Radio-iodination of monoclonal antibody using potassium [125I]-(4-isothiocyanatobenzylammonio)-iodo-decahydro-closo-dodecaborate (iodo-DABI).
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.
Orlova
Anna
A
Unit of Biomedical Radiation Sciences, Rudbeck Laboratory, Uppsala University, S-751 85 Uppsala, Sweden.
Bruskin
Alexander
A
Sivaev
Igor
I
Sjöberg
Stefan
S
Lundqvist
Hans
H
Tolmachev
Vladimir
V
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
D000911:Antibodies, Monoclonal; D018796:Immunoconjugates; D007457:Iodine Radioisotopes; D009942:Organometallic Compounds; D019275:Radiopharmaceuticals; C510145:potassium (125I)-(4-isothiocyanatobenzylammonio)iodo-decahydro-closo-dodecaborate