@article{oai:repo.qst.go.jp:00078127,
 author = {Xie, Lin and Hanyu, Masayuki and Fujinaga, Masayuki and Zhang, Yiding and Kuan, Hu and Minegishi, Katsuyuki and Jiang, Cuiping and Kurosawa, Fuki and Morokoshi, Yukie and Li, Huizi and Hasegawa, Sumitaka and Nagatsu, Kotaro and Ming-Rong, Zhang and Lin, Xie and Masayuki, Hanyu and Masayuki, Fujinaga and Zhang, Yiding and Kuan, Hu and Katsuyuki, Minegishi and Fuki, Kurosawa and Yukie, Morokoshi and Li, Huizi and Sumitaka, Hasegawa and Kotaro, Nagatsu and Zhang, Ming-Rong},
 issue = {2},
 journal = {The Journal of Nuclear Medicine},
 month = {Aug},
 note = {Targeted radionuclide therapy (TRT) targeting oncoproteins facilitates the delivery of therapeutic radionuclides to tumor tissues with high precision. Herein, we developed two new radiopharmaceuticals, 4-131I-iodo- and 4-211At-astato-N-[4-(6-(isopropylamino)pyridine-4-yl)-1,3-thiazol-2-yl]-N-methylbenzamide (131I-IITM and 211At-AITM), targeting the ectopic metabotropic glutamate receptor 1 (mGluR1) in melanomas for TRT studies. Methods: 131I-IITM and 211At-AITM were synthesized by reacting a stannyl precursor with 131I-NaI and 211At in the presence of an oxidizing agent. The therapeutic efficacy and safety of the two radiopharmaceuticals were investigated using mGluR1-expressing B16F10 melanoma cells and melanoma-bearing mice. Results: 131I-IITM and 211At-AITM were obtained with radiochemical purity of >99% and radiochemical yields of 42.7% ± 10.4% and 28.9% ± 9.9%, respectively, based on the total radioactivity of used radionuclides. 131I-IITM and 211At-AITM exhibited maximum uptakes of 4.66% ± 0.70% ID/g and 7.68% ± 0.71% ID/g in the targeted melanomas, respectively, and were rapidly cleared from non-target organs after intravenous injection. Both agents markedly inhibited melanoma growth compared with the controls (61.00% and 95.68%, respectively). In the melanoma model, considerably greater therapeutic efficacy with negligible toxicity was observed using 211At-AITM. Conclusion: The non-toxic radiopharmaceuticals 131I-IITM and 211At-AITM are useful high-precision TRT agents that can be used to target the oncoprotein mGluR1 for melanoma therapy.},
 pages = {242--248},
 title = {131I-IITM and 211At-AITM: Two Novel Small-molecule Radiopharmaceuticals Targeting Oncoprotein Metabotropic Glutamate Receptor 1},
 volume = {61},
 year = {2019}
}