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Development of tyrosine-based radiotracer 99mTc-N4-Tyrosine for breast cancer imaging.

Kong FL, Ali MS, Rollo A, Smith DL, Zhang Y, Yu DF, Yang DJ - J. Biomed. Biotechnol. (2012)

Bottom Line: The purpose of this study was to develop an efficient way to synthesize (99m)Tc-O-[3-(1,4,8,11-tetraazabicyclohexadecane)-propyl]-tyrosine ((99m)Tc-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 (99m)Tc with high radiochemical purity (>95%).

View Article: PubMed Central - PubMed

Affiliation: Department of Experimental Diagnostic Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA. kongfanlin2007@gmail.com

ABSTRACT
The purpose of this study was to develop an efficient way to synthesize (99m)Tc-O-[3-(1,4,8,11-tetraazabicyclohexadecane)-propyl]-tyrosine ((99m)Tc-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 (99m)Tc with high radiochemical purity (>95%). Cellular uptake of (99m)Tc-N4-Tyrosine was much higher than that of (99m)Tc-N4 and the clinical gold standard (18)F-2-deoxy-2-fluoro-glucose ((18)F-FDG) in rat breast tumor cells in vitro. Tissue uptake and dosimetry estimation in normal rats revealed that (99m)Tc-N4-Tyrosine could be safely administered to humans. Evaluation in breast tumor-bearing rats showed that although (99m)Tc-N4-Tyrosine appeared to be inferior to (18)F-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. (99m)Tc-N4-Tyrosine could thus be a useful radiotracer for use in breast tumor diagnostic imaging.

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In vitro cellular uptake of 99mTc-N4-Tyrosine, 99mTc-N4, and 18F-FDG in cells from rat breast tumor cell line 13762. Data are expressed as mean percent of cellular uptake ± standard deviation (%Uptake ± SD) measured at 15, 30, 60, 120, and 240 minutes after coincubation with 99mTc-N4-Tyrosine.
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fig3: In vitro cellular uptake of 99mTc-N4-Tyrosine, 99mTc-N4, and 18F-FDG in cells from rat breast tumor cell line 13762. Data are expressed as mean percent of cellular uptake ± standard deviation (%Uptake ± SD) measured at 15, 30, 60, 120, and 240 minutes after coincubation with 99mTc-N4-Tyrosine.

Mentions: The cellular uptake kinetics of 99mTc-N4-Tyrosine, 99mTc-N4, and 18F-FDG in rat breast tumor cells is shown in Figure 3. The uptake for 99mTc-N4-Tyrosine increased dramatically up to 240 minutes, but this was not true for the 99mTc-N4 chelator, suggesting that 99mTc-N4-Tyrosine can enter tumor cells specifically and accumulate rapidly. In addition, the mean %Uptake of 99mTc-N4-Tyrosine was much higher than that of 18F-FDG, which indicated that 99mTc-N4-Tyrosine had better imaging potential than 18F-FDG in this in vitro breast cancer model.


Development of tyrosine-based radiotracer 99mTc-N4-Tyrosine for breast cancer imaging.

Kong FL, Ali MS, Rollo A, Smith DL, Zhang Y, Yu DF, Yang DJ - J. Biomed. Biotechnol. (2012)

In vitro cellular uptake of 99mTc-N4-Tyrosine, 99mTc-N4, and 18F-FDG in cells from rat breast tumor cell line 13762. Data are expressed as mean percent of cellular uptake ± standard deviation (%Uptake ± SD) measured at 15, 30, 60, 120, and 240 minutes after coincubation with 99mTc-N4-Tyrosine.
© Copyright Policy - open-access
Related In: Results  -  Collection

Show All Figures
getmorefigures.php?uid=PMC3303751&req=5

fig3: In vitro cellular uptake of 99mTc-N4-Tyrosine, 99mTc-N4, and 18F-FDG in cells from rat breast tumor cell line 13762. Data are expressed as mean percent of cellular uptake ± standard deviation (%Uptake ± SD) measured at 15, 30, 60, 120, and 240 minutes after coincubation with 99mTc-N4-Tyrosine.
Mentions: The cellular uptake kinetics of 99mTc-N4-Tyrosine, 99mTc-N4, and 18F-FDG in rat breast tumor cells is shown in Figure 3. The uptake for 99mTc-N4-Tyrosine increased dramatically up to 240 minutes, but this was not true for the 99mTc-N4 chelator, suggesting that 99mTc-N4-Tyrosine can enter tumor cells specifically and accumulate rapidly. In addition, the mean %Uptake of 99mTc-N4-Tyrosine was much higher than that of 18F-FDG, which indicated that 99mTc-N4-Tyrosine had better imaging potential than 18F-FDG in this in vitro breast cancer model.

Bottom Line: The purpose of this study was to develop an efficient way to synthesize (99m)Tc-O-[3-(1,4,8,11-tetraazabicyclohexadecane)-propyl]-tyrosine ((99m)Tc-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 (99m)Tc with high radiochemical purity (>95%).

View Article: PubMed Central - PubMed

Affiliation: Department of Experimental Diagnostic Imaging, The University of Texas MD Anderson Cancer Center, Houston, TX 77030, USA. kongfanlin2007@gmail.com

ABSTRACT
The purpose of this study was to develop an efficient way to synthesize (99m)Tc-O-[3-(1,4,8,11-tetraazabicyclohexadecane)-propyl]-tyrosine ((99m)Tc-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 (99m)Tc with high radiochemical purity (>95%). Cellular uptake of (99m)Tc-N4-Tyrosine was much higher than that of (99m)Tc-N4 and the clinical gold standard (18)F-2-deoxy-2-fluoro-glucose ((18)F-FDG) in rat breast tumor cells in vitro. Tissue uptake and dosimetry estimation in normal rats revealed that (99m)Tc-N4-Tyrosine could be safely administered to humans. Evaluation in breast tumor-bearing rats showed that although (99m)Tc-N4-Tyrosine appeared to be inferior to (18)F-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. (99m)Tc-N4-Tyrosine could thus be a useful radiotracer for use in breast tumor diagnostic imaging.

Show MeSH
Related in: MedlinePlus