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Oncotarget Targeted alpha therapy using astatine (211At)-labeled phenylalanine


FOR IMMEDIATE RELEASE
2020-04-14

Oncotarget Volume 11 Issue 15 reported that C6 glioma, U-87MG, and GL261 cell lines were subjected to a cellular 211At-PA uptake analysis that included an evaluation of the uptake inhibition by the system L amino acid transporter inhibitor 2-aminobicyclo- -heptane-2-carboxylic acid.

BCH significantly inhibited para-211At-PA uptake in C6 glioma, U-87MG, and GL261 cells compared to baseline, suggesting an uptake contribution by system L amino acid transporters.

Dr. Tadashi Watabe from The Department of Nuclear Medicine and Tracer Kinetics, Graduate School of Medicine, Osaka University, Suita, Japan as well as The Institute for Radiation Sciences, Osaka University, Suita, Japan said, "Targeted alpha therapy has received attention as an effective form of radionuclide treatment, particularly for refractory and/or recurrent malignant tumors such as malignant glioma."

"Targeted alpha therapy has received attention as an effective form of radionuclide treatment, particularly for refractory and/or recurrent malignant tumors such as malignant glioma."

- Dr. Tadashi Watabe, The Department of Nuclear Medicine and Tracer Kinetics, Graduate School of Medicine and The Institute for Radiation Sciences

Targeted alpha therapy has received attention as an effective form of radionuclide treatment, particularly for refractory and/or recurrent malignant tumors such as malignant glioma.

Many malignant tumors, including glioma, exhibit upregulated amino acid transport and glucose transport.

Additionally, phenylalanine derivatives such as 18F-fluoro-borono-PA and 4-borono-L-PA specifically target tumors and are used mainly in the context of boron neutron capture therapy.

Figure 1: (A) Reaction scheme for the labeling of para-borono-L-phenylalanine (BPA) with 211At (represented by para-211At-PA). (B) Radiochromatogram obtained by eluting a solid-phase extraction-purified para-211At-PA solution on a reverse-phase high-performance liquid chromatography column under a gradient.

In addition, 211At can be combined with small-molecule compounds to enable rapid distribution to the target.

In this study, The Authors evaluated the selectivity of 211At-para-astato-L-PA for amino acid transporters focusing on LAT1, as well as the treatment effect of this derivative in mouse glioma xenograft and allograft models.

The Umetani/Wu Research Team concluded in their Oncotarget Research Paper, "we have demonstrated the cellular uptake of 211At-PA and the tumor growth suppression effects of this PA derivative in mouse xenograft and allograft models of malignant glioma. Our findings suggest that 211At-PA could be useful as an alpha therapy specific for system L amino acid transporters expressed on malignant tumors."

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DOI - https://doi.org/10.18632/oncotarget.27552

Full text - https://www.oncotarget.com/article/27552/text/

Correspondence to - Tadashi Watabe - watabe@tracer.med.osaka-u.ac.jp

Keywords - alpha therapy, astatine, glioma, LAT1, phenylalanine

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