Targeted delivery of radiolabeled imaging and therapeutic agents: bifunctional radiopharmaceuticals.
Targeted delivery of radiolabeled imaging and therapeutic agents: bifunctional radiopharmaceuticals.
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放射性标记成像和治疗剂的靶向递送：双功能放射性药物。
DOI：
10.1615/critrevtherdrugcarriersyst.v16.i2.20
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发表时间：
1999
影响因子：
2.7
通讯作者：
H. Saji
中科院分区：
文献类型：
--
作者：
H. Saji
放射性诊断和治疗剂的临床应用构成了无创医学、核医学的伟大进步之一。核医学领域中使用的放射性试剂被称为“放射性药物”，并且需要在靶组织中表现出高度且特异性的放射性定位。在用于放射性药物的放射性核素中，99mTc和(111)In等放射性金属因其核物理特性和广泛的可用性而备受关注。然而，由于这些金属元素不是生物活性分子的组成部分，因此它们不能简单地替换具有生物学意义的化合物中的常见组成原子。因此，对生物特异性放射性药物的需求对金属放射性核素标记的生物活性分子的合理设计构成了巨大的挑战，并演变成一代双功能放射性药物。分子含有生物活性位点和用于结合金属放射性核素的螯合基团，其中螯合基团的连接不会影响母体化合物的固有生物特异性。本文介绍了用于靶向诊断和治疗的大分子和小分子双功能放射性药物的研究最新进展。
Clinical application of radioactive diagnostic and therapeutic agents constitutes one of the great advances in noninvasive medicine, nuclear medicine. The radioactive agents used in the nuclear medical field are called "radiopharmaceuticals," and are required to exhibit high and specific localization of radioactivity into target tissue. Among radionuclides used in radiopharmaceuticals, radiometals such as 99mTc and (111)In have received much attention because of their nuclear physical characteristics and widespread availability. However, since these metallic elements are not constituents of bioactive molecules, they cannot simply replace common constituent atoms in biologically interesting compounds. Thus, demand for biospecific radiopharmaceuticals constitutes a great challenge in rational design of biologically active molecules labeled with metallic radionuclides, and evolves into a generation of bifunctional radiopharmaceuticals. Molecules contain both a biologically active site and a chelating group for binding the metallic radionuclide in which attachment of a chelating group does not affect the inherent biospecificity of the mother compound. This paper describes recent progress in research of macro- and small-molecular bifunctional radiopharmaceuticals for targeted diagnosis and therapy.