title: A 96-well automated radioiodide uptake assay for sodium/iodide symporter inhibitors.
abstract: A high-throughput screening method based on radioiodide uptake in human embryonic kidney 293 cells expressing the human sodium/iodide symporter was developed. Central to assay development was a homogeneous cell culture in the 96-well microplate coupled with the use of scintillation proximity technology. The assay is fast and highly reproducible with a Z' greater than 0.8. The automated procedure allows the screening of 4,000 compounds per day. Using this methodology, several known substrates of the sodium/iodide symporter were evaluated in a single day. Inhibition of iodide uptake was shown to follow the series PF(6)(-) > ClO(4)(-) > BF(4)(-) > SCN(-) >> NO(3)(-) > IO(4)(-) > N(3)(-) >> Br(-), in accord with the literature. This method represents an initial approach to the search for inhibitors of iodide transport mediated by the sodium/iodide symporter.
authors.affiliation: iBiTecS, Service de Chimie Bioorganique et de Marquage, CEA, Gif sur Yvette, France.
authors.forename: Nathalie
authors.initials: N
authors.lastname: Lecat-Guillet
authors.forename: Goulven
authors.initials: G
authors.lastname: Merer
authors.forename: Roman
authors.initials: R
authors.lastname: Lopez
authors.forename: Thierry
authors.initials: T
authors.lastname: Pourcher
authors.forename: Bernard
authors.initials: B
authors.lastname: Rousseau
authors.forename: Yves
authors.initials: Y
authors.lastname: Ambroise
mesh_terms: D001331:Automation; D002384:Catalysis; D002460:Cell Line; D003584:Cytological Techniques; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007457:Iodine Radioisotopes / Q000378:metabolism; D027981:Symporters / Q000037:antagonists & inhibitors*; D000099209:Sodium-Iodide Symporters
chemical_list: D007457:Iodine Radioisotopes; D027981:Symporters; D000099209:Sodium-Iodide Symporters