In vitro investigations of the direct effects of complex anions on thyroidal iodide uptake: Identification of novel inhibitors

Toxicology in Vitro : an International Journal Published in Association with BIBRA
P A JonesM D Barratt

Abstract

Iodide uptake (IU) by thyrocytes from the plasma against chemical and electrical gradients is by a specific iodide transporter or 'pump'. Perchlorate (ClO(4)(-)) and other univalent, symmetrical anions are competitive inhibitors of iodide uptake (IU), and apparent K(i) for individual anions can be correlated with ion size. This study uses cultured thyrocytes and a broad range of anion size, in particular a series of spherical hexafluoride ions, in order to understand more about the parameters governing the activity of competitive inhibitors of IU. (125)I uptake and organification by cultured porcine thyrocytes was combined with biochemical enzyme inhibition studies on thyroid peroxidase in order to identify specific effects on IU. Known inhibitors were used in a validation phase and demonstrated that a combination of the in vitro thyrocyte (125)I assay and thyroid peroxidase inhibition assay could be used to identify selective inhibitors that can be difficult to identify using thyrocytes alone. Anions of less than, or similar, volume to I(-) (35.0 A(3)) were weak inhibitors with potency increasing proportional to ion size up to an apparent maximum for AsF(6)(-) (94.45 A(3)); this correlation was strong (r = 0.96). PF(6)(-), AsF...Continue Reading

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Citations

Jun 26, 2010·European Journal of Nuclear Medicine and Molecular Imaging·Maite Jauregui-OsoroPhilip J Blower
Sep 5, 2007·Assay and Drug Development Technologies·Nathalie Lecat-GuilletYves Ambroise
Mar 1, 2008·Chembiochem : a European Journal of Chemical Biology·Nathalie Lecat-GuilletYves Ambroise
Sep 8, 2009·Analytical Biochemistry·Fanny WaltzYves Ambroise
May 13, 2008·ChemMedChem·Nathalie Lecat-Guillet, Yves Ambroise
Aug 3, 2005·Toxicology in Vitro : an International Journal Published in Association with BIBRA·J JanosekI Holoubek
Jun 21, 2017·Critical Reviews in Toxicology·Marie-Emilie Willemin, Annie Lumen

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