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潜在的靶向 Auger 治疗候选物:生产和放射化学方面的考虑。

Potent candidates for Targeted Auger Therapy: Production and radiochemical considerations.

机构信息

Dzhelepov Laboratory of Nuclear Problems, Joint Institute for Nuclear Research, Dubna, Moscow Region, Russian Federation.

Dzhelepov Laboratory of Nuclear Problems, Joint Institute for Nuclear Research, Dubna, Moscow Region, Russian Federation; Department of High-Energy Chemistry and Radioecology, D. Mendeleev University of Chemical Technology of Russia, Moscow, Russian Federation.

出版信息

Nucl Med Biol. 2021 Mar-Apr;94-95:1-19. doi: 10.1016/j.nucmedbio.2020.12.001. Epub 2020 Dec 13.

Abstract

Targeted Auger Therapy represents great potential for the therapy of diseases which require a high degree of selectivity on the cellular level (e.g. for therapy of metastatic cancers). Due to their high Linear Energy Transfer (LET), Auger emitters, combined with selective biological systems which enable delivery of radionuclides close to the DNA of the targeting cell, can be extremely selective and powerful treatment tools. There are two main aspects associated with the development of efficient radiopharmaceuticals based on Auger Emitters: a) the availability of suitable Auger-emitting radionuclides for therapy and b) the design of targeting vectors which can deliver Auger emitters into/close to the nucleus. In the present review, we address the first aspect by defining important parameters for the selection of radionuclides for application to Targeted Auger Therapy and form a categorized list of the most promising radionuclides, their possible production routes, and their use in the synthesis of radiopharmaceuticals.

摘要

靶向 Auger 治疗在需要高度细胞水平选择性的疾病治疗方面具有巨大潜力(例如,转移性癌症的治疗)。由于其高线性能量传递(LET),与能够将放射性核素递送至靶向细胞 DNA 附近的选择性生物系统相结合的 Auger 发射器可以成为极其选择性和强大的治疗工具。基于 Auger 发射器开发高效放射性药物有两个主要方面:a)治疗用合适的 Auger 发射放射性核素的可用性,b)设计能够将 Auger 发射器递送至/靠近细胞核的靶向载体。在本综述中,我们通过定义用于靶向 Auger 治疗的放射性核素选择的重要参数来解决第一个方面,并对最有前途的放射性核素进行分类,列出它们可能的生产途径及其在放射性药物合成中的应用。

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