title: A rapid luciferase transfection assay for transcription activation effects and stability control of estrogenic drugs in cell cultures.
abstract: A rapid assay system for measuring the potential of estrogenic drugs is introduced. Luciferase induction could be measured in estrogen-receptor-positive human MCF-7 breast cancer cells, which had been transfected with a novel luciferase reporter plasmid ERE luc. The minimal requirement was 1 h exposure to the inducing drug and 3.5 h of incubation after removal of the drug. The assay system was used to measure the stability of the drug diaqua-[1,2-bis (2,6-dichloro-4-hydroxyphenyl) ethylenediamine] platinum(II) sulfate, containing an estrogenic ligand and reactive platinum. Luciferase activity was observed only when the drug was in the culture medium and cells for short times, whereas the estrogenic ligand alone remained active. It is assumed that binding of the platinum moiety to macromolecular constituents of the culture or cells renders the drug inaccessible for binding to the estrogen receptor.
authors.affiliation: Institut für Biophysik und physikalische Biochemie, Universität Regensburg, Germany.
authors.forename: T
authors.initials: T
authors.lastname: Meyer
authors.forename: R
authors.initials: R
authors.lastname: Koop
authors.forename: E
authors.initials: E
authors.lastname: von Angerer
authors.forename: H
authors.initials: H
authors.lastname: Schönenberger
authors.forename: E
authors.initials: E
authors.lastname: Holler
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology*; D001943:Breast Neoplasms / Q000378:metabolism; D004789:Enzyme Activation / Q000187:drug effects; D004958:Estradiol / Q000494:pharmacology; D004968:Estrogens, Non-Steroidal / Q000494:pharmacology*; D005260:Female; D006801:Humans; D008156:Luciferases / Q000235:genetics*; D009944:Organoplatinum Compounds / Q000494:pharmacology*; D011960:Receptors, Estrogen / Q000187:drug effects; D014158:Transcription, Genetic / Q000187:drug effects; D014162:Transfection; D014407:Tumor Cells, Cultured
chemical_list: D000970:Antineoplastic Agents; D004968:Estrogens, Non-Steroidal; D009944:Organoplatinum Compounds; D011960:Receptors, Estrogen; D004958:Estradiol; C042922:dichloro(1,2-bis(4-hydroxyphenyl)ethylenediamine)platinum II; D008156:Luciferases