ArticleNuclear medicine and biology2010
Preparation and in vivo evaluation of radioiodinated closo-decaborate(2-) derivatives to identify structural components that provide low retention in tissues.
Article in Nuclear medicine and biology, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.
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Who cites it
8 citing papers in PubMed.
- The Different Strategies for the Radiolabeling of [Pharmaceutics · 2024Review
- Primary Amine Nucleophilic Addition to NitriliumInternational journal of molecular sciences · 2021Article
- Investigation on the reactivity of nucleophilic radiohalogens with arylboronic acids in water: access to an efficient single-step method for the radioiodination and astatination of antibodies.Chemical science · 2020Article
- Article
- Article
- Immuno-PET for Clinical Theranostic Approaches.International journal of molecular sciences · 2016Review
- Production of [(211)At]-astatinated radiopharmaceuticals and applications in targeted α-particle therapy.Cancer biotherapy & radiopharmaceuticals · 2013Review
- Reagents for astatination of biomolecules. 5. Evaluation of hydrazone linkers in (211)At- and (125)I-labeled closo-decaborate(2-) conjugates of Fab' as a means of decreasing kidney retention.Bioconjugate chemistry · 2011Article
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4 authors.
Funding
Abstract
introductionIn vivo deastatination of (211)At-labeled biomolecules can severely limit their use in endoradiotherapy. Our studies have shown that the use of closo-decaborate(2-) moiety for (211)At-labeling of biomolecules provides high in vivo stability towards deastatination. However, data from those studies have also been suggestive that some astatinated closo-decaborate(2-) catabolites may be retained in tissues. In this study, we investigated the in vivo distributions of several structurally simple closo-decaborate(2-) derivatives to gain information on the effects of functional groups if catabolites are released into the blood system from the carrier biomolecule.
methodsThirteen closo-decaborate(2-) derivatives were synthesized and radioiodinated for evaluation. Tissue concentrations of the radioiodinated compounds were obtained in groups of five mice at 1 and 4 h postinjection (pi). Dual-label ((125)I and (131)I) experiments permitted evaluation of two compounds in each set of mice.
resultsAll of the target compounds were readily synthesized. Radioiodination reactions were conducted with chloramine-T and Na[(125/131)I]I in water to give high yields (75-96%) of the desired compounds. Biodistribution data at 1 and 4 h pi (representing catabolites released into the blood system) showed small differences in tissue concentrations for some compounds, but large differences for others. The results indicate that formal (overall) charge on the compounds could not be used as a predictor of tissue localization or retention. However, derivatives containing carboxylate groups generally had lower tissue concentrations. Acid cleavable hydrazone functionalities appeared to be the best candidates for further study.
conclusionsFurther studies incorporating hydrazone functionalities into pendant groups for biomolecule radiohalogenation are warranted.
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