{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,9,29]],"date-time":"2026-09-29T13:33:56Z","timestamp":1790688836301,"version":"4.1.0"},"reference-count":50,"publisher":"Oxford University Press (OUP)","issue":"1","content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":[],"published-print":{"date-parts":[[2015,3]]},"DOI":"10.1093\/toxsci\/kfu259","type":"journal-article","created":{"date-parts":[[2014,12,10]],"date-time":"2014-12-10T01:15:19Z","timestamp":1418174119000},"page":"105-113","source":"Crossref","is-referenced-by-count":26,"title":["Functional and Molecular Effects of Mercury Compounds on the Human OCTN1 Cation Transporter: C50 and C136 Are the Targets for Potent Inhibition"],"prefix":"10.1093","volume":"144","author":[{"given":"Michele","family":"Galluccio","sequence":"first","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Lorena","family":"Pochini","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Valentina","family":"Peta","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Maria","family":"Iann\u00ec","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Mariafrancesca","family":"Scalise","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Cesare","family":"Indiveri","sequence":"additional","affiliation":[],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"286","published-online":{"date-parts":[[2014,12,8]]},"reference":[{"key":"key\n\t\t\t\t20170508180821_kfu259-B1","volume-title":"Toxicological Profile for Mercury","author":"ATSDR (Agency for Toxic Substrate and Disease Registry)","year":"2007"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B2","doi-asserted-by":"crossref","first-page":"385","DOI":"10.1080\/10937401003673750","article-title":"Transport of inorganic mercury and methylmercury in target tissues and organs","volume":"13","author":"Bridges","year":"2010","journal-title":"J. Toxicol. Environ. Health. B. Crit. Rev."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B3","doi-asserted-by":"crossref","first-page":"121","DOI":"10.1038\/nature13306","article-title":"Crystal structure of the human glucose transporter GLUT1","volume":"510","author":"Deng","year":"2014","journal-title":"Nature"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B4","doi-asserted-by":"crossref","first-page":"700","DOI":"10.1002\/jat.2855","article-title":"Toxicity of ethylmercury (and Thimerosal): a comparison with methylmercury","volume":"33","author":"Dorea","year":"2013","journal-title":"J. Appl. Toxicol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B5","doi-asserted-by":"crossref","first-page":"12","DOI":"10.1152\/physiolgenomics.00014.2004","article-title":"Novel slc22 transporter homologs in fly, worm, and human clarify the phylogeny of organic anion and cation transporters","volume":"18","author":"Eraly","year":"2004","journal-title":"Physiol. Genomics"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B6","doi-asserted-by":"crossref","first-page":"215","DOI":"10.1016\/j.pep.2009.06.015","article-title":"Over-expression in E. coli and purification of the human OCTN1 transport protein","volume":"68","author":"Galluccio","year":"2009","journal-title":"Protein. Expr. Purif."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B7","doi-asserted-by":"crossref","first-page":"215","DOI":"10.1038\/nrd3028","article-title":"Membrane transporters in drug development","volume":"9","author":"Giacomini","year":"2010","journal-title":"Nat. Rev. Drug. Discov."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B8","doi-asserted-by":"crossref","first-page":"29069","DOI":"10.1074\/jbc.M113.500066","article-title":"FAD synthesis and degradation in the nucleus create a local flavin cofactor pool","volume":"288","author":"Giancaspero","year":"2013","journal-title":"J. Biol. Chem."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B9","doi-asserted-by":"crossref","first-page":"5299","DOI":"10.1016\/j.bbagen.2013.08.003","article-title":"Glutathione controls the redox state of the mitochondrial carnitine\/acylcarnitine carrier Cys residues by glutathionylation","volume":"1830","author":"Giangregorio","year":"2013","journal-title":"Biochim. Biophys. Acta"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B10","doi-asserted-by":"crossref","first-page":"5256","DOI":"10.1073\/pnas.0408624102","article-title":"Discovery of the ergothioneine transporter","volume":"102","author":"Grundemann","year":"2005","journal-title":"Proc. Natl Acad. Sci. U. S. A."