organic cation transport proteins


Summary: A family of proteins involved in the transport of organic cations. They play an important role in the elimination of a variety of endogenous substances, xenobiotics, and their metabolites from the body.

Top Publications

  1. Matsumoto T, Kanamoto T, Otsuka M, Omote H, Moriyama Y. Role of glutamate residues in substrate recognition by human MATE1 polyspecific H+/organic cation exporter. Am J Physiol Cell Physiol. 2008;294:C1074-8 pubmed publisher
    ..These results suggest that all of these glutamate residues are involved in binding and/or transport of TEA and cimetidine but that their individual roles are different. ..
  2. Katsuda H, Yamashita M, Katsura H, Yu J, Waki Y, Nagata N, et al. Protecting cisplatin-induced nephrotoxicity with cimetidine does not affect antitumor activity. Biol Pharm Bull. 2010;33:1867-71 pubmed
    ..From these results, cimetidine clearly inhibits nephrotoxicity induced by cisplatin without any influence on the antitumor activity of cisplatin on osteosarcoma in vitro and in vivo. ..
  3. Morrow C, Ghattas M, Smith C, Bonisch H, Bryce R, Hickinson D, et al. Src family kinase inhibitor Saracatinib (AZD0530) impairs oxaliplatin uptake in colorectal cancer cells and blocks organic cation transporters. Cancer Res. 2010;70:5931-41 pubmed publisher
    ..These data suggest that oxaliplatin uptake in CRC is attenuated by saracatinib via inhibition of OCT2, a potential consideration for the clinical development of this SFK inhibitor. ..
  4. Moreno Navarrete J, Ortega F, Rodríguez Hermosa J, Sabater M, Pardo G, Ricart W, et al. OCT1 Expression in adipocytes could contribute to increased metformin action in obese subjects. Diabetes. 2011;60:168-76 pubmed publisher
    ..OCT1 gene expression and protein levels are detectable in adipose tissue. Increased OCT1 gene expression in adipose tissue of obese subjects might contribute to increased metformin action in these subjects. ..
  5. Nies A, Hofmann U, Resch C, Schaeffeler E, Rius M, Schwab M. Proton pump inhibitors inhibit metformin uptake by organic cation transporters (OCTs). PLoS ONE. 2011;6:e22163 pubmed publisher
    ..Further studies are needed to elucidate the clinical relevance of this drug-drug interaction with potential consequences on metformin disposition and/or efficacy. ..
  6. Kuriki S, Okada R, Suzuki K, Ito Y, Morita E, Naito M, et al. SLC22A12 W258X frequency according to serum uric acid level among Japanese health checkup examinees. Nagoya J Med Sci. 2011;73:41-8 pubmed
    ..The observed SUA level changes in individuals with 258WX suggested that lifestyle factors could influence the levels of those with 258WX...
  7. Sayed Ahmed M, Al Shabanah O, Hafez M, Aleisa A, Al Rejaie S. Inhibition of gene expression of heart fatty acid binding protein and organic cation/carnitine transporter in doxorubicin cardiomyopathic rat model. Eur J Pharmacol. 2010;640:143-9 pubmed publisher
    ..The progressive increase in cardiotoxicity enzymatic indices and the decrease in H-FABP and OCTN2 expression may point to the possible contribution of H-FABP and OCTN2 as a mechanism during development of doxorubicin cardiotoxicity. ..
  8. Nakamura M, Anzai N, Jutabha P, Sato H, Sakurai H, Ichida K. Concentration-dependent inhibitory effect of irbesartan on renal uric acid transporters. J Pharmacol Sci. 2010;114:115-8 pubmed
    ..The inhibitory effects of irbesartan exceeded those of losartan and other ARBs, and the results suggest that irbesartan can reduce serum uric acid level. ..
  9. Duan H, Wang J. Selective transport of monoamine neurotransmitters by human plasma membrane monoamine transporter and organic cation transporter 3. J Pharmacol Exp Ther. 2010;335:743-53 pubmed publisher
    ..hPMAT, on the other hand, is a major uptake(2) transporter for 5-HT and dopamine and may play a more important role in transporting these two neurotransmitters in the central nervous system. ..

