Radiobromination of monoclonal antibody using potassium [76Br] (4 isothiocyanatobenzyl-ammonio)-bromo-decahydro-closo-dodecaborate (Bromo-DABI)

Alexander Bruskin, Igor Sivaev, Mikael Persson, Hans Lundqvist, Jörgen Carlsson, Stefan Sjöberg, Vladimir Tolmachev

Research output: Contribution to journalArticlepeer-review

39 Citations (Scopus)

Abstract

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.

Original languageEnglish
Pages (from-to)205-211
Number of pages7
JournalNuclear Medicine and Biology
Volume31
Issue number2
DOIs
Publication statusPublished - Feb 2004
Externally publishedYes

Keywords

  • (4 isothiocyanatobenzyl- ammonio)-bromo-decahydro-closo-dodecaborate
  • Indirect radiobromination
  • Monoclonal antibody

ASJC Scopus subject areas

  • Molecular Medicine
  • Radiology Nuclear Medicine and imaging
  • Cancer Research

Fingerprint Dive into the research topics of 'Radiobromination of monoclonal antibody using potassium [<sup>76</sup>Br] (4 isothiocyanatobenzyl-ammonio)-bromo-decahydro-closo-dodecaborate (Bromo-DABI)'. Together they form a unique fingerprint.

Cite this