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B11","doi-asserted-by":"crossref","first-page":"51","DOI":"10.1016\/0378-1119(89)90358-2","article-title":"Site-directed mutagenesis by overlap extension using the polymerase chain reaction","volume":"77","author":"Ho","year":"1989","journal-title":"Gene"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B12","doi-asserted-by":"crossref","first-page":"1607","DOI":"10.1016\/j.cell.2012.04.012","article-title":"Three-dimensional structures of membrane proteins from genomic sequencing","volume":"149","author":"Hopf","year":"2012","journal-title":"Cell"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B13","doi-asserted-by":"crossref","first-page":"616","DOI":"10.1126\/science.1087619","article-title":"Structure and mechanism of the glycerol-3-phosphate transporter from Escherichia coli","volume":"301","author":"Huang","year":"2003","journal-title":"Science"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B50","doi-asserted-by":"crossref","first-page":"724","DOI":"10.1007\/s12033-012-9586-8","article-title":"Strategies of bacterial over expression of membrane transporters relevant in human health: the successful case of the three members of OCTN subfamily","volume":"54","author":"Indiveri","year":"2013","journal-title":"Mol. Biotechnol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B14","doi-asserted-by":"crossref","first-page":"293","DOI":"10.1016\/0005-2728(94)90048-5","article-title":"Kinetic characterization of the reconstituted ornithine carrier from rat liver mitochondria","volume":"1188","author":"Indiveri","year":"1994","journal-title":"Biochim. Biophys. Acta"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B15","first-page":"108","article-title":"The carnitine transporter network: interactions with drugs","volume":"4","author":"Indiveri","year":"2010","journal-title":"Curr. Chem. Biol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B16","doi-asserted-by":"crossref","first-page":"53","DOI":"10.1016\/0005-2728(92)90019-X","article-title":"The mitochondrial carnitine carrier: characterization of SH-groups relevant for its transport function","volume":"1140","author":"Indiveri","year":"1992","journal-title":"Biochim. Biophys. Acta"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B17","doi-asserted-by":"crossref","first-page":"832","DOI":"10.1007\/s11095-010-0076-z","article-title":"Gene knockout and metabolome analysis of carnitine\/organic cation transporter OCTN1","volume":"27","author":"Kato","year":"2010","journal-title":"Pharm. Res."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B18","doi-asserted-by":"crossref","first-page":"363","DOI":"10.1038\/nprot.2009.2","article-title":"Protein structure prediction on the Web: a case study using the Phyre server","volume":"4","author":"Kelley","year":"2009","journal-title":"Nat. Protoc."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B19","doi-asserted-by":"crossref","first-page":"20","DOI":"10.1186\/1742-2094-7-20","article-title":"Mercury induces inflammatory mediator release from human mast cells","volume":"7","author":"Kempuraj","year":"2010","journal-title":"J. Neuroinflammation"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B20","first-page":"1315","article-title":"Novel localization of OCTN1, an organic cation\/carnitine transporter, to mammalian mitochondria","volume":"345","author":"Lamhonwah","year":"2006","journal-title":"Biophysics. Arch. Biochem. Biophys."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B21","article-title":"Pro-inflammatory effects of metals in persons and animals exposed to tobacco smoke","author":"Milnerowicz","year":"2014","journal-title":"J. Trace Elem. Med. Biol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B22","doi-asserted-by":"crossref","first-page":"1580","DOI":"10.1248\/bpb.31.1580","article-title":"Functional characterization of ergothioneine transport by rat organic cation\/carnitine transporter Octn1 (slc22a4)","volume":"31","author":"Nakamura","year":"2008","journal-title":"Biol. Pharm. Bull."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B23","doi-asserted-by":"crossref","first-page":"1266","DOI":"10.1016\/j.bcp.2010.06.032","article-title":"Inactivation by Hg2+ and methylmercury of the glutamine\/amino acid transporter (ASCT2) reconstituted in liposomes: prediction of the involvement of a CXXC motif by homology modelling","volume":"80","author":"Oppedisano","year":"2010","journal-title":"Biochem. Pharmacol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B24","doi-asserted-by":"crossref","first-page":"2551","DOI":"10.1016\/j.bbamem.2011.05.011","article-title":"The B degrees AT1 amino acid transporter from rat kidney reconstituted in liposomes: kinetics and inactivation by methylmercury","volume":"1808","author":"Oppedisano","year":"2011","journal-title":"Biochim. Biophys. Acta"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B25","doi-asserted-by":"crossref","first-page":"279","DOI":"10.1016\/0076-6879(79)56029-7","article-title":"Direct methods for measuring metabolite