More Information


  1. Minematsu T, Giacomini K. Interactions of tyrosine kinase inhibitors with organic cation transporters and multidrug and toxic compound extrusion proteins. Mol Cancer Ther. 2011;10:531-9 pubmed publisher
    ..The study provides the basis for further clinical DDI studies with TKIs. ..
  2. Yamauchi K, Shikanai T, Nakamura Y, Kobayashi H, Ogasawara M, Maeyama K. [Roles of histamine in the pathogenesis of bronchial asthma and reevaluation of the clinical usefulness of antihistamines]. Yakugaku Zasshi. 2011;131:185-91 pubmed
    ..H1-blockers are recommended as first-line drugs to treat allergic rhinitis in the guidelines. Therefore H1-blockers are strongly recommended for patients with both asthma and allergic rhinitis...
  3. Galluccio M, Amelio L, Scalise M, Pochini L, Boles E, Indiveri C. Over-expression in E. coli and purification of the human OCTN2 transport protein. Mol Biotechnol. 2012;50:1-7 pubmed publisher
    ..The resulting protein was expressed in E. coli Rosetta(DE3)pLysS and purified by Ni(2+)-chelating chromatography. A yield of about 3.5 mg purified protein per liter of cell culture was obtained with this procedure. ..
  4. Kido Y, Matsson P, Giacomini K. Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2. J Med Chem. 2011;54:4548-58 pubmed publisher
    ..Two compounds showed different kinetics of interaction with the common polymorphism OCT2-A270S, suggesting a role of genetics in modulating renal DDIs. ..
  5. Chen L, Pawlikowski B, Schlessinger A, More S, Stryke D, Johns S, et al. Role of organic cation transporter 3 (SLC22A3) and its missense variants in the pharmacologic action of metformin. Pharmacogenet Genomics. 2010;20:687-99 pubmed publisher
    ..Our study suggests that OCT3 plays a role in the therapeutic action of metformin and that genetic variants of OCT3 may modulate metformin and catecholamine action. ..
  6. Xuan C, Zhang B, Yang T, Deng K, Li M, Tian R. Association between OCTN1/2 gene polymorphisms (1672C-T, 207G-C) and susceptibility of Crohn's disease: a meta-analysis. Int J Colorectal Dis. 2012;27:11-9 pubmed publisher
    ..Significant associations were not found in the East Asian population. This meta-analysis suggests that OCTN1/2 polymorphisms were associated with susceptibility of CD in the Caucasian population but not in the East Asian population. ..
  7. Pochini L, Scalise M, Galluccio M, Amelio L, Indiveri C. Reconstitution in liposomes of the functionally active human OCTN1 (SLC22A4) transporter overexpressed in Escherichia coli. Biochem J. 2011;439:227-33 pubmed publisher
    ..77 mM was calculated. Acetylcholine and ?-butyrobetaine behaved as competitive inhibitors of TEA (tetraethylammonium) transport with K(i) values of 0.44 and 0.63 mM respectively. ..
  8. Tin A, Woodward O, Kao W, Liu C, Lu X, Nalls M, et al. Genome-wide association study for serum urate concentrations and gout among African Americans identifies genomic risk loci and a novel URAT1 loss-of-function allele. Hum Mol Genet. 2011;20:4056-68 pubmed publisher
    ..Our data support the importance of multi-ethnic GWAS in the identification of novel risk loci as well as functional variants. ..
  9. Chu S, Ma Y, Feng D, Zhang H, Qiu J, Zhu Z. Effect of 5-Aza-2'-deoxycytidine on SLC22A18 in glioma U251 cells. Mol Med Rep. 2012;5:138-41 pubmed publisher
    ..The hypermethylation of SLC22A18 may be related to the transcriptional silencing of this gene. The growth inhibitory effects of 5-Aza-CdR treatment in vivo remain recognizable. ..
