title: High-efficiency astatination of antibodies using N-iodosuccinimide as the oxidising agent in labelling of N-succinimidyl 3-(trimethylstannyl)benzoate.
abstract: Monoclonal antibodies C215, reactive with colorectal carcinomas, and MOv18, reactive with most of the ovarian carcinomas, were radiohalogenated with [211At]astatine. The radiohalogen was conjugate coupled to antibodies via the intermediate labelling reagent N-succinimidyl-3-(trimethylstannyl)benzoate (m-MeATE) in a two-step, single-pot reaction. Optimisation of the labelling of the reagent was achieved using N-iodosuccinimide, NIS, as the oxidising agent. The yields ranged from 69-95% in the labelling of 0.1-1.0 nmole of the m-MeATE precursor. Subsequent conjugation to antibodies resulted in yields of 58+/-7%. In vitro binding to tumour cells showed that the immunoreactivity of both antibodies was retained after astatine labelling.
authors.affiliation: Department of Radiation Physics, Göteborg University, Sahlgrenska University Hospital, SE-413 45, Göteborg, Sweden. sture.lindegren@radfys.gu.se
authors.forename: S
authors.initials: S
authors.lastname: Lindegren
authors.forename: H
authors.initials: H
authors.lastname: Andersson
authors.forename: T
authors.initials: T
authors.lastname: Bäck
authors.forename: L
authors.initials: L
authors.lastname: Jacobsson
authors.forename: B
authors.initials: B
authors.lastname: Karlsson
authors.forename: G
authors.initials: G
authors.lastname: Skarnemark
mesh_terms: D000911:Antibodies, Monoclonal / Q000276:immunology* / Q000378:metabolism; D001246:Astatine / Q000276:immunology* / Q000378:metabolism; D001565:Benzoates / Q000276:immunology; D015179:Colorectal Neoplasms / Q000000981:diagnostic imaging / Q000276:immunology* / Q000378:metabolism; D006801:Humans; D011877:Radionuclide Imaging; D013388:Succinimides / Q000737:chemistry*; D014298:Trimethyltin Compounds / Q000276:immunology; D014407:Tumor Cells, Cultured / Q000000981:diagnostic imaging / Q000276:immunology / Q000378:metabolism
chemical_list: D000911:Antibodies, Monoclonal; D001565:Benzoates; D013388:Succinimides; D014298:Trimethyltin Compounds; C061345:N-succinimidyl 3-(trimethylstannyl)benzoate; C008155:N-iodosuccinimide; D001246:Astatine