Transport mechanisms of 3-[123I]iodo-alpha-methyl-L-tyrosine in a human glioma cell line: comparison with [3H]methyl]-L-methionine

J Nucl Med. 2000 Jul;41(7):1250-5.

Abstract

The amino acid analog 3-[(123)I]iodo-alpha-methyl-L-tyrosine (IMT) is under clinical evaluation as a SPECT tracer of amino acid transport in brain tumors. This study investigated the carrier systems involved in IMT transport in human glioma cells in comparison with [3H-methyl]-L-methionine (3H-MET).

Methods: Human glioma cells, type 86HG-39, were cultured and incubated for 1 min at 37 degrees C with IMT and 3H-MET in the lag phase (1.2 d after seeding), exponential growth phase (3 d after seeding), and plateau phase (8 d after seeding). Experiments were performed in the presence and absence of Na+, during inhibition of system L amino acid transport by 2-aminobicyclo[2.2.1 ]heptane-2-carboxylic acid (BCH), and during inhibition of system A amino acid transport by 2-(methylamino)-isobutyric acid (MeAIB).

Results: IMT and 3H-MET uptake decreased by 55%-73% when the cells entered from the exponential growth phase into the plateau phase (P< 0.05; n = 3-11). Inhibition by BCH reduced uptake of IMT in the lag phase, exponential growth phase, and plateau phase by 90%-98% (P < 0.001; n = 3-6) and the uptake of 3H-MET by 73%-83% (P < 0.001; n = 3-11). In a Na+-free medium 3H-MET uptake was reduced by 23%-33% (P < 0.05; n = 3-11), whereas IMT uptake was not significantly different. MeAIB showed no significant effect on IMT or 3H-MET uptake in either phase.

Conclusion: Transport of both IMT and 3H-MET depends on the proliferation rate of human glioma cells in vitro and is dominated by BCH-sensitive transport. These data indicate that system L is induced in rapidly proliferating glioma cells and is the main contributor to the uptake of both tracers. 3H-MET transport showed a minor Na+ dependency that was not attributable to system A. The similarity of transport mechanisms of both tracers emphasizes the clinical equivalence of IMT SPECT and (11)C-MET PET for the diagnostic evaluation of gliomas.

Publication types

  • Comparative Study

MeSH terms

  • Amino Acids / pharmacology
  • Amino Acids, Cyclic*
  • Aminoisobutyric Acids / pharmacology
  • Biological Transport
  • Blood-Brain Barrier
  • Brain Neoplasms / diagnostic imaging
  • Brain Neoplasms / metabolism*
  • Brain Neoplasms / pathology
  • Cell Division
  • Glioblastoma / diagnostic imaging
  • Glioblastoma / metabolism*
  • Glioblastoma / pathology
  • Humans
  • In Vitro Techniques
  • Methionine / analogs & derivatives
  • Methionine / pharmacokinetics*
  • Methyltyrosines / pharmacokinetics*
  • Radiopharmaceuticals / pharmacokinetics*
  • Tomography, Emission-Computed
  • Tomography, Emission-Computed, Single-Photon
  • Tumor Cells, Cultured / metabolism
  • Tumor Cells, Cultured / pathology

Substances

  • Amino Acids
  • Amino Acids, Cyclic
  • Aminoisobutyric Acids
  • Methyltyrosines
  • Radiopharmaceuticals
  • 2-aminobicyclo(2,2,1)heptane-2-carboxylic acid
  • 2-(methylamino)isobutyric acid
  • 3-iodo-alpha-methyltyrosine
  • Methionine