Design, synthesis, and biological activity of novel triazole amino acids used to probe binding interactions between ligand and neutral amino acid transport protein SN1 |
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Authors: | Gajewski Mariusz Seaver Ben Esslinger C Sean |
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Institution: | NIH-COBRE Center for Structural and Functional Neuroscience, Department of Pharmaceutical and Biomedical Sciences, The University of Montana, Missoula, MT 59812, USA. |
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Abstract: | Novel triazole amino acids were synthesized as probes to investigate ligand-protein binding interactions of the neutral amino acid transporter SN1. The bonding hypothesis to be tested was that the side chains of endogenous substrates are acting as H-bond acceptors. Although limited inhibition of (3)H-L-glutamine uptake by SN1 expressing oocytes was observed, the synthetic compounds show a trend that suggests a hydrogen bond interaction just outside the endogenous ligand binding pocket. |
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