TY - JOUR
T1 - Direct astatination of a tumour-binding protein, human epidermal growth factor, using nido-carborane as a prosthetic group
AU - Sjöström, A.
AU - Tolmachev, V.
AU - Lebeda, O.
AU - Koziorowski, J.
AU - Carlsson, J.
AU - Lundqvist, H.
N1 - Funding Information:
The authors want to thank the staff of The Svedberg Laboratory (Uppsala, Sweden) and particularly Lars EINARSSON for irradiation of targets and production of 211At, Professor Stefan SJÖBERG at the Department of Organic Chemistry at Uppsala University for providing us with ANC-1 and finally the Swedish Cancer Society and the Swedish Medical Research Council for financial support.
Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.
PY - 2003/5/1
Y1 - 2003/5/1
N2 - 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.
AB - 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.
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U2 - 10.1023/A:1023912728929
DO - 10.1023/A:1023912728929
M3 - Article
AN - SCOPUS:0038439415
VL - 256
SP - 191
EP - 197
JO - Journal of Radioanalytical and Nuclear Chemistry
JF - Journal of Radioanalytical and Nuclear Chemistry
SN - 0236-5731
IS - 2
ER -