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Nair RN, Mishra JK, Li F, et al. Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors. Medchemcomm. 2016;7(5):900-905doi: 10.1039/C5MD00579E.
Nair, R. N., Mishra, J. K., Li, F., Tortosa, M., Yang, C., Doherty, J. R., Cameron, M., Cleveland, J. L., Roush, W. R., & Bannister, T. D. (2016). Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors. MedChemComm, 7(5), 900-905. https://doi.org/10.1039/C5MD00579E
Nair, Reji N, et al. "Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors." MedChemComm vol. 7,5 (2016): 900-905. doi: https://doi.org/10.1039/C5MD00579E
Nair RN, Mishra JK, Li F, Tortosa M, Yang C, Doherty JR, Cameron M, Cleveland JL, Roush WR, Bannister TD. Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors. Medchemcomm. 2016 May 01;7(5):900-905. doi: 10.1039/C5MD00579E. Epub 2016 Feb 23. PMID: 27347360; PMCID: PMC4917231.
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Medchemcomm. 2016 May 01;7(5):900-905. doi: 10.1039/C5MD00579E. Epub 2016 Feb 23.

Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors.

MedChemComm

Reji N Nair, Jitendra K Mishra, Fangzheng Li, Mariola Tortosa, Chunying Yang, Joanne R Doherty, Michael Cameron, John L Cleveland, William R Roush, Thomas D Bannister

Affiliations

  1. Department of Chemistry, The Scripps Research Institute, 110 Scripps Way, Jupiter, FL 33458, USA.
  2. Department of Tumor Biology, Moffitt Cancer Center & Research Institute, 12902 Magnolia Drive, Tampa, FL 33612, USA.
  3. Department of Cancer Biology, The Scripps Research Institute, 110 Scripps Way, Jupiter, FL 33458, USA.
  4. Department of Molecular Therapeutics, The Scripps Research Institute, 110 Scripps Way, Jupiter, FL 33458, USA.

PMID: 27347360 PMCID: PMC4917231 DOI: 10.1039/C5MD00579E

Abstract

Glutamine and tyrosine-based amino acid conjugates of monocarboxylate transporter types 1 and 2 inhibitors (MCT1/2) were designed, synthesized and evaluated for their potency in blocking the proliferation of a human B lymphoma cell line that expresses the transporters Asct2, LAT1 and MCT1. Appropriate placement of an amino acid transporter recognition element was shown to augment anti-tumour efficacy vs. Raji cells. Amino acid conjugation also improves the pharmacodynamic properties of experimental MCT1/2 inhibitors.

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