Imaging cancer L-amino acid transporter system with Tc-99m-labeled alpha-methyltyrosine

TL;DRAbstract

1537 Objectives This study was to develop a 99mTc-labeled α-methyl tyrosine (AMT) using L,L- ethylenedicysteine (EC) as a chelator and evaluate its imaging potential in breast tumor-bearing rats. Methods The amino and acid groups of AMT were protected with tert-butyloxycarbonyl (BOC) and ethyl ester. Dibromopropane was then reacted with protected AMT to afford 3-bromopropyl AMT (N-BOC, ethyl ester). EC-AMT was synthesized by reacting EC and 3-bromopropyl AMT (N-BOC, ethyl ester) in the solution of ethanol/potassium carbonate. After de-BOC and de-ester, EC-AMT was labeled with 99mTc in the presence of tin (II) chloride. Rhenium-EC-AMT was synthesized by reacting EC-AMT with rhenium (oxo) trichloride, and used as a reference standard for 99mTc-EC-AMT. To assess the cellular uptake kinetics, 13762 rat breast cancer cells (50,000 cells/well) were incubated with 99mTc-EC-AMT at 0-2 h. To investigate the amino acid transport mechanism, same cell line was used to conduct the competitive inhib

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