<i>In vivo</i> stability of <sup>211</sup>At-radiopharmaceuticals: on the impact of halogen bond formation

Yssartier, Thibault; Liu, Lu; Pardoue, Sylvain; Le Questel, Jean-Yves; Guérard, François; Montavon, Gilles; Galland, Nicolas

doi:10.1039/d3md00579h

RSC Med. Chem.

2024

DOI: 10.1039/d3md00579h

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In vivo stability of ²¹¹At-radiopharmaceuticals: on the impact of halogen bond formation

Thibault Yssartier,

Lu Liu,

Sylvain Pardoue

et al.

Abstract: Astatine's ability to form halogen bond interactions with iodothyronine deiodinases regulates the in vivo stability of astatoaryl prosthetic groups.

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2024

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Cited by 3 publications

References 66 publications

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Comparison of Different Organometallics Towards Electrophilic Aromatic ²¹¹At‐Astatinations of Highly Reactive Tetrazines

Poulie,

Müller,

Bom Pedersen

et al. 2024

Chemistry A European J

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Organometallics can be used as precursors for electrophilic 211At‐statinations. In this report, we compared the potential of aryl trimethylsilanes, ‐germanes, or –stannanes to be used as precursors to 211At‐label highly reactive tetrazines. Tetrazines can be used for pretargeted radioligand therapies or be applied as synthons to radiolabel rapidly and orthogonally a broad set of precursors such as peptides, mAbs or nanomedicines. All precursors could successfully be synthesized and radiolabeled. The reactivity of organogermanium reagents ranged between those of respective organotin and organosilicon precursors. Moreover, organogermanium reagents proved promising for accessing more complex and polar tetrazine scaffolds. In contrast to organotin derivatives, the use of protecting groups could be avoided for organogermanium and ‐silicon precursors. The developed 211At‐labeled tetrazines could be labeled in radiochemical conversions of 60‐90%. Organogermanium and ‐silicon precursors were clearly advantaged as additional deprotection steps could avoided. Reported labeling procedures allow astatinations of highly reactive tetrazines to be used for pretargeted approaches or to applied as highly reactive synthons to label the next‐generation of 211At‐labeled radiopharmaceuticals.

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Comparison of Different Organometallics Towards Electrophilic Aromatic ²¹¹At‐Astatinations of Highly Reactive Tetrazines

Poulie,

Müller,

Bom Pedersen

et al. 2024

Chemistry A European J

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Synthesis Principle and Practice with Radioactive Iodines and Astatine: Advances Made So Far

Dong,

Zhang,

et al. 2024

J. Org. Chem.

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Radioactive iodines and astatine, possessing distinct exploitable nuclear properties, play indispensable roles in the realms of nuclear imaging and therapy. Their analogous chemical characteristics shape the design, preparation, and substrate range for tracers labeled with these radiohalogens through interconnected radiosynthetic chemistry. This perspective systematically explores the labeling methods by types of halogenating reagents� nucleophilic and electrophilic�underpinning the rational design of such compounds. It delves into the rapidly evolving synthetic strategies and reactions in radioiodination and radioastatination over the past decade, comparing their intrinsic relationships and highlighting variations. This comparative analysis illuminates potential radiosynthetic methods for exploration. Moreover, stability concerns related to compounds labeled with radioactive iodines and astatine are addressed, offering valuable insights for radiochemists and physicians alike.

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Astatine-211 radiolabelling chemistry: from basics to advanced biological applications

Vanermen,

Ligeour,

Oliveira

et al. 2024

EJNMMI radiopharm. chem.

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In vivo stability of ²¹¹At-radiopharmaceuticals: on the impact of halogen bond formation

Abstract: Astatine's ability to form halogen bond interactions with iodothyronine deiodinases regulates the in vivo stability of astatoaryl prosthetic groups.

Cited by 3 publications

References 66 publications

Comparison of Different Organometallics Towards Electrophilic Aromatic ²¹¹At‐Astatinations of Highly Reactive Tetrazines

Comparison of Different Organometallics Towards Electrophilic Aromatic ²¹¹At‐Astatinations of Highly Reactive Tetrazines

Synthesis Principle and Practice with Radioactive Iodines and Astatine: Advances Made So Far

Astatine-211 radiolabelling chemistry: from basics to advanced biological applications

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In vivo stability of 211At-radiopharmaceuticals: on the impact of halogen bond formation

Abstract: Astatine's ability to form halogen bond interactions with iodothyronine deiodinases regulates the in vivo stability of astatoaryl prosthetic groups.

Cited by 3 publications

References 66 publications

Comparison of Different Organometallics Towards Electrophilic Aromatic 211At‐Astatinations of Highly Reactive Tetrazines

Comparison of Different Organometallics Towards Electrophilic Aromatic 211At‐Astatinations of Highly Reactive Tetrazines

Synthesis Principle and Practice with Radioactive Iodines and Astatine: Advances Made So Far

Astatine-211 radiolabelling chemistry: from basics to advanced biological applications

Contact Info

Product

Resources

About

In vivo stability of ²¹¹At-radiopharmaceuticals: on the impact of halogen bond formation

Comparison of Different Organometallics Towards Electrophilic Aromatic ²¹¹At‐Astatinations of Highly Reactive Tetrazines

Comparison of Different Organometallics Towards Electrophilic Aromatic ²¹¹At‐Astatinations of Highly Reactive Tetrazines