Specific Cytotoxicity of Targeted 177 Lu and 212 Pb-Based Radiopharmaceuticals.

Autor: Pankratov AA; P. A. Hertsen Moscow Oncology Research Institute - Affiliated Branch of National Medical Research Radiological Centre, Ministry of Health of the Russian Federation, Moscow, Russia., Nemtsova ER; P. A. Hertsen Moscow Oncology Research Institute - Affiliated Branch of National Medical Research Radiological Centre, Ministry of Health of the Russian Federation, Moscow, Russia. nemtz@yandex.ru., Plyutinskaya AD; P. A. Hertsen Moscow Oncology Research Institute - Affiliated Branch of National Medical Research Radiological Centre, Ministry of Health of the Russian Federation, Moscow, Russia., Vorontsova MS; P. A. Hertsen Moscow Oncology Research Institute - Affiliated Branch of National Medical Research Radiological Centre, Ministry of Health of the Russian Federation, Moscow, Russia., Chuvilin DY; National Research Center Kurchatov Institute, Moscow, Russia., Egorova BV; National Research Center Kurchatov Institute, Moscow, Russia., Kokov KV; National Research Center Kurchatov Institute, Moscow, Russia., Deev SM; M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia.; Research School of Chemistry and Applied Biomedical Sciences, National Research Tomsk Polytechnic University, Tomsk, Russia., Lebedenko EN; M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia.; Research School of Chemistry and Applied Biomedical Sciences, National Research Tomsk Polytechnic University, Tomsk, Russia., Proshkina GM; M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia., Shul'ga AA; M. M. Shemyakin and Yu. A. Ovchinnikov Institute of Bioorganic Chemistry, Russian Academy of Sciences, Moscow, Russia.; Research School of Chemistry and Applied Biomedical Sciences, National Research Tomsk Polytechnic University, Tomsk, Russia., Golovachenko VA; Technology of Medical Polymers Company, St. Petersburg, Russia., Shegai PV; P. A. Hertsen Moscow Oncology Research Institute - Affiliated Branch of National Medical Research Radiological Centre, Ministry of Health of the Russian Federation, Moscow, Russia., Kaprin AD; P. A. Hertsen Moscow Oncology Research Institute - Affiliated Branch of National Medical Research Radiological Centre, Ministry of Health of the Russian Federation, Moscow, Russia.
Jazyk: angličtina
Zdroj: Bulletin of experimental biology and medicine [Bull Exp Biol Med] 2021 Sep; Vol. 171 (5), pp. 627-632. Date of Electronic Publication: 2021 Oct 09.
DOI: 10.1007/s10517-021-05283-4
Abstrakt: Two radiopharmaceutical preparations were developed on the basis of artificial targeted polypeptide ZHER2 specific to HER2/neu tumor marker and radionuclides 177 Lu (ZHER2-HSA-chelator- 177 Lu) or 212 Pb (ZHER2-HSA-chelator- 212 Pb). The objective was to evaluate in vitro the cytotoxic activity of the targeted radiopharmaceuticals using two cultured human breast cancer cell lines with different expression of HER2/neu: SK-BR3 (high expression of HER2/neu) and MCF-7 (low expression of HER2/neu). It was shown that the cytotoxic effect of both preparations was significantly higher against the SK-BR-3 cells. The cytotoxicity correlated with the incubation period (it was higher after 72 h than after 24 h) and was significantly more pronounced in comparison with activity of radionuclide salts without a specific ligand. In vivo preclinical study of these pharmaceuticals seems to be very promising in animals with xenografted tumors showing high expression of HER2/neu marker.
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Databáze: MEDLINE
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