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

Alexander S. Ivanov; Megan E. Simms; Vyacheslav S. Bryantsev; Paul D. Benny; Justin R. Griswold; Laetitia H. Delmau; Nikki A. Thiele

doi:10.1039/d2cc03156f

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

Alexander S. Ivanov, Megan E. Simms, Vyacheslav S. Bryantsev, Paul D. Benny, Justin R. Griswold, Laetitia H. Delmau, Nikki A. Thiele

Research output: Contribution to journal › Article › peer-review

14 Scopus citations

Abstract

The coordination chemistry of Ra²⁺ is poorly defined, hampering efforts to design effective chelators for ²²³Ra-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.

Original language	English
Pages (from-to)	9938-9941
Number of pages	4
Journal	Chemical Communications
Volume	58
Issue number	71
DOIs	https://doi.org/10.1039/d2cc03156f
State	Published - Aug 19 2022

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title = "Elucidating the coordination chemistry of the radium ion for targeted alpha therapy",

abstract = "The coordination chemistry of Ra2+ is poorly defined, hampering efforts to design effective chelators for 223Ra-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.",

author = "Ivanov, {Alexander S.} and Simms, {Megan E.} and Bryantsev, {Vyacheslav S.} and Benny, {Paul D.} and Griswold, {Justin R.} and Delmau, {Laetitia H.} and Thiele, {Nikki A.}",

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AU - Ivanov, Alexander S.

AU - Simms, Megan E.

AU - Bryantsev, Vyacheslav S.

AU - Benny, Paul D.

AU - Griswold, Justin R.

AU - Delmau, Laetitia H.

AU - Thiele, Nikki A.

PY - 2022/8/19

Y1 - 2022/8/19

N2 - The coordination chemistry of Ra2+ is poorly defined, hampering efforts to design effective chelators for 223Ra-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.

AB - The coordination chemistry of Ra2+ is poorly defined, hampering efforts to design effective chelators for 223Ra-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.

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JO - Chemical Communications

JF - Chemical Communications

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ER -

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

Abstract

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