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

Aleksandr S IvanovMegan E SimmsVyacheslav S BryantsevPaul D BennyJustin R GriswoldLaetitia H DelmauNikki A Thiele
Published in: Chemical communications (Cambridge, England) (2022)
The coordination chemistry of Ra 2+ is poorly defined, hampering efforts to design effective chelators for 223 Ra-based targeted alpha therapy. Here, we report the complexation thermodynamics of Ra 2+ with the biomedically-relevant chelators DOTA and macropa. Our work reveals the highest affinity chelator to date for Ra 2+ and advances our understanding of key factors underlying complex stability and selectivity for this underexplored ion.
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