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Small-molecule inhibitors of sodium iodide symporter function
Nathalie Lecat-Guillet1, Goulven Merer, Roman Lopez
1Department of Bioorganic Chemistry and Isotopic Labelling, CEA, Institute of Biology and Technology (iBiTecS), Gif-sur-Yvette 91191, France.
Chembiochem : a European Journal of Chemical Biology
|March 1, 2008
Summary
Researchers identified novel chemical inhibitors for the sodium/iodide symporter (NIS) to understand its regulation. These compounds offer potential pharmacological tools for studying NIS trafficking and activation mechanisms.
Area of Science:
- Biochemistry
- Molecular Biology
- Pharmacology
Background:
- The sodium/iodide symporter (NIS) is crucial for iodide uptake in thyroid follicular cells.
- While NIS is well-characterized at the molecular level, its post-translational regulation remains largely unknown.
Purpose of the Study:
- To identify and characterize small organic molecules that inhibit NIS function.
- To provide starting points for developing pharmacological tools to study NIS trafficking and activation.
Main Methods:
- Screening of a library of 17,020 druglike compounds.
- Fluorescence measurement of membrane potential to assess inhibitor action.
- Analysis of iodide discharge from preloaded cells.
Main Results:
- Discovery of novel chemical inhibitors of NIS with potencies as low as 40 nM.
- Inhibitors do not disrupt the sodium gradient across the cell membrane.
- Inhibitors induce immediate and complete iodide discharge, suggesting specific modification of NIS activity.
Conclusions:
- New chemical inhibitors of NIS have been identified.
- These inhibitors likely act through distinct mechanisms to modify NIS activity.
- The identified compounds are valuable tools for further research into NIS regulation.
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