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Issue 5, 2016
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Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors

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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.

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

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Publication details

The article was received on 14 Dec 2015, accepted on 19 Feb 2016 and first published on 23 Feb 2016


Article type: Research Article
DOI: 10.1039/C5MD00579E
Citation: Med. Chem. Commun., 2016,7, 900-905
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    Exploiting the co-reliance of tumours upon transport of amino acids and lactate: Gln and Tyr conjugates of MCT1 inhibitors

    R. N. Nair, J. K. Mishra, F. Li, M. Tortosa, C. Yang, J. R. Doherty, M. Cameron, J. L. Cleveland, W. R. Roush and T. D. Bannister, Med. Chem. Commun., 2016, 7, 900
    DOI: 10.1039/C5MD00579E

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