  10. Seo P, Park J, Park M, Kim Y, Kim S, Jung J, et al. A Golgi-localized MATE transporter mediates iron homoeostasis under osmotic stress in Arabidopsis. Biochem J. 2012;442:551-61 pubmed publisher
    ..The BCD1 protein is localized to the Golgi complex. We propose that the BCD1 transporter plays a role in sustaining iron homoeostasis by reallocating excess iron released from stress-induced cellular damage. ..
  11. Chu S, Ma Y, Feng D, Zhang H, Zhu Z, Li Z, et al. Correlation of low SLC22A18 expression with poor prognosis in patients with glioma. J Clin Neurosci. 2012;19:95-8 pubmed publisher
    ..This study suggests that SLC22A18 functions as a tumor suppressor in glioma and represents a candidate biomarker for long-term survival in this disease. ..
  12. Pochini L, Scalise M, Galluccio M, Pani G, Siminovitch K, Indiveri C. The human OCTN1 (SLC22A4) reconstituted in liposomes catalyzes acetylcholine transport which is defective in the mutant L503F associated to the Crohn's disease. Biochim Biophys Acta. 2012;1818:559-65 pubmed publisher
    ..These data identify a new transport role for OCTN1 and raise the possibility that its involvement in the non-neuronal acetylcholine system may be relevant to the pathogenesis of Crohn's disease. ..
  13. Angelini S, Pantaleo M, Ravegnini G, Zenesini C, Cavrini G, Nannini M, et al. Polymorphisms in OCTN1 and OCTN2 transporters genes are associated with prolonged time to progression in unresectable gastrointestinal stromal tumours treated with imatinib therapy. Pharmacol Res. 2013;68:1-6 pubmed publisher
    ..Further investigations are required in an attempt to further personalize GIST therapy. ..
  14. Franke R, Kosloske A, Lancaster C, Filipski K, Hu C, Zolk O, et al. Influence of Oct1/Oct2-deficiency on cisplatin-induced changes in urinary N-acetyl-beta-D-glucosaminidase. Clin Cancer Res. 2010;16:4198-206 pubmed publisher
    ..1; 95% confidence interval, 2.1-31; P = 0.0078). Cimetidine is able to inhibit OCT2-mediated uptake of cisplatin in the kidney, and subsequently ameliorate nephrotoxicity likely with minimal effect on uptake in tumor cells. ..
  15. Ciarimboli G, Holle S, Vollenbröcker B, Hagos Y, Reuter S, Burckhardt G, et al. New clues for nephrotoxicity induced by ifosfamide: preferential renal uptake via the human organic cation transporter 2. Mol Pharm. 2011;8:270-9 pubmed publisher
    ..We propose that the nephrotoxicity of ifosfamide is due to its selective uptake by hOCT2 into renal proximal tubular cells, and that coadministration of cimetidine may be used to prevent ifosfamide-induced nephrotoxicity. ..
  16. Yokosho K, Yamaji N, Ma J. An Al-inducible MATE gene is involved in external detoxification of Al in rice. Plant J. 2011;68:1061-9 pubmed publisher
    ..Taken together, our results show that OsFRDL4 is an Al-induced citrate transporter localized at the plasma membrane of rice root cells and is one of the components of high Al tolerance in rice. ..
  17. Horvath G, Mendes E, Schmid N, Schmid A, Conner G, Fregien N, et al. Rapid nongenomic actions of inhaled corticosteroids on long-acting ?(2)-agonist transport in the airway. Pulm Pharmacol Ther. 2011;24:654-9 pubmed publisher
    ..Potency rank order and other 'classical' features of anti-inflammatory effects do not apply to inhaled corticosteroids' rapid drug transport actions. ..
  18. Filippo C, Ardon O, Longo N. Glycosylation of the OCTN2 carnitine transporter: study of natural mutations identified in patients with primary carnitine deficiency. Biochim Biophys Acta. 2011;1812:312-20 pubmed publisher
    ..Glycosylation does not affect maturation of OCTN2 transporters to the plasma membrane, but the 3 asparagines that are normally glycosylated are located in a region important for substrate recognition and turnover rate. ..
