Design, synthesis, and biological activity of novel triazole amino acids used to probe binding interactions between ligand and neutral amino acid transport protein SN1.
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.
Gajewski
Mariusz
M
NIH-COBRE Center for Structural and Functional Neuroscience, Department of Pharmaceutical and Biomedical Sciences, The University of Montana, Missoula, MT 59812, USA.
Seaver
Ben
B
Esslinger
C Sean
CS
D026921:Amino Acid Transport Systems, Neutral / Q000737:chemistry / Q000378:metabolism*; D000596:Amino Acids / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000818:Animals; D006860:Hydrogen Bonding; D008024:Ligands; D008958:Models, Molecular; D015335:Molecular Probes; D051381:Rats; D014230:Triazoles / Q000737:chemistry*; D014981:Xenopus
D026921:Amino Acid Transport Systems, Neutral; D000596:Amino Acids; D008024:Ligands; D015335:Molecular Probes; D014230:Triazoles; C403222:system N protein 1