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Preparation, radioiodination, and in vitro evaluation of a nido-carborane-dextran conjugate, a potential residualizing label for tumor targeting proteins and peptides
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology. (BMS)
Uppsala University, Disciplinary Domain of Science and Technology, Chemistry, Department of Chemistry.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology. (BMS)
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2004 (English)In: Journal of Radioanalytical and Nuclear Chemistry, ISSN 0236-5731, E-ISSN 1588-2780, Vol. 261, no 1, 107-112 p.Article in journal (Refereed) Published
Abstract [en]

Polysaccharides are not degradable by proteolytic enzymes in lysosomes and do not diffuse through cellular membranes. Thus, attached to an internalizing, targeting protein, such polysaccharide linkers, will remain intracellularly after protein degradation. They can be labeled with halogens and provide then a so called residualizing label. Such an approach improves tumor-to-non-tumor radioactivity ratio and, consequently, the results of radionuclide diagnostics and therapy. In this study we present a new approach to obtain a stable halogenation of the polysaccharide dextran using 7-(3-amino-propyl)-7,8-dicarba-nido-undecaborate (-) (ANC). Dextran T10 was partially oxidized by metaperiodate, and ANC was coupled to dextran by reductive amination. The conjugate was then labeled with 125I using either Chloramine-T or IodoGen as oxidants. Labeling efficiency was 69-85%. Stability of the label was evaluated in rat liver homogenates. Under these conditions, the ANC-dextran conjugate was found to be more stable than labeled albumin, which was used as a control protein.

Place, publisher, year, edition, pages
2004. Vol. 261, no 1, 107-112 p.
National Category
Organic Chemistry
Identifiers
URN: urn:nbn:se:uu:diva-69963DOI: 10.1023/B:JRNC.0000030942.76919.6bOAI: oai:DiVA.org:uu-69963DiVA: diva2:97874
Available from: 2006-05-17 Created: 2006-05-17 Last updated: 2017-11-21Bibliographically approved

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Tolmachev, VladimirSjöberg, StefanCarlsson, JörgenLundqvist, Hans

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Department of Oncology, Radiology and Clinical ImmunologyDepartment of Chemistry
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