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Cited by 228

The DOI matches its Crossref record; 5 of the 5 references it cites were found in a registry or an index.

MCT1-mediated transport of a toxic molecule is an effective strategy for targeting glycolytic tumors

Open access
Birsoy, Kivanç, Wang, Tim, Possemato, Richard, Yilmaz, Omer H, Koch, Catherine E, Chen, Walter W, Hutchins, Amanda W, Gultekin, Yetis, Peterson, Tim R, Carette, Jan E, Brummelkamp, Thijn R, Clish, Clary B, Sabatini, David M·2013·Nature Genetics
DOI 10.1038/ng.2471
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Abstract

There is increasing evidence that oncogenic transformation modifies the metabolic program of cells. A common alteration is the upregulation of glycolysis, and efforts to target glycolytic enzymes for anticancer therapy are under way. Here, we performed a genome-wide haploid genetic screen to identify resistance mechanisms to 3-bromopyruvate (3-BrPA), a drug candidate that inhibits glycolysis in a poorly understood fashion. We identified the SLC16A1 gene product, MCT1, as the main determinant of 3-BrPA sensitivity. MCT1 is necessary and sufficient for 3-BrPA uptake by cancer cells. Additionally, SLC16A1 mRNA levels are the best predictor of 3-BrPA sensitivity and are most elevated in glycolytic cancer cells. Furthermore, forced MCT1 expression in 3-BrPA–resistant cancer cells sensitizes tumor xenografts to 3-BrPA treatment in vivo. Our results identify a potential biomarker for 3-BrPA sensitivity and provide proof of concept that the selectivity of cancer-expressed transporters can be exploited for delivering toxic molecules to tumors.

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Metadata

Authors
Birsoy, K., Wang, T., Possemato, R., Yilmaz, O. H., Koch, C. E., Chen, W. W., Hutchins, A. W., Gultekin, Y., Peterson, T. R., Carette, J. E., Brummelkamp, T. R., Clish, C. B., & Sabatini, D. M.
Venue
Nature Genetics
Publisher
Springer Science and Business Media LLC
Published
2012-12-02
Volume
45
Issue
1
Pages
104-108
ISSN
  • 1061-4036 (ISSN-L)
  • 1546-1718
DOI
10.1038/ng.2471
OpenAlex
W2081651784
Cited by
228
References
5
FWCI
7.92
Type
journal article
Language
en
Open access
green

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CoChat. (2026). Citation check: MCT1-mediated transport of a toxic molecule is an effective strategy for targeting glycolytic tumors. https://app.cochat.ai/papers/10.1038/ng.2471
The paper
Birsoy, K., Wang, T., Possemato, R., Yilmaz, O. H., Koch, C. E., Chen, W. W., Hutchins, A. W., Gultekin, Y., Peterson, T. R., Carette, J. E., Brummelkamp, T. R., Clish, C. B., & Sabatini, D. M. (2013). MCT1-mediated transport of a toxic molecule is an effective strategy for targeting glycolytic tumors. Nature Genetics. https://doi.org/10.1038/ng.2471

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.