161TB-DOTA-PSMA-617的制备及新细胞模型表征

IF 0.8 Q3 Engineering
O. A. Shashkova, N. A. Verlov, K. O. Avrov, S. V. Soloveva, L. A. Terekhina, A. A. Pinevich, S. V. Shatik, V. V. Zaicev, E. B. Furkina, M. A. Nadporozskiy, V. S. Burdakov, I. A. Kulakov, T. A. Shtam, A. A. Stanzevskiy, M. P. Samoylovich, A. L. Konevega
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引用次数: 0

摘要

terbie -161是一种放射性同位素,其特征是β-发射、俄歇电子发射、转换电子发射,以及在较小程度上的伽马和x射线。以俄罗斯生产的组分为基础合成了与DOTA-PSMA-617配体的Tb-161放射偶联物(被认为是一种有前景的前列腺癌放射治疗药物)。研究了161Tb-DOTA-PSMA-617的理化性质。利用表达人类PSMA的转基因小鼠癌细胞CT26-PSMA细胞模型,在体外细胞系和小鼠体内研究了放射性偶联物与细胞膜受体的结合能力。研究了该放射缀合物的药代动力学和生物分布。放射性药物在表达人类PSMA的肿瘤中表现出与对照肿瘤不同的高度特异性积累。它在肾脏和其他动物器官中没有明显的积累。测定该放射性药物的血半衰期为38.4 min。因此,根据主要标准,合成的放射性偶联物161Tb-DOTA-PSMA-617是一种很有前景的治疗前列腺癌的放射性药物。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Preparation and Characterization of 161TB-DOTA-PSMA-617 Using a New Cell Model

Preparation and Characterization of 161TB-DOTA-PSMA-617 Using a New Cell Model

Terbium-161 is a radioisotope characterized by β-emission, emission of Auger electrons, conversion electrons, and, to a lesser extent, gamma and X-rays. Tb-161 radioconjugate with the DOTA-PSMA-617 ligand (considered as a promising drug for radiotherapy of prostate cancer) was synthesized on the basis of components produced in Russian Federation. The physicochemical characteristics of 161Tb-DOTA-PSMA-617 were investigated. The ability of the radioconjugate to bind to cell membrane receptor was studied on cell line in vitro and in mice in vivo using a new CT26-PSMA cell model representing genetically modified mouse carcinoma cells expressing human PSMA. The pharmacokinetics and biodistribution of the radioconjugate were investigated. The radiopharmaceutical demonstrated highly specific accumulation in the tumor expressing human PSMA unlike in the control tumor. It was not significantly accumulated in the kidneys and other animals’ organs. The blood half-life time of the radiopharmaceutical was determined as 38.4 min. Thus, according to the main criteria, the synthesized radioconjugate 161Tb-DOTA-PSMA-617 is a promising radiopharmaceutical for the treatment of prostate cancer.

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来源期刊
Nanotechnologies in Russia
Nanotechnologies in Russia NANOSCIENCE & NANOTECHNOLOGY-
CiteScore
1.20
自引率
0.00%
发文量
0
期刊介绍: Nanobiotechnology Reports publishes interdisciplinary research articles on fundamental aspects of the structure and properties of nanoscale objects and nanomaterials, polymeric and bioorganic molecules, and supramolecular and biohybrid complexes, as well as articles that discuss technologies for their preparation and processing, and practical implementation of products, devices, and nature-like systems based on them. The journal publishes original articles and reviews that meet the highest scientific quality standards in the following areas of science and technology studies: self-organizing structures and nanoassemblies; nanostructures, including nanotubes; functional and structural nanomaterials; polymeric, bioorganic, and hybrid nanomaterials; devices and products based on nanomaterials and nanotechnology; nanobiology and genetics, and omics technologies; nanobiomedicine and nanopharmaceutics; nanoelectronics and neuromorphic computing systems; neurocognitive systems and technologies; nanophotonics; natural science methods in a study of cultural heritage items; metrology, standardization, and monitoring in nanotechnology.
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