Synthesis of 99mTc-EC-AMT as an imaging probe for amino acid transporter systems in breast cancer

Kong, Fan Lin; Zhang, Yinhan; Ali, Mohammad; Oh, Chanksok; Mendez, Richard; Kohanim, Saady; Tsao, Ning; Chanda, Mithu; Huang, Wen Chien; Yang, David J.

doi:10.1097/mnm.0b013e328339ea48

Cited by 7 publications

(2 citation statements)

References 21 publications

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“…High uptake was found in the kidneys, which was consistent with the planar scintigraphic imaging findings in the breast tumor-bearing rats (see Figure 5). This high kidney uptake may be a result of the low lipophilicity of 99m Tc-N4-Tyrosine, or it may be related to the biological characteristics of 99m Tc-labeled tyrosine because similar results were also observed in the previously developed tyrosine-based radiotracers 99m Tc-N4-AMT, 99m Tc-EC-AMT, and 99m Tc-EC-Tyrosine [14, 15]. …”

Section: Resultsmentioning

confidence: 54%

Development of Tyrosine-Based RadiotracerTc99m-N4-Tyrosine for Breast Cancer Imaging

Kong

Ali

Rollo

et al. 2012

Journal of Biomedicine and Biotechnology

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The purpose of this study was to develop an efficient way to synthesize 99mTc-O-[3-(1,4,8,11-tetraazabicyclohexadecane)-propyl]-tyrosine (99mTc-N4-Tyrosine), a novel amino acid-based radiotracer, and evaluate its potential in breast cancer gamma imaging. Precursor N4-Tyrosine was synthesized using a 5-step procedure, and its total synthesis yield was 38%. It was successfully labeled with 99mTc with high radiochemical purity (>95%). Cellular uptake of 99mTc-N4-Tyrosine was much higher than that of 99mTc-N4 and the clinical gold standard 18F-2-deoxy-2-fluoro-glucose (18F-FDG) in rat breast tumor cells in vitro. Tissue uptake and dosimetry estimation in normal rats revealed that 99mTc-N4-Tyrosine could be safely administered to humans. Evaluation in breast tumor-bearing rats showed that although 99mTc-N4-Tyrosine appeared to be inferior to 18F-FDG in distinguishing breast tumor tissue from chemical-induced inflammatory tissue, it had high tumor-to-muscle uptake ratios and could detect breast tumors clearly by planar scintigraphic imaging. 99mTc-N4-Tyrosine could thus be a useful radiotracer for use in breast tumor diagnostic imaging.

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Section: Resultsmentioning

confidence: 54%

Development of Tyrosine-Based RadiotracerTc99m-N4-Tyrosine for Breast Cancer Imaging

Kong

Ali

Rollo

et al. 2012

Journal of Biomedicine and Biotechnology

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“…It is transported into glioma cells mainly by system L. However, [ 123 I]IMT is cleared rapidly, so that imaging must be performed within 45 min [ 19 ]. Tyrosine analogs with 99m Tc labels, such as [ 99m Tc]Tc-EC-AMT (EC: L,L -ethylenedicysteine, AMT: α-methyl tyrosine) and [ 99m Tc]Tc-EC-tyrosine, have attracted more attention, and the transport of both tracers involves system L [ 20 ]. However, the synthesis process of the 99m Tc-labeled compounds is complex, and the yield is low, so the clinical application is limited.…”

Section: Introductionmentioning

confidence: 99%

Radiolabeling and Biological Evaluation of Novel 99mTc-Nitrido and 99mTc-Oxo Complexes with 4-Methoxy-L-Phenylalanine Dithiocarbamate for Tumor Imaging

et al. 2022

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To develop novel radiolabeled amino acid tumor imaging agents, 4-methoxy-L-phenylalanine dithiocarbamate (MOPADTC) was synthesized successfully, and two kinds of 99mTc-labeled complexes ([99mTc]TcN-MOPADTC and [99mTc]TcO-MOPADTC) with high radiochemical purities (RCP > 95%) were obtained. The in vitro stability and partition coefficient were determined, and the results show that both of these complexes have good in vitro stability; [99mTc]TcO-MOPADTC is hydrophilic, while [99mTc]TcN-MOPADTC is slightly lipophilic. The biodistribution of [99mTc]TcN-MOPADTC and [99mTc]TcO-MOPADTC in mice bearing S180 tumors shows that the tumor uptake and tumor/muscle ratio of [99mTc]TcO-MOPADTC were higher than the tumor uptake and tumor/muscle ratio of [99mTc]TcN-MOPADTC. In addition, the tumor retention of [99mTc]TcO-MOPADTC is better than the tumor retention of [99mTc]TcN-MOPADTC. A competitive inhibition assay was performed, and the results indicate that [99mTc]TcO-MOPADTC may enter cells primarily via the L-alanine/L-serine/L-cysteine (ASC) system. Single-photon emission computed tomography (SPECT) imaging of [99mTc]TcO-MOPADTC shows obvious accumulation in tumor sites, suggesting that [99mTc]TcO-MOPADTC is a novel potential tumor-imaging agent.

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PET Radiopharmaceuticals in Oncology Beyond FDG

Song

Huang

2017

Personalized Pathway-Activated Systems Imaging in Oncology

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Synthesis of 99mTc-EC-AMT as an imaging probe for amino acid transporter systems in breast cancer

Abstract: The results indicate that (99m)Tc-EC-AMT, a new amino acid transporter-based radiotracer, is suitable for breast tumor imaging.

Cited by 7 publications

References 21 publications

Development of Tyrosine-Based RadiotracerTc99m-N4-Tyrosine for Breast Cancer Imaging

Development of Tyrosine-Based RadiotracerTc99m-N4-Tyrosine for Breast Cancer Imaging

Radiolabeling and Biological Evaluation of Novel 99mTc-Nitrido and 99mTc-Oxo Complexes with 4-Methoxy-L-Phenylalanine Dithiocarbamate for Tumor Imaging

PET Radiopharmaceuticals in Oncology Beyond FDG

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