title: Bromine-80m radiotoxicity and the potential for estrogen receptor-directed therapy with auger electrons.
abstract: While theoretically feasible, estrogen receptor (ER)-directed radiotherapy of hormone-dependent cancers has not been realized because no ER-seeking ligand with an appropriate radiotoxic potential has been identified. Since an appropriate nuclide is a key component we studied the 4.4-h half-life, Auger electron-emitting nuclide bromine-80m. When incorporated into DNA this nuclide was radiotoxic to cells in culture and caused substantial chromosomal damage, while similar concentrations of bromine-80m as bromide or bromoantipyrine were without effect. The mean lethal dose for bromine-80m was 45 atoms per nucleus which is consistent with use in receptor-positive cancers with limited numbers of ER.
authors.affiliation: Ben May Institute, University of Chicago, Illinois 60637.
authors.forename: E R
authors.initials: ER
authors.lastname: DeSombre
authors.forename: P V
authors.initials: PV
authors.lastname: Harper
authors.forename: A
authors.initials: A
authors.lastname: Hughes
authors.forename: R C
authors.initials: RC
authors.lastname: Mease
authors.forename: S J
authors.initials: SJ
authors.lastname: Gatley
authors.forename: O T
authors.initials: OT
authors.lastname: DeJesus
authors.forename: J L
authors.initials: JL
authors.lastname: Schwartz
mesh_terms: D000818:Animals; D001967:Bromine Radioisotopes / Q000633:toxicity*; D001973:Bromodeoxyuridine; D002460:Cell Line; D004249:DNA Damage; D004583:Electrons; D006207:Half-Life; D008722:Methods; D009376:Neoplasms, Hormone-Dependent / Q000532:radiotherapy*; D011960:Receptors, Estrogen / Q000378:metabolism*
chemical_list: D001967:Bromine Radioisotopes; D011960:Receptors, Estrogen; D001973:Bromodeoxyuridine