Design, synthesis, and biological activity of novel triazole amino acids used to probe binding interactions between ligand and neutral amino acid transport protein SN1

Bioorg Med Chem Lett. 2007 Aug 1;17(15):4163-6. doi: 10.1016/j.bmcl.2007.05.061. Epub 2007 May 23.

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.

Publication types

  • Research Support, N.I.H., Extramural

MeSH terms

  • Amino Acid Transport Systems, Neutral / chemistry
  • Amino Acid Transport Systems, Neutral / metabolism*
  • Amino Acids / chemical synthesis
  • Amino Acids / chemistry*
  • Amino Acids / pharmacology*
  • Animals
  • Hydrogen Bonding
  • Ligands
  • Models, Molecular
  • Molecular Probes
  • Rats
  • Triazoles / chemistry*
  • Xenopus

Substances

  • Amino Acid Transport Systems, Neutral
  • Amino Acids
  • Ligands
  • Molecular Probes
  • Triazoles
  • system N protein 1