Abstract
The inverse electron-demand Diels-Alder reaction between tetrazine (Tz) and trans-cyclooctene (TCO) facilitates the efficient radiosynthesis of 225Ac-labelled radioimmunoconjugates in a two-step method, outperforming conventional approaches based on isothiocyanate couplings.
MeSH terms
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Actinium / chemistry*
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Animals
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Cell Line, Tumor
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Cycloaddition Reaction*
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Electrons*
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Humans
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Immunoconjugates / chemistry*
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Immunoconjugates / pharmacokinetics
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Mice
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Mice, Nude
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Neoplasms, Experimental / diagnostic imaging*
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Radiopharmaceuticals / chemical synthesis*
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Radiopharmaceuticals / chemistry*
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Radiopharmaceuticals / pharmacokinetics
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Tissue Distribution
Substances
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Actinium-225
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Immunoconjugates
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Radiopharmaceuticals
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Actinium