TY - JOUR
T1 - Radiobromination of monoclonal antibody using potassium [76Br] (4 isothiocyanatobenzyl-ammonio)-bromo-decahydro-closo-dodecaborate (Bromo-DABI)
AU - Bruskin, Alexander
AU - Sivaev, Igor
AU - Persson, Mikael
AU - Lundqvist, Hans
AU - Carlsson, Jörgen
AU - Sjöberg, Stefan
AU - Tolmachev, Vladimir
N1 - Funding Information:
This work was financially supported by grants from the Swedish Cancer Society (Cancerfonden), the Swedish Royal Academy of Sciences, and INTAS (grant 99-00806). The authors wish to thank Genentech for their generous gift of Trastuzumab. The authors also wish to thank Mr. Lars Einarsson (The Svedberg Laboratory, Uppsala, Sweden) and the personnel at Uppsala University PET center for technical support.
Copyright:
Copyright 2008 Elsevier B.V., All rights reserved.
PY - 2004/2
Y1 - 2004/2
N2 - The use of charged linkers in attaching radiohalogens to tumor-seeking biomolecules may improve intracellular retention of the radioactive label after internalization and degradation of targeting proteins. Derivatives of polyhedral boron clusters, such as closo-dodecaborate (2-) anion, might be possible charged linkers. In this study, a bifunctional derivative of closo-dodecaborate, (4-isothiocyanatobenzyl-ammonio)-undecahydro-closo- dodecaborate (DABI) was labeled with positron-emitting nuclide 76Br (T = 16.2 h) and coupled to anti-HER2/neu humanized antibody Trastuzumab. The overall labeling yield at optimized conditions was 80.7 ± 0.6%. The label was proven to be stable in vitro in physiological and a set of denaturing conditions. The labeled antibody retained its capacity to bind to HER-2/neu antigen expressing cells. The results of the study demonstrated feasibility for using derivatives of closo-dodecaborate in indirect labeling of antibodies for radioimmunoPET.
AB - The use of charged linkers in attaching radiohalogens to tumor-seeking biomolecules may improve intracellular retention of the radioactive label after internalization and degradation of targeting proteins. Derivatives of polyhedral boron clusters, such as closo-dodecaborate (2-) anion, might be possible charged linkers. In this study, a bifunctional derivative of closo-dodecaborate, (4-isothiocyanatobenzyl-ammonio)-undecahydro-closo- dodecaborate (DABI) was labeled with positron-emitting nuclide 76Br (T = 16.2 h) and coupled to anti-HER2/neu humanized antibody Trastuzumab. The overall labeling yield at optimized conditions was 80.7 ± 0.6%. The label was proven to be stable in vitro in physiological and a set of denaturing conditions. The labeled antibody retained its capacity to bind to HER-2/neu antigen expressing cells. The results of the study demonstrated feasibility for using derivatives of closo-dodecaborate in indirect labeling of antibodies for radioimmunoPET.
KW - (4 isothiocyanatobenzyl- ammonio)-bromo-decahydro-closo-dodecaborate
KW - Indirect radiobromination
KW - Monoclonal antibody
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U2 - 10.1016/j.nucmedbio.2003.08.005
DO - 10.1016/j.nucmedbio.2003.08.005
M3 - Article
C2 - 15013486
AN - SCOPUS:1542285455
VL - 31
SP - 205
EP - 211
JO - Nuclear Medicine and Biology
JF - Nuclear Medicine and Biology
SN - 0969-8051
IS - 2
ER -