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

0185755 - UJF-V 20033071 RIV NL eng J - Journal Article
Sjostrom, A. - Tolmachev, V. - Lebeda, Ondřej - Koziorowski, J. - Carlsson, J. - Lundqvist, H.
Direct astatination of a tumour-binding protein, human epidermal growth factor, using nido-carborane as a prosthetic group.
Journal of Radioanalytical and Nuclear Chemistry. Roč. 256, č. 7 (2003), s. 191-197. ISSN 0236-5731. E-ISSN 1588-2780
R&D Projects: GA AV ČR KSK4055109
Keywords : neutron-capture therapy * astatine-211
Subject RIV: CH - Nuclear ; Quantum Chemistry
Impact factor: 0.472, year: 2003

We have investigated a method for direct astatine labeling of proteins. Binding sites for astatine were created by coupling of a nido-carborane derivative to a protein, the human epidermal growth factor (hEGF), using two different conjugation methods - by glutaraldehyde cross-linking or by introduction of sulfohydryl groups by Traut's reagent with subsequent linking of ANC-1 with m-maleimidobenzoyl-N-hydroxysulfosuccinimide ester. The conjugates were astatinated using the Chloramine-T method in high yield. The best labeling was obtained by the glutaraldehyde conjugate with an average yield of 68+/-9%. In vitro stability tests indicated that the glutaraldehyde conjugated label was as stable as hEGF labeled with astatobenzoate.
Permanent Link: http://hdl.handle.net/11104/0002095