Glycolysis is often upregulated in tumour cells but it can be inhibited by 3-bromopyruvate. Birsoy and colleagues found that monocarboxylate transporter 1 (MCT1) is required for 3-bromopyruvate uptake. The expression of SLC16A1 (which encodes MCT1) mRNA is a determinant of tumour cell sensitivity to 3-bromopyruvate, and its forced expression in tumour cells rendered xenografts sensitive to 3-bromopyruvate, indicating that MCT1 could be a biomarker of sensitivity to this drug.
ORIGINAL RESEARCH PAPER
Birsoy, K. et al. MCT1-mediated transport of a toxic molecule is an effective strategy for targeting glycolytic tumors. Nature Genet. 2 Dec 2012 (doi:10.1038/ng.2471)
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Alderton, G. Transporting drugs. Nat Rev Cancer 13, 7 (2013). https://doi.org/10.1038/nrc3443
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DOI: https://doi.org/10.1038/nrc3443