  19. Chu S, Feng D, Ma Y, Zhang H, Zhu Z, Li Z, et al. Promoter methylation and downregulation of SLC22A18 are associated with the development and progression of human glioma. J Transl Med. 2011;9:156 pubmed publisher
    ..SLC22A18 downregulation via promoter methylation is associated with the development and progression of glioma, suggesting that SLC22A18 is an important tumor suppressor in glioma. ..
  20. Jutabha P, Anzai N, Kitamura K, Taniguchi A, Kaneko S, Yan K, et al. Human sodium phosphate transporter 4 (hNPT4/SLC17A3) as a common renal secretory pathway for drugs and urate. J Biol Chem. 2010;285:35123-32 pubmed publisher
    ..Our findings will complete a model of urate secretion in the renal tubular cell, where intracellular urate taken up via OAT1 and/or OAT3 from the blood exits from the cell into the lumen via hNPT4. ..
  21. Ciarimboli G. Role of organic cation transporters in drug-induced toxicity. Expert Opin Drug Metab Toxicol. 2011;7:159-74 pubmed publisher
    ..Defining the pharmacogenomics of these transporters will be essential to personalized medicine, enabling physicians to choose drugs for patients based on efficacy, availability, cost, safety, tolerability and convenience. ..
  22. Shin H, Takeda M, Enomoto A, Fujimura M, Miyazaki H, Anzai N, et al. Interactions of urate transporter URAT1 in human kidney with uricosuric drugs. Nephrology (Carlton). 2011;16:156-62 pubmed publisher
    ..In addition, a cell line that stably expressing URAT1 could be a useful tool for the development of uricosuric drugs. ..
  23. Sakata T, Anzai N, Kimura T, Miura D, Fukutomi T, Takeda M, et al. Functional analysis of human organic cation transporter OCT3 (SLC22A3) polymorphisms. J Pharmacol Sci. 2010;113:263-6 pubmed
  24. D Argenio G, Petillo O, Margarucci S, Torpedine A, Calarco A, Koverech A, et al. Colon OCTN2 gene expression is up-regulated by peroxisome proliferator-activated receptor gamma in humans and mice and contributes to local and systemic carnitine homeostasis. J Biol Chem. 2010;285:27078-87 pubmed publisher
    ..This study reveals a PPARgamma-dependent absorption machinery in colon that is likely involved in the health of colon epithelium, in the microbiota-host interactions and in the absorption of nutraceuticals and drugs. ..
  25. Wempe M, Jutabha P, Quade B, Iwen T, Frick M, Ross I, et al. Developing potent human uric acid transporter 1 (hURAT1) inhibitors. J Med Chem. 2011;54:2701-13 pubmed publisher
    ..Compounds with submicromolar (i.e., IC(50) < 1000 nM) inhibitors were prepared by brominating the corresponding phenols to produce compounds with potent uricosuric activity. ..
  26. Yonezawa A, Inui K. Importance of the multidrug and toxin extrusion MATE/SLC47A family to pharmacokinetics, pharmacodynamics/toxicodynamics and pharmacogenomics. Br J Pharmacol. 2011;164:1817-25 pubmed publisher
    ..In this review, we summarize recent findings on MATE1/SLC47A1 and MATE2-K/SLC47A2 and discuss the importance of these transporters to the pharmacokinetics, pharmacodynamics/toxicodynamics and pharmacogenomics of cationic drugs. ..
  27. Jong N, Nakanishi T, Liu J, Tamai I, McKeage M. Oxaliplatin transport mediated by organic cation/carnitine transporters OCTN1 and OCTN2 in overexpressing human embryonic kidney 293 cells and rat dorsal root ganglion neurons. J Pharmacol Exp Ther. 2011;338:537-47 pubmed publisher
    ..OCTN1-mediated transport of oxaliplatin appears to contribute to its neuronal accumulation and treatment-limiting neurotoxicity more so than OCTN2 or OCTs. ..
