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Characterization of small-molecule inhibitors of the sodium iodide symporter

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dc.creatorLindenthal, Sabinespa
dc.creatorLecat-Guillet, Nathaliespa
dc.creatorOndo Méndez, Alejandro Oyono
dc.creatorAmbroise, Yvesspa
dc.creatorRousseau, Bernardspa
dc.creatorPourcher, Thierryspa
dc.date.accessioned2020-08-19T14:41:52Z
dc.date.available2020-08-19T14:41:52Z
dc.date.created2009-03spa
dc.description.abstractThe sodium/iodide symporter (NIS) mediates the active transport of iodide from the bloodstream into thyrocytes. NIS function is strategic for the diagnosis and treatment of various thyroid diseases. In addition, a promising anti-cancer strategy based on targeted NIS gene transfer in non-thyroidal cells is currently developed. However, only little information is available concerning the molecular mechanism of NIS-mediated iodide translocation. Ten small molecules have recently been identified using a high-throughput screening method for their inhibitory effect on iodide uptake of NIS-expressing mammalian cells. In the present study, we analyzed these compounds for their rapid and reversible effects on the iodide-induced current in NIS-expressing Xenopus oocytes. Four molecules almost completely inhibited the iodide-induced current; for three of them the effect was irreversible, for one compound the initial current could be fully re-established after washout. Three molecules showed a rapid inhibitory effect of about 75%, half of which was reversible. Another three compounds inhibited the iodide-induced current from 10 to 50%. Some molecules altered the membrane conductance by themselves, i.e. in the absence of iodide. For one of these molecules the observed effect was also found in water-injected oocytes whereas for some others the iodide-independent effect was associated with NIS expression. The tested molecules show a surprisingly high variability in their possible mode of action, and thus are promising tools for further functional characterization of NIS on a molecular level, and they could be useful for medical applications.eng
dc.format.mimetypeapplication/pdf
dc.identifier.doihttps://doi.org/10.1677/JOE-08-0246
dc.identifier.issnISSN: 0022-0795
dc.identifier.issnEISSN: 1479-6805
dc.identifier.urihttps://repository.urosario.edu.co/handle/10336/27355
dc.language.isoengspa
dc.publisherSociety for Endocrinologyspa
dc.relation.citationEndPage365
dc.relation.citationIssueNo. 3
dc.relation.citationStartPage357
dc.relation.citationTitleJournal of Endocrinology
dc.relation.citationVolumeVol. 200
dc.relation.ispartofJournal of Endocrinology, ISSN: 0022-0795;EISSN: 1479-6805, Vol.200, No.3 (2009); pp. 357–365spa
dc.relation.urihttps://joe.bioscientifica.com/view/journals/joe/200/3/357.xmlspa
dc.rights.accesRightsinfo:eu-repo/semantics/openAccess
dc.rights.accesoAbierto (Texto Completo)spa
dc.sourceJournal of Endocrinologyspa
dc.source.instnameinstname:Universidad del Rosario
dc.source.reponamereponame:Repositorio Institucional EdocUR
dc.subject.keywordSymportersspa
dc.subject.keywordantagonists & inhibitorsspa
dc.subject.keywordMolecular structurespa
dc.subject.keywordDrug evaluationspa
dc.subject.keywordpreclinicalspa
dc.subject.keywordOocytesspa
dc.subject.keywordmetabolismspa
dc.titleCharacterization of small-molecule inhibitors of the sodium iodide symporterspa
dc.title.TranslatedTitleCaracterización de inhibidores de molécula pequeña del simportador de yoduro de sodiospa
dc.typearticleeng
dc.type.hasVersioninfo:eu-repo/semantics/publishedVersion
dc.type.spaArtículospa
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