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2004 (English)In: Nuclear Medicine and Biology, ISSN 0969-8051, E-ISSN 1872-9614, Vol. 31, no 2, p. 205-11Article in journal (Refereed) Published
Abstract [en]
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 (76)Br (T 1/2 = 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.
Keywords
Adenocarcinoma/*metabolism/*radionuclide imaging, Antibodies; Monoclonal/chemistry/*diagnostic use/*pharmacokinetics, Boron Compounds/chemical synthesis/*diagnostic use/*pharmacokinetics, Cell Line; Tumor, Drug Stability, Humans, Isotope Labeling/*methods, Metabolic Clearance Rate, Radiopharmaceuticals/chemical synthesis/diagnostic use/pharmacokinetics, Research Support; Non-U.S. Gov't
National Category
Organic Chemistry
Identifiers
urn:nbn:se:uu:diva-72891 (URN)15013486 (PubMedID)
2005-06-212005-06-212017-12-14Bibliographically approved