transport and distribution in mitochondria","volume":"56","author":"Palmieri","year":"1979","journal-title":"Methods Enzymol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B26","doi-asserted-by":"crossref","first-page":"533","DOI":"10.1038\/nature12042","article-title":"Crystal structure of a eukaryotic phosphate transporter","volume":"496","author":"Pedersen","year":"2013","journal-title":"Nature"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B27","doi-asserted-by":"crossref","first-page":"F1583","DOI":"10.1152\/ajprenal.00496.2006","article-title":"Inorganic mercury interacts with cysteine residues (C451 and C474) of hOCT2 to reduce its transport activity","volume":"292","author":"Pelis","year":"2007","journal-title":"Am. J. Physiol. Renal. Physiol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B28","doi-asserted-by":"crossref","first-page":"471","DOI":"10.1038\/ng1339","article-title":"Functional variants of OCTN cation transporter genes are associated with Crohn disease","volume":"36","author":"Peltekova","year":"2004","journal-title":"Nat. Genet."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B46","doi-asserted-by":"crossref","first-page":"1444","DOI":"10.1016\/j.bmc.2007.10.053","article-title":"Synthesis and characterization of carnitine nitro-derivatives","volume":"16","author":"Piermatti","year":"2008","journal-title":"Bioorg. Med. Chem."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B29","doi-asserted-by":"crossref","first-page":"68","DOI":"10.3109\/15376516.2012.719166","article-title":"Inhibition of the OCTN2 carnitine transporter by HgCl2 and methylmercury in the proteoliposome experimental model: insights in the mechanism of toxicity","volume":"23","author":"Pochini","year":"2013","journal-title":"Toxicol. Mech. Methods"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B47","doi-asserted-by":"crossref","first-page":"394","DOI":"10.1016\/j.cbi.2008.10.052","article-title":"Inactivation by omeprazole of the carnitine transporter (OCTN2) reconstituted in liposomes","volume":"179","author":"Pochini","year":"2009","journal-title":"Chem. Biol. Interact."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B30","doi-asserted-by":"crossref","first-page":"227","DOI":"10.1042\/BJ20110544","article-title":"Reconstitution in liposomes of the functionally active human OCTN1 (SLC22A4) transporter overexpressed in Escherichia coli","volume":"439","author":"Pochini","year":"2011","journal-title":"Biochem. J."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B31","doi-asserted-by":"crossref","first-page":"1013","DOI":"10.1016\/j.lfs.2012.04.027","article-title":"Regulation by physiological cations of acetylcholine transport mediated by human OCTN1 (SLC22A4). Implications in the non-neuronal cholinergic system","volume":"91","author":"Pochini","year":"2012","journal-title":"Life Sci."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B48","doi-asserted-by":"crossref","first-page":"851","DOI":"10.1177\/1087057113493006","article-title":"OCTN cation transporters in health and disease: role as drug targets and assay development","volume":"18","author":"Pochini","year":"2013","journal-title":"J. Biomol. Screen."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B32","doi-asserted-by":"crossref","first-page":"559","DOI":"10.1016\/j.bbamem.2011.12.014","article-title":"The human OCTN1 (SLC22A4) reconstituted in liposomes catalyzes acetylcholine transport which is defective in the mutant L503F associated to the Crohn\u2019s disease","volume":"1818","author":"Pochini","year":"2012","journal-title":"Biochim. Biophys. Acta"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B33","doi-asserted-by":"crossref","first-page":"422","DOI":"10.1016\/j.bcp.2014.03.014","article-title":"Nimesulide binding site in the B0AT1 (SLC6A19) amino acid transporter. Mechanism of inhibition revealed by proteoliposome transport assay and molecular modelling","volume":"89","author":"Pochini","year":"2014","journal-title":"Biochem. Pharmacol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B34","doi-asserted-by":"crossref","first-page":"82","DOI":"10.1016\/j.autneu.2010.04.011","article-title":"Acetylcholine as an age-dependent non-neuronal source in the heart","volume":"156","author":"Rana","year":"2010","journal-title":"Auton. Neurosci."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B35","doi-asserted-by":"crossref","first-page":"59","DOI":"10.1016\/j.bbrc.2012.04.105","article-title":"Over-expression in Escherichia coli, purification and reconstitution in liposomes of the third member of the OCTN sub-family: the mouse carnitine transporter OCTN3","volume":"422","author":"Scalise","year":"2012","journal-title":"Biochem. Biophys. Res. Commun."