[161Tb]Tb-Thz-Phe-D-Trp-Lys-Thr-DOTA: A potential radiopharmaceutical for the treatment of neuroendocrine tumors |
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| Institution: | 1. Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;2. National Research Center ‘Kurchatov Institute’, 123182 Moscow, Russian Federation;3. Institute of Chemical Reagents and High Purity Chemical Substances, National Research Center ‘Kurchatov Institute’, 107076 Moscow, Russian Federation;4. N. N. Blokhin National Medical Research Center of Oncology of the Ministry of Health of the Russian Federation, 115478 Moscow, Russian Federation;1. M. V. Lomonosov Institute of Fine Chemical Technologies, MIREA - Russian Technological University, 119454 Moscow, Russian Federation;2. Peptide Chemistry Research Center, K. N. Toosi University of Technology, P.O. Box 15875-4416, Tehran, Iran;3. Medical Biology Research Center, Kermanshah University of Medical Sciences, P. O. Box 67155-1616, Kermanshah, Iran;4. St. Petersburg State University, 199034 St. Petersburg, Russian Federation;5. Immanuel Kant Baltic Federal University, 236016 Kaliningrad, Russian Federation;1. A. N. Frumkin Institute of Physical Chemistry and Electrochemistry, Russian Academy of Sciences, 119071 Moscow, Russian Federation;2. Interdepartmental Center for Analytical Research in Physics, Chemistry and Biology of the Presidium of the Russian Academy of Sciences, 117997 Moscow, Russian Federation;3. Institute of Petrochemistry and Catalysis, Ufa Federal Research Center of the Russian Academy of Sciences, 450075 Ufa, Russian Federation;4. Photochemistry Center, FRC ‘Crystallography and Photonics’, Russian Academy of Sciences, 119333 Moscow, Russian Federation;1. Lomonosov Moscow State University, Department of Chemistry, Leninskie Gory 1/3, 119991, Moscow, Russia;2. Lomonosov Moscow State University, Department of Soil Science, Leninskie Gory 1/12, 119991, Moscow, Russia;1. Herzen State Pedagogical University of Russia, 191186 St. Petersburg, Russian Federation;2. Department of Chemistry, M. V. Lomonosov Moscow State University, 119991 Moscow, Russian Federation;3. G. V. Plekhanov Russian University of Economics, 117997 Moscow, Russian Federation;4. A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, 664033 Irkutsk, Russian Federation |
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| Abstract: | Thz-Phe-D-Trp-Lys-Thr-DOTA, a conjugate of the DOTA chelator and the Thz-Phe-D-Trp-Lys-Thr pentapeptide, was labeled with 152Eu and 161Tb radionuclides, where 161Tb has decay characteristics suitable for its use in cancer therapy. For the 152Eu]Eu-Thz-Phe-D-Trp-Lys-Thr-DOTA complex, the biodistribution in nude mice bearing IMR-32 tumors was evaluated for the first time. It was shown that the complexes of the conjugate demonstrate accumulation in the tumor at the level of DOTA-TATE, another peptide conjugate widely used in nuclear medicine for the diagnosis and therapy of neuroendocrine tumors, which allows Thz-Phe-D-Trp-Lys-Thr-DOTA to be considered as a potential biological vector for radiopharmaceuticals. |
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| Keywords: | peptide receptor radionuclide therapy somatostatin analogs neuroendocrine tumors short peptides |
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