  28. Scalise M, Galluccio M, Accardi R, Cornet I, Tommasino M, Indiveri C. Human OCTN2 (SLC22A5) is down-regulated in virus- and nonvirus-mediated cancer. Cell Biochem Funct. 2012;30:419-25 pubmed publisher
    ..These data demonstrate for the first time that the OCTN2 transporter is generally down-regulated in virus and nonvirus-mediated epithelial cancers, probably via methylation of its promoter region. ..
  29. Schlegel G, Keller J, Hirche F, Geissler S, Schwarz F, Ringseis R, et al. Expression of genes involved in hepatic carnitine synthesis and uptake in dairy cows in the transition period and at different stages of lactation. BMC Vet Res. 2012;8:28 pubmed publisher
  30. Zhang J, Zhou W. Ameliorative effects of SLC22A2 gene polymorphism 808 G/T and cimetidine on cisplatin-induced nephrotoxicity in Chinese cancer patients. Food Chem Toxicol. 2012;50:2289-93 pubmed publisher
    ..007). These results suggested that SLC22A2 gene polymorphism 808 G/T and cimetidine could attenuate cisplatin nephrotoxicity in Chinese cancer patients. But the renoprotection mechanism of cimetidine might be damaged by the mutation. ..
  31. Scalise M, Galluccio M, Pochini L, Indiveri C. Over-expression in Escherichia coli, purification and reconstitution in liposomes of the third member of the OCTN sub-family: the mouse carnitine transporter OCTN3. Biochem Biophys Res Commun. 2012;422:59-63 pubmed publisher
    ..3)H]carnitine transport was inhibited by carnitine analogues and some Cys and NH(2) reagents. This paper represents the first outcome in over-expressing, in active form, the third member of the OCTN sub-family, mOCTN3, in E. coli. ..
  32. Yoon Y, Lee D, Ki C, Lee S, Kim J, Lee Y, et al. SLC22A5 mutations in a patient with systemic primary carnitine deficiency: the first Korean case confirmed by biochemical and molecular investigation. Ann Clin Lab Sci. 2012;42:424-8 pubmed
    ..The plasma free carnitine level normalized to 66.6 ?mol/L at 4 weeks after treatment. To the best of our knowledge, this is the first report of a CDSP patient confirmed by molecular genetic investigation. ..
  33. Zhang Y, Csanaky I, Lehman McKeeman L, Klaassen C. Loss of organic anion transporting polypeptide 1a1 increases deoxycholic acid absorption in mice by increasing intestinal permeability. Toxicol Sci. 2011;124:251-60 pubmed publisher
    ..Taken together, the current data suggest that Oatp1a1 does not mediate the hepatic uptake of DCA or TDCA, but lack of Oatp1a1 increases intestinal permeability and thus enhances the absorption of DCA in mice. ..
  34. Martini M, Ferrara A, Giachelia M, Panieri E, Siminovitch K, Galeotti T, et al. Association of the OCTN1/1672T variant with increased risk for colorectal cancer in young individuals and ulcerative colitis patients. Inflamm Bowel Dis. 2012;18:439-48 pubmed publisher
    ..Our data demonstrate that OCTN1 could have a role in modulating the severity of chronic inflammation associated with SCC in early age and in UC patients, and that its polymorphisms may help to predict malignant progression of IBD. ..
  35. Yonezawa A, Inui K. Organic cation transporter OCT/SLC22A and H(+)/organic cation antiporter MATE/SLC47A are key molecules for nephrotoxicity of platinum agents. Biochem Pharmacol. 2011;81:563-8 pubmed publisher
  36. Konig J, Zolk O, Singer K, Hoffmann C, Fromm M. Double-transfected MDCK cells expressing human OCT1/MATE1 or OCT2/MATE1: determinants of uptake and transcellular translocation of organic cations. Br J Pharmacol. 2011;163:546-55 pubmed publisher
    ..0 to 7.5. Our data demonstrate functional interplay between OCT1/OCT2-mediated uptake and efflux by MATE1. Moreover, MATE1 function in human kidney might be modified by changes in luminal pH values. ..
