molecule taken from the lab to the bedside

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Abstract

At the beginning of the twenty-first century, 3-bromopyruvate (3BP), a simple alkylating chemical compound was presented to the scientific community as a potent anticancer agent, able to cause rapid toxicity to cancer cells without bystander effects on normal tissues. The altered metabolism of cancers, an essential hallmark for their progression, also became their Achilles heel by facilitating 3BP’s selective entry and specific targeting. Treatment with 3BP has been administered in several cancer type models both in vitro and in vivo, either alone or in combination with other anticancer therapeutic approaches. These studies clearly demonstrate 3BP’s broad action against multiple cancer types. Clinical trials using 3BP are needed to further support its anticancer efficacy against multiple cancer types thus making it available to more than 30 million patients living with cancer worldwide. This review discusses current knowledge about 3BP related to cancer and discusses also the possibility of its use in future clinical applications as it relates to safety and treatment issues.

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Acknowledgments

This work was supported by the strategic programme UID/BIA/04050/2013 (POCI-01-0145-FEDER-007569) funded by national funds through the FCT I.P. and by the ERDF through the COMPETE2020 - Programa Operacional Competitividade e Internacionalização (POCI). João Azevedo-Silva received a fellowship from the Portuguese government from the FCT through FSE (Fundo Social Europeu) and POPH (Programa Operacional Potencial Humano) [grant number SFRH/BD/76038/2011]. Co-author Peter L. Pedersen was supported by NIH grant NCI CA l0951 for many years for cancer research that led to a number of the findings described in this review.

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Authors and Affiliations

  1. Centre of Molecular and Environmental Biology (CBMA), Department of Biology, University of Minho, Portugal, Campus de Gualtar, 4710-057, Braga, Portugal

    J. Azevedo-Silva, O. Queirós, A. Preto & M. Casal

  2. CESPU, Instituto de Investigação e Formação Avançada em Ciências e Tecnologias da Saúde, Rua Central de Gandra, 1317, 4585-116, Gandra, PRD, Portugal

    O. Queirós

  3. Life and Health Sciences Research Institute (ICVS), School of Health Sciences, University of Minho, Campus de Gualtar, 4710-057, Braga, Portugal

    F. Baltazar

  4. ICVS/3B’s - PT Government Associate Laboratory, Guimarães, Braga, Portugal

    F. Baltazar

  5. Institute of Genetics and Microbiology, University of Wroclaw, Przybyszewskiego 63/77, 51-148, Wroclaw, Poland

    S. Ułaszewski

  6. Institut des Sciences de la Vie, Université Catholique de Louvain-la-Neuve, 1, Place de l’Université, 1348, Louvain-la-Neuve, Belgium

    A. Goffeau

  7. KoDiscovery, LLC, University of Maryland BioPark, Suites 502 E & F, 801 West Baltimore St, Baltimore, MD, 21201, USA

    Y. H. Ko

  8. Departments of Biological Chemistry and Oncology, Member at Large, Sidney Kimmel Comprehensive Cancer Center, School of Medicine, John Hopkins University, Baltimore, 21205-2185, USA

    P. L. Pedersen

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  1. J. Azevedo-Silva
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  8. A. Preto
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  9. M. Casal
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Azevedo-Silva, J., Queirós, O., Baltazar, F. et al. The anticancer agent 3-bromopyruvate: a simple but powerful molecule taken from the lab to the bedside. J Bioenerg Biomembr 48, 349–362 (2016). https://doi.org/10.1007/s10863-016-9670-z

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