Chemical and Radiochemical Considerations in Radiolabeling with α-Emitting Radionuclides
Chemical and Radiochemical Considerations in Radiolabeling with α-Emitting Radionuclides
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DOI：
10.2174/1874471011104030214
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发表时间：
2011-01-01
影响因子：
2.3
通讯作者：
Wilbur, D. Scott
中科院分区：
文献类型：
--
作者：
Wilbur, D. Scott
回顾化学和放射化学的因素，必须考虑时，放射性标记的目标剂与α -发射放射性核素提出。本文讨论了在研制α -放射药物时选择放射性核素和选择螯合或键合试剂的重要因素。化学参数，如物理性质和挂件组放射性标签，进行了审查。该综述的主要部分概述了放射性金属螯合物和标记条件的发展，以及这些试剂/条件在α发射放射性金属中的应用。强调了含有胺和羧酸配位基团的无环和大环螯合物，以及用于生物分子偶联的双功能螯合物的例子。介绍了60多种放射性金属结合螯合剂。At-211放射性标记与放射性金属的放射性标记是分离的，并对用于放射性标记的各种试剂进行了综述。虽然不是所有的At-211标记试剂都进行了审查（由于最近的另一项审查），但在用At-211标记的垂坠基团的发展中研究了近50种试剂。本综述还讨论了所使用的放射性核素如何影响α -放射药物的治疗剂量，以及如何尽量减少对放射性药物的辐射损伤。
A review of chemical and radiochemical factors that must be considered when radiolabeling targeting agents with alpha-emitting radionuclides is presented. The review discusses factors that are important in choice of radionuclide and choice of chelation or bonding reagents to use in the development of an alpha-emitting radiopharmaceutical. Chemical parameters, such as physical properties and pendant groups for radiolabeling, are reviewed. A major portion of the review outlines the development of chelates and labeling conditions for radiometals, and application of these reagents/conditions to alpha-emitting radiometals. Acyclic and macrocyclic chelates containing amine and carboxylic acid coordination groups are highlighted, with examples of bifunctional chelates for biomolecule conjugation. Information is presented on over 60 radiometal-binding chelates. At-211 radiolabeling is separated from that of radiometals, and the various reagents used for radiolabeling have been reviewed. Although not all At-211-labeling reagents are reviewed (due to another recent review), nearly 50 reagents studied in the development of pendant groups for labeling with At-211 are described. The review also discusses how therapeutic doses of alpha-emitting radiopharmaceuticals can be affected by the radionuclide used and how radiation damage to the radiopharmaceutical can be minimized.