Elucidating the coordination chemistry of the radium ion for targeted alpha therapy

The coordination chemistry of Ra2+ is poorly defined, hampering efforts to design effective chelators for Ra-223-based targeted alpha therapy. Here, we report the complexation thermodynamics of Ra2+ with the biomedically-relevant chelators DOTA and macropa. Our work reveals the highest affinity chelator to date for Ra2+ and advances our understanding of key factors underlying complex stability and selectivity for this underexplored ion.

Automated summary

In this study, we report the complexation thermodynamics of Ra2+ with two biomedically-relevant chelators, DOTA and macropa. Our findings reveal the highest affinity chelator for Ra2+ to date and advance our understanding of key factors determining complex stability and selectivity for this underexplored ion.