Radioprotective Molecules
Iodide entrapment in the thyroid gland is essential, and plays a key role in dysfunctions such as thyroid and breast cancers, thyroiditis, Graves–Basedow disease, and Hashimoto's disease.
The accidents at Chernobyl and Fukushima have revealed growing public concerns, as exposure to radioactive iodine increases the risk of cancer and birth defects. There is an urgent need to find radioprotective molecules to prevent and treat body contamination.
Yves Ambroise and colleagues at the Biology and Technology Institute (IBiTecS, France) identified an important class of compounds that efficiently block iodide transport by inhibiting the sodium iodide symporter, and their results are reported in ChemMedChem.
During a hit optimization program, they synthesized and tested more than 100 molecules for their capacity to block iodide entrapment in rat thyroid cells. They identified a new lead compound with nanomolar activity and low toxicity. This discovery opens new perspectives for the development of novel anti-thyroid drugs and radioprotective molecules, as well as pharmacological tools for further investigation of iodide traffic at the cellular level.
About the Author
Yves Ambroise is a research group leader in the Biology and Technology Institute (IBiTecS) at the French Alternative Energies and Atomic Energy Commission (CEA). His main areas of interest are chemical biology and drug discovery using techniques such as high-throughput screening, chemical optimization, and target identification by chemical proteomic methods. His research focuses on the mechanism of iodide uptake in the thyroid gland. He is a member of the Laboratory of Excellence in Research on Medication and Innovative Therapeutics (LERMIT).
Author: Yves Ambroise, Alternative Energies and Atomic Energy Commission, CEA, Gif-sur-Yvette (France), http://www-dsv.cea.fr/institutes/institute-of-biology-and-technology-saclay-ibitec-s/units/molecular-labelling-and-bio-organic-chemistry-scbm/bioorganic-chemistry-laboratory-lcb/transport-and-metabolism-of-iodine-y.-ambroise
Title: Synthesis and Evaluation of 3,4-Dihydropyrimidin-2(1H)-ones as Sodium Iodide Symporter Inhibitors
ChemMedChem 2013, 8, No. 1, Permalink to the article: http://dx.doi.org/10.1002/cmdc.201200417
Media Contact
More Information:
http://www.wiley.comAll latest news from the category: Life Sciences and Chemistry
Articles and reports from the Life Sciences and chemistry area deal with applied and basic research into modern biology, chemistry and human medicine.
Valuable information can be found on a range of life sciences fields including bacteriology, biochemistry, bionics, bioinformatics, biophysics, biotechnology, genetics, geobotany, human biology, marine biology, microbiology, molecular biology, cellular biology, zoology, bioinorganic chemistry, microchemistry and environmental chemistry.
Newest articles
Machine learning algorithm reveals long-theorized glass phase in crystal
Scientists have found evidence of an elusive, glassy phase of matter that emerges when a crystal’s perfect internal pattern is disrupted. X-ray technology and machine learning converge to shed light…
Mapping plant functional diversity from space
HKU ecologists revolutionize ecosystem monitoring with novel field-satellite integration. An international team of researchers, led by Professor Jin WU from the School of Biological Sciences at The University of Hong…
Inverters with constant full load capability
…enable an increase in the performance of electric drives. Overheating components significantly limit the performance of drivetrains in electric vehicles. Inverters in particular are subject to a high thermal load,…
