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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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Supplementary files

Article information


Submitted
14 Dec 2015
Accepted
19 Feb 2016
First published
23 Feb 2016

Med. Chem. Commun., 2016,7, 900-905
Article type
Research Article

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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