Direct astatination of a peptide, human epidermal growth factor, using nido-carborane as a prosthetic group

• 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.

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