A 96-well automated radioiodide uptake assay for sodium/iodide symporter inhibitors

作者：Lecat Guillet Nathalie; Merer Goulven; Lopez Roman; Pourcher Thierry; Rousseau Bernard; Ambroise Yves^*

来源：Assay and Drug Development Technologies, 2007, 5(4): 535-540.

DOI：10.1089/adt.2007.068

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 PF6- > ClO4- > BF4- > SCN- >> NO3- > IO4- > 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.

• 出版日期2007-8
• 单位中国地震局