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B36","doi-asserted-by":"crossref","first-page":"472","DOI":"10.3390\/pharmaceutics5030472","article-title":"Proteoliposomes as tool for assaying membrane transporter functions and interactions with xenobiotics","volume":"5","author":"Scalise","year":"2013","journal-title":"Pharmaceutics"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B37","doi-asserted-by":"crossref","first-page":"139","DOI":"10.1016\/S0946-672X(02)80015-3","article-title":"The impact of food contaminants on the bioavailability of trace metals","volume":"16","author":"Sch\u00fcmann","year":"2002","journal-title":"J. Trace Elem. Med. Biol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B38","doi-asserted-by":"crossref","first-page":"40064","DOI":"10.1074\/jbc.M005340200","article-title":"Molecular and functional characterization of organic cation\/carnitine transporter family in mice","volume":"275","author":"Tamai","year":"2000","journal-title":"J. Biol. Chem."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B39","doi-asserted-by":"crossref","first-page":"2509","DOI":"10.1021\/mp400193r","article-title":"Functional analysis of novel variants in the organic cation\/ergothioneine transporter 1 identified in Singapore populations","volume":"10","author":"Toh","year":"2013","journal-title":"Mol. Pharm."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B40","doi-asserted-by":"crossref","first-page":"1205","DOI":"10.1007\/s10534-011-9479-5","article-title":"Effects of heavy metal cations on the mitochondrial ornithine\/citrulline transporter reconstituted in liposomes","volume":"24","author":"Tonazzi","year":"2011","journal-title":"Biometals"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B49","doi-asserted-by":"crossref","first-page":"e82286","DOI":"10.1371\/journal.pone.0082286","article-title":"Molecular mechanism of inhibition of the mitochondrial carnitine\/acylcarnitine transporter by omeprazole revealed by proteoliposome assay, mutagenesis and bioinformatics","volume":"8","author":"Tonazzi","year":"2013","journal-title":"PLoS One"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B41","doi-asserted-by":"crossref","first-page":"161","DOI":"10.1016\/0304-4157(92)90037-B","article-title":"What we can learn from the effects of thiol reagents on transport proteins","volume":"1113","author":"van Iwaarden","year":"1992","journal-title":"Biochim. Biophys. Acta"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B42","doi-asserted-by":"crossref","first-page":"384","DOI":"10.1038\/nature01339","article-title":"Nicotinic acetylcholine receptor alpha7 subunit is an essential regulator of inflammation","volume":"421","author":"Wang","year":"2003","journal-title":"Nature"},{"key":"key\n\t\t\t\t20170508180821_kfu259-B43","doi-asserted-by":"crossref","first-page":"1558","DOI":"10.1038\/bjp.2008.185","article-title":"Acetylcholine beyond neurons: the non-neuronal cholinergic system in humans","volume":"154","author":"Wessler","year":"2008","journal-title":"Br. J. Pharmacol."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B44","doi-asserted-by":"crossref","first-page":"768","DOI":"10.1016\/S0022-3565(24)38199-6","article-title":"Novel membrane transporter OCTN1 mediates multispecific, bidirectional, and pH-dependent transport of organic cations","volume":"289","author":"Yabuuchi","year":"1999","journal-title":"J. Pharmacol. Exp. Ther."},{"key":"key\n\t\t\t\t20170508180821_kfu259-B45","doi-asserted-by":"crossref","first-page":"559","DOI":"10.1007\/s10126-013-9508-1","article-title":"Selenoneine, a novel selenium-containing compound, mediates detoxification mechanisms against methylmercury accumulation and toxicity in zebrafish embryo","volume":"15","author":"Yamashita","year":"2013","journal-title":"Mar. Biotechnol. (NY)"}],"container-title":["Toxicological Sciences"],"original-title":[],"language":"en","link":[{"URL":"http:\/\/academic.oup.com\/toxsci\/article-pdf\/144\/1\/105\/16687732\/kfu259.pdf","content-type":"unspecified","content-version":"vor","intended-application":"similarity-checking"}],"deposited":{"date-parts":[[2025,5,14]],"date-time":"2025-05-14T00:13:48Z","timestamp":1747181628000},"score":1,"resource":{"primary":{"URL":"https:\/\/academic.oup.com\/toxsci\/article-lookup\/doi\/10.1093\/toxsci\/kfu259"}},"subtitle":[],"short-title":[],"issued":{"date-parts":[[2014,12,8]]},"references-count":50,"journal-issue":{"issue":"1","published-online":{"date-parts":[[2014,12,8]]},"published-print":{"date-parts":[[2015,3]]}},"URL":"https:\/\/doi.org\/10.1093\/toxsci\/kfu259","relation":{},"ISSN":["1096-0929","1096-6080"],"issn-type":[{"value":"1096-0929","type":"electronic"},{"value":"1096-6080","type":"print"}],"subject":[],"published":{"date-parts":[[2014,12,8]]}}}