  37. Mazzini M, Tadros T, Siwik D, Joseph L, Bristow M, Qin F, et al. Primary carnitine deficiency and sudden death: in vivo evidence of myocardial lipid peroxidation and sulfonylation of sarcoendoplasmic reticulum calcium ATPase 2. Cardiology. 2011;120:52-8 pubmed publisher
    ..These findings suggest that increased oxidant stress may contribute to myocardial dysfunction and arrhythmogenesis in this disorder. ..
  38. Tabara Y, Kohara K, Kawamoto R, Hiura Y, Nishimura K, Morisaki T, et al. Association of four genetic loci with uric acid levels and reduced renal function: the J-SHIPP Suita study. Am J Nephrol. 2010;32:279-86 pubmed publisher
    ..We also identified a common nonsense mutation, W258X, responsible for renal hypouricemia. Here, we investigated clinical implications of these genetic variants by cross-sectional and longitudinal genetic epidemiological analysis...
  39. Wright A, Rudan I, Hastie N, Campbell H. A 'complexity' of urate transporters. Kidney Int. 2010;78:446-52 pubmed publisher
  40. Wempe M, Quade B, Jutabha P, Iwen T, Frick M, Rice P, et al. Human uric acid transporter 1 (hURAT1): an inhibitor structure-activity relationship (SAR) study. Nucleosides Nucleotides Nucleic Acids. 2011;30:1312-23 pubmed publisher
    ..e., urate) or inhibitor. We discuss the inhibitor structure-activity relationship and how electronically donating or withdrawing groups attached to the B-ring can decrease or increase inhibitory potency, respectively. ..
  41. Luci S, Geissler S, König B, Koch A, Stangl G, Hirche F, et al. PPARalpha agonists up-regulate organic cation transporters in rat liver cells. Biochem Biophys Res Commun. 2006;350:704-8 pubmed
    ..We conclude that PPARalpha agonists increase carnitine concentrations in livers of rats and cells by an increased uptake of carnitine into the cell but not by an increased carnitine biosynthesis. ..
  42. Filipski K, Loos W, Verweij J, Sparreboom A. Interaction of Cisplatin with the human organic cation transporter 2. Clin Cancer Res. 2008;14:3875-80 pubmed publisher
    ..However, known variants in SLC22A2 do not substantially contribute to explaining interindividual pharmacokinetic variability, suggesting that other mechanisms, controlling OCT2 expression, might be involved. ..
  43. Shikata E, Yamamoto R, Takane H, Shigemasa C, Ikeda T, Otsubo K, et al. Human organic cation transporter (OCT1 and OCT2) gene polymorphisms and therapeutic effects of metformin. J Hum Genet. 2007;52:117-22 pubmed
    ..In this study it is suggested that OCT1 and OCT2 gene polymorphisms have little contribution to the clinical efficacy of metformin. ..
  44. Keller T, Schwarz D, Bernhard F, Dötsch V, Hunte C, Gorboulev V, et al. Cell free expression and functional reconstitution of eukaryotic drug transporters. Biochemistry. 2008;47:4552-64 pubmed publisher
    ..The V max of PAH (-)/KG (2-) antiport was increased by Cl (-) in a manner independent of gradients, and PAH (-)/KG (2-) antiport was independent of membrane potential in the absence or presence of Cl (-). ..
  45. Luci S, Hirche F, Eder K. Fasting and caloric restriction increases mRNA concentrations of novel organic cation transporter-2 and carnitine concentrations in rat tissues. Ann Nutr Metab. 2008;52:58-67 pubmed publisher
    ..Increased tissue carnitine concentrations in fasted and calorie-restricted rats might be at least in part due to increased uptake of carnitine by OCTN2. ..
  46. Cabrito T, Teixeira M, Duarte A, Duque P, Sá Correