Vanermen Maarten, Ligeour Mathilde, Oliveira Maria-Cristina, Gestin Jean-François, Elvas Filipe, Navarro Laurent, Guérard François
Molecular Imaging and Radiology (MIRA), University of Antwerp, Wilrijk, Belgium.
Nantes Université, Inserm, CNRS, Université d'Angers, CRCI2NA, Nantes, France.
EJNMMI Radiopharm Chem. 2024 Oct 4;9(1):69. doi: 10.1186/s41181-024-00298-4.
At-radiopharmaceuticals are currently the subject of growing studies for targeted alpha therapy of cancers, which leads to the widening of the scope of the targeting vectors, from small molecules to peptides and proteins. This has prompted, during the past decade, to a renewed interest in developing novel At-labelling approaches and novel prosthetic groups to address the diverse scenarios and to reach improved efficiency and robustness of procedures as well as an appropriate in vivo stability of the label.
Translated from the well-known (radio)iodine chemistry, the long preferred electrophilic astatodemetallation using trialkylaryltin precursors is now complemented by new approaches using electrophilic or nucleophilic At. Alternatives to the astatoaryl moiety have been proposed to improve labelling stability, and the range of prosthetic groups available to label proteins has expanded.
In this report, we cover the evolution of radiolabelling chemistry, from the initial strategies developed in the late 1970's to the most recent findings.
砹放射性药物目前正成为癌症靶向α治疗日益增多的研究对象，这导致靶向载体的范围不断扩大，从小分子到肽和蛋白质。在过去十年中，这促使人们重新关注开发新型砹标记方法和新型辅基，以应对各种情况，并提高程序的效率和稳健性以及标记在体内的适当稳定性。
从著名的（放射性）碘化学衍生而来，长期以来首选的使用三烷基芳基锡前体的亲电砹脱金属反应，现在有了使用亲电或亲核砹的新方法作为补充。人们已经提出了砹芳基部分的替代物以提高标记稳定性，并且可用于标记蛋白质的辅基范围也有所扩大。
在本报告中，我们涵盖了放射性标记化学的发展历程，从20世纪70年代末开发的初始策略到最新的研究成果。
