Radiochemistry and Radioprobe Development Group

​Development of radiolabeling methods 

Radiopharmaceuticals have been used for the diagnosis of various disorders and for the treatment of cancer. The group focuses on expanding state-of-the-art radiolabeling methods and automated synthesis system we have for the production of radiopharmaceuticals. The improvement of radiolabeling methods and the production of new radiopharmaceuticals has also been achieved by the application of new labeling intermediates developed in the group. We can produce radiolabeled compounds with a molar activity of the highest level in the world. Intra/inter-institutional research projects have been in progress offering radiolabeled compounds for pre-clinical application. 

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hot cell

Research and development of radiopharmaceuticals 

The group also focuses on the development of radiopharmaceuticals which are used for the diagnosis of various disorders and for cancer therapy. The candidates of radiopharmaceuticals labeled with an appropriate radionuclide for imaging or cancer therapy are designed based on the target (receptors, enzymes, transporters, etc.), and the candidates synthesized undergo in vitro and in vivo pre-clinical evaluation. Many radiopharmaceuticals developed in the group have been applied for clinical investigation. Furthermore, we have studied drug-repositioning of radiopharmaceuticals using animal models. The compounds with an ultra-high molar activity have been used for the investigation of in vivo kinetics of pharmaceutical candidates and molecular imaging studies in small animals. Intra/inter-institutional research projects have been in progress. 

PET device for small animals

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Kikuchi Tatsuya Group leader

• Kikuchi Tatsuya Group leader
• Xie Lin Principal Researcher
• Fujinaga Masayuki Principal Researcher
• Yamasaki Tomoteru Principal Researcher
• Okamura Toshimitsu Senior Researcher
• Hanyu Masayuki Senior Researcher
• Okada Maki Researcher
• Mori Wakana Researcher
• Kumata Katsushi Technical Staff
• Zhang Yiding Technical Staff

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Selected Publications

1. Zhang Y.,Xie L.,Fujinaga M.,Kurihara Y.,Ogawa M.,Kumata K.,Mori W.,Kokufuta T.,Nengaki N.,Wakizaka H.,Luo R.,Wang F.,Hu K.,Zhang MR.:L-[5-11C]Glutamine PET imaging noninvasively tracks dynamic responses of glutaminolysis in non-alcoholic steatohepatitis.Acta Pharmaceutica Sinica B,15(2),681–691,(2025)
2. Xie L., Lulu Z., Hu K., Hanyu M., Yiding Z., Fujinaga M., Minegishi K., Takayuki O., Nagatsu K., Cuiping J., Shimokawa T., Okonogi N., Yamada S., Feng W., Rui W., Zhang MR.: A 211At-labelled mGluR1 inhibitor induces cancer senescence to elicit long-lasting anti-tumor efficacy.Cell Reports Medicine 4(4), 100960, (2023)
3. Kikuchi T., Ogawa M., Okamura T., Gee AD., Zhang MR.: Rapid ‘on-column’ preparation of hydrogen [11C]cyanide from [11C]methyl iodide via [11C]formaldehyde. Chemical Science ​,13(12), 3556–3562,(2022)
4. Okamura T., Tsukamoto S., Okada M., Kikuchi T., Aizawa R., Wakizaka H., Nengaki N., Ogawa M., Ishii, H., Zhang MR.: Imaging the activity of the sodium iodide symporter in the brain with 9-pentyl-6-[11C]thiocyanatopurine. Bioconjugate Chemistry ​,33(9), 1654–1662 (2022)
5. Fujinaga M., Ohkubo T., Yamasaki T., Kumata K., Nengaki N., Zhang MR.: Scandium triflate-catalyzed N-[18F]fluoroalkylation of aryl- or heteroaryl-amines with [18F]epifluorohydrin under mild conditions.Organic Letters ​,24(22), 4024–4028 ,(2022)
6. Hu K., Wu W., Geng H., Zhang Y., Hanyu M., Zhang L., Liu Y., Nagatsu K., Suzuki H., Guo J., Wu YD., Li Z., Wang F., Zhang MR.: Whole-body PET tracking of a D-dodecapeptide and its Radiotheranostic Potential for PD-L1 Overexpressing Tumors.Acta Pharmaceutica Sinca B ​,12(3), 1363–1376, (2022).
7. Xie L., Hu K., Duo Y., Shimokawa T., Kumata K., Zhang Y., Jiang C., Zhang L., Nengaki N., Wakizaka H., Cao Y., Zhang MR.: Off-tumor IDO1 target engagements determine the cancer-immune set point and predict the immunotherapeutic efficacy. Journal for ImmunoTherapy of Cancer 9(6), e002616 (2021)
8. Hu K., Xie L., Zhang Y., Hanyu M., Yang Z., Nagatsu K., Suzuki H., Ouyang J., Ji X., Wei J., Xu H., Farokhzad OC., Liang H., Lu W., Tao W., Zhang MR.: Marriage of black phosphorus and Cu2+ as effective photothermal agents for PET-guided combination cancer therapy.Nature communications ​,11(1),2778,(2020)
9. Yamasaki T., Zhang X., Kumata K., Zhang Y., Deng X., Fujinaga M., Chen Z., Mori W., Hu K., Wakizaka H., Hatori A., Xie L., Ogawa M., Nengaki N., Van R., Shao Y., Sheffler DJ., Cosford NDP., Liang SH., Zhang MR.: Identification and development of a new positron emission tomography ligand 4-(2- Fluoro-4-[11C]methoxyphenyl)-5-((1-methyl-1H-pyrazol-3-yl)methoxy)picolinamide for imaging metabotropic glutamate receptor subtype 2 (mGlu2). Journal of Medicinal Chemistry,​ 63(20), 11469–11483, (2020)
10. Xie L., Hanyu M., Fujinaga M., Zhang Y., Hu K., Minegishi K., Jiang C., Kurosawa F., Morokoshi Y., Li HK., Hasegawa S., Nagatsu K., Zhang MR.: 131I-IITM and 211At-AITM: Two novel small-molecule radiopharmaceuticals targeting oncoprotein metabotropic glutamate receptor 1. Journal of Nuclear Medicine,​ 61(2), 242–248, (2020)
11. Mori W., Yamasaki T., Fujinaga M., Ogawa M., Zhang Y., Hatori A., Xie L., Kumata K., Wakizaka H., Kurihara Y., Ohkubo T., Nengaki N., Zhang MR.: Development of 2-(2-(3-(4-([18F]Fluoromethoxy- d2)phenyl)-7-methyl-4-oxo-3,4-dihydroquinazolin-2-yl)ethyl)-4-isopropoxyisoindoline-1,3-dione for positron-emission-tomography imaging of phosphodiesterase 10A in the brain. Journal of Medicinal Chemistry ​,62(2), 688–698 ,(2019)