title: Radio-iodination of monoclonal antibody using potassium [125I]-(4-isothiocyanatobenzylammonio)-iodo-decahydro-closo-dodecaborate (iodo-DABI).
abstract: BACKGROUND
  Negatively-charged polyhedral boron clusters can be easily halogenated with highly stable boron-halogen bonds and are promising in radionuclide diagnostics and cancer therapy.
  
  
  METHODS
  The radio-iodination conditions for the closo-dodecaborate anion and for the conjugation of its labeled isothiocyanatobenzylammonio derivative to the monoclonal antibody (mAb) were optimized.
  
  
  RESULTS
  The labeling yield was about 90% and the overall conjugation yield was 55-60%. The in vitro stability of the radio-iodinated mAb was good under physiological and non-physiological conditions. The immunoreactivity of the labeled mAb (SK-BR-3 cells) was retained in the one-pot two-step labeling.
  
  
  CONCLUSIONS
  Negatively-charged polyhedral boron clusters can be used for indirect radio-iodination of mAbs.
authors.affiliation: Unit of Biomedical Radiation Sciences, Rudbeck Laboratory, Uppsala University, S-751 85 Uppsala, Sweden.
authors.forename: Anna
authors.initials: A
authors.lastname: Orlova
authors.forename: Alexander
authors.initials: A
authors.lastname: Bruskin
authors.forename: Igor
authors.initials: I
authors.lastname: Sivaev
authors.forename: Stefan
authors.initials: S
authors.lastname: Sjöberg
authors.forename: Hans
authors.initials: H
authors.lastname: Lundqvist
authors.forename: Vladimir
authors.initials: V
authors.lastname: Tolmachev
mesh_terms: D000911:Antibodies, Monoclonal / Q000737:chemistry* / Q000493:pharmacokinetics; D004355:Drug Stability; D006801:Humans; D018796:Immunoconjugates / Q000737:chemistry* / Q000493:pharmacokinetics; D007457:Iodine Radioisotopes / Q000737:chemistry* / Q000493:pharmacokinetics; D007553:Isotope Labeling / Q000379:methods; D009942:Organometallic Compounds / Q000138:chemical synthesis* / Q000493:pharmacokinetics; D019275:Radiopharmaceuticals / Q000138:chemical synthesis* / Q000493:pharmacokinetics
chemical_list: D000911:Antibodies, Monoclonal; D018796:Immunoconjugates; D007457:Iodine Radioisotopes; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; C510145:potassium (125I)-(4-isothiocyanatobenzylammonio)iodo-decahydro-closo-dodecaborate