AI Article Synopsis
- The Na(+)/I(-) symporter (NIS) is crucial for iodide uptake in thyroid cells, but how it is regulated after being created (post-translational regulation) is not fully understood.
- This study aimed to find and understand inhibitors of NIS, screening over 17,000 drug-like compounds to identify new chemical inhibitors with strong effects.
- The inhibitors discovered do not affect the sodium gradient and lead to quick iodide release, suggesting they modify NIS activity through different mechanisms.
Article Abstract
The Na(+)/I(-) symporter (NIS) mediates iodide uptake into thyroid follicular cells. Although NIS has been cloned and thoroughly studied at the molecular level, the biochemical processes involved in post-translational regulation of NIS are still unknown. The purpose of this study was to identify and characterize inhibitors of NIS function. These small organic molecules represent a starting point in the identification of pharmacological tools for the characterization of NIS trafficking and activation mechanisms. The screening of a collection of 17,020 druglike compounds revealed new chemical inhibitors with potencies down to 40 nM. Fluorescence measurement of membrane potential indicates that these inhibitors do not act by disrupting the sodium gradient. They allow immediate and total iodide discharge from preloaded cells in accord with a specific modification of NIS activity, probably through distinct mechanisms.
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| http://dx.doi.org/10.1002/cbic.200700682 | DOI Listing |
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