| Literature DB >> 34626281 |
A A Pankratov1, E R Nemtsova2, A D Plyutinskaya1, M S Vorontsova1, D Yu Chuvilin3, B V Egorova3, K V Kokov3, S M Deev4,5, E N Lebedenko4,5, G M Proshkina4, A A Shul'ga4,5, V A Golovachenko6, P V Shegai1, A D Kaprin1.
Abstract
Two radiopharmaceutical preparations were developed on the basis of artificial targeted polypeptide ZHER2 specific to HER2/neu tumor marker and radionuclides 177Lu (ZHER2-HSA-chelator-177Lu) or 212Pb (ZHER2-HSA-chelator-212Pb). 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.Entities:
Keywords: 177Lu and 212Pb radionuclides; targeted radiopharmaceutical
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Year: 2021 PMID： 34626281 DOI： 10.1007/s10517-021-05283-4
Source DB: PubMed Journal: Bull Exp Biol Med ISSN： 0007-4888 Impact factor: 0.804