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Direct astatination of a peptide, human epidermal growth factor, using nido-carborane as a prosthetic group
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology.
Uppsala University, Disciplinary Domain of Medicine and Pharmacy, Faculty of Medicine, Department of Oncology, Radiology and Clinical Immunology.
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2000 (English)In: Nuclear medicine communications, ISSN 0143-3636, E-ISSN 1473-5628, Vol. 21, no 6, p. 594-Article, book review (Other academic) Published
Abstract [en]

Purpose

The aim of the study was to evaluate direct astatine labelling of proteins with the use of nido-carborane as prosthetic group for attachments of astatine. Methods: Human epidermal growth factor, hEGF, was conjugated to 7-(3-amino-propyl)-7,8-dicarbanido-undecaborate (-), ANC, using two different conjugation methods, glutaraldehyde crosslinking and coupling via Traut's reagent. The hEGF-ANC conjugates were astatine labelled using the Chloramine-T method. The stability of the labelled compounds was tested by incubation at 37°C. Results: The conjugates were astatinated using the Chloramine-T method in high yield. The best labelling yields were obtained by the glutaraldehyde conjugate with an average yield of 70.5±2.2%. In vitro stability tests indicated that the introduced label was as stable as hEGF labelled with astatobenzoate. Conclusion: Conjugation of nido-carboranes to peptides creates binding sites for direct astatine labelling that can be performed in mild conditions (p 7.2) with high labelling yields.

Place, publisher, year, edition, pages
2000. Vol. 21, no 6, p. 594-
National Category
Medical and Health Sciences
Identifiers
URN: urn:nbn:se:uu:diva-59969Archive number: 00006231-200006000-00126OAI: oai:DiVA.org:uu-59969DiVA, id: diva2:87879
Available from: 2008-10-17 Created: 2008-10-17 Last updated: 2017-12-01Bibliographically approved

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