Chemical Sciences Division, Oak Ridge National Laboratory, Oak Ridge, Tennessee 37831, USA.
Radioisotope Science and Technology Division, Oak Ridge National Laboratory, Oak Ridge, Tennessee 37831, USA.
Chem Commun (Camb). 2022 Sep 1;58(71):9938-9941. doi: 10.1039/d2cc03156f.
The coordination chemistry of Ra is poorly defined, hampering efforts to design effective chelators for Ra-based targeted alpha therapy. Here, we report the complexation thermodynamics of Ra with the biomedically-relevant chelators DOTA and macropa. Our work reveals the highest affinity chelator to date for Ra and advances our understanding of key factors underlying complex stability and selectivity for this underexplored ion.
镭的配位化学研究还不够完善,这给设计基于镭的靶向 α 治疗的有效螯合剂带来了困难。在这里,我们报告了镭与生物医学相关配体 DOTA 和大环多胺的配合热力学。我们的工作揭示了迄今为止对镭具有最高亲和力的配体,并深入了解了这种研究较少的离子的配合稳定性和选择性的关键因素。