A simple route to [11C]N-Me labeling of aminosuberic acid for proof of feasibility imaging of the x(C)⁻ transporter

Bioorg Med Chem Lett. 2014 Dec 1;24(23):5512-5. doi: 10.1016/j.bmcl.2014.10.004. Epub 2014 Oct 13.

Abstract

Oxidative stress has been implicated in a variety of conditions, including cancer, heart failure, diabetes, neurodegeneration and other diseases. A potential biomarker for oxidative stress is the cystine/glutamate transporter, system x(C)(-). L-Aminosuberic acid (L-ASu) has been identified as a system x(C)(-) substrate. Here we report a facile method for [(11)C]N-Me labeling of L-ASu, automation of the radiochemical process, and preliminary PET imaging with EL4 tumor bearing mice. The results demonstrate uptake in the tumor above background, warranting further studies on the use of radiolabeled analogs of L-ASu as a PET imaging agent for system x(C)(-).

Keywords: C-11; Cystine transporter; N-methylation; Oxidative stress; Radiolabelling.

MeSH terms

  • Amino Acid Transport System y+ / metabolism
  • Amino Acids, Dicarboxylic / metabolism*
  • Animals
  • Cells, Cultured
  • Diagnostic Imaging / methods*
  • Membrane Transport Proteins
  • Mice
  • Molecular Structure
  • Neoplasms / metabolism*
  • Oxidative Stress
  • Up-Regulation

Substances

  • Amino Acid Transport System y+
  • Amino Acids, Dicarboxylic
  • Membrane Transport Proteins
  • 2-aminosuberic acid