l-Type amino acid transporter 1 activity of 1,2,3-triazolyl analogs of l-histidine and l-tryptophan.

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ID: 1876
2019
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Abstract
A series of 1,2,3-triazole analogs of the amino acids l-histidine and l-tryptophan were modeled, synthesized and tested for l-type amino acid transporter 1 (LAT1; SLC7A5) activity to guide the design of amino acid-drug conjugates (prodrugs). These triazoles were conveniently prepared by the highly convergent Huisgen 1,3-dipolar cycloaddition (Click Chemistry). Despite comparable predicted binding modes, triazoles generally demonstrated reduced cell uptake and LAT1 binding potency relative to their natural amino acid counterparts. The structure-activity relationship (SAR) data for these triazoles has important ramifications for treating cancer and brain disorders using amino acid prodrugs or LAT1 inhibitors.
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hall2019ltypebioorganic Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors Colton Hall, Hannah Wolfe, Alyssa Wells, Huan-Chieh Chien, Claire Colas, Avner Schlessinger, Kathleen M Giacomini, Allen A Thomas
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Journal Bioorganic & medicinal chemistry letters
Year 2019
DOI
S0960-894X(19)30414-7
URL
Keywords Keywords not found

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