Chemical aspects of metal ion chelation in the synthesis and application antibody-based radiotracers.
Chemical aspects of metal ion chelation in the synthesis and application antibody-based radiotracers.
复制标题
DOI：
10.1002/jlcr.3590
复制
发表时间：
2018-07
影响因子：
1.8
通讯作者：
Holland JP
中科院分区：
文献类型：
--
作者：
Boros E;Holland JP
放射性金属越来越容易获得，并经常用于设计用于成像和治疗的放射性示踪剂。从γ射线和β+粒子（成像）的发射到俄歇电子、β -和α-粒子（治疗）的核性质，加上较长的半衰期，与单克隆抗体在体内相对较长的生物半衰期完美匹配。抗体的放射性金属标记需要将金属螯合物结合到单克隆抗体上。这种螯合物必须在处理抗体所需的温和条件下协调金属，并在金属离子协调后提供高动力学、热力学和代谢稳定性，以防止在到达目标位点之前放射性核素在体内释放。在此，我们回顾了不同的放射性金属的作用，这些放射性金属已经发现了用于成像和放射免疫治疗的放射性标记抗体的设计。描述了每种放射性核素的核合成、配位偏好和与常用和新型螯合物的放射性标记特性，以及它们的临床前和临床应用实例。概述了基于抗体的放射性药物的最新趋势，以促进放射金属在成像和治疗中的化学和应用的持续发展。我们回顾了不同的放射性金属的作用，已经发现在成像和放射免疫治疗抗体的放射性标记的应用。概述了它们的核合成、配位偏好、与常用和新型螯合物的放射性标记特性，以及它们的临床前和临床应用的例子。
Radiometals are becoming increasingly accessible and are utilized frequently in the design of radiotracers for imaging and therapy. Nuclear properties ranging from the emission of γ-ray and β+-particles (imaging) to Auger electron, β− and α-particles (therapy) in combination with long half-lives are ideally matched with the relatively long biological half-life of monoclonal antibodies in vivo. Radiometal labelling of antibodies requires the incorporation of a metal chelate onto the monoclonal antibody. This chelate must coordinate the metal under mild conditions required for the handling of antibodies, as well as provide high kinetic, thermodynamic and metabolic stability once the metal ion is coordinated in order to prevent in vivo release of the radionuclide before the target site is reached. Herein, we review the role of different radiometals that have found applications the design of radiolabelled antibodies for imaging and radioimmunotherapy. Each radionuclide is described with regard to its nuclear synthesis, coordinative preference, and radiolabelling properties with commonly used and novel chelates, as well as examples of their preclinical and clinical applications. An overview of recent trends in antibody-based radiopharmaceuticals is provided to spur continued development of the chemistry and application of radiometals for imaging and therapy. We review the role of different radiometals that have found applications for the radiolabelling of antibodies for imaging and radioimmunotherapy. An overview of their nuclear synthesis, coordinative preference, and radiolabelling properties with commonly used and novel chelates, as well as examples of their preclinical and clinical applications is provided.
登录
查看更多内容
影响因子：
4.7
作者：
Agarwal, Paresh;Bertozzi, Carolyn R.
通讯作者：
Bertozzi, Carolyn R.
影响因子：
3.1
作者：
Abou DS;Ku T;Smith-Jones PM
通讯作者：
Smith-Jones PM
影响因子：
45.3
作者：
DeNardo, GL;DeNardo, SJ;Lewis, JP
通讯作者：
Lewis, JP
影响因子：
4.7
作者：
Deri MA;Ponnala S;Kozlowski P;Burton-Pye BP;Cicek HT;Hu C;Lewis JS;Francesconi LC
通讯作者：
Francesconi LC
影响因子：
2.8
作者：
Aime, S;Barge, A;Bombieri, G
通讯作者：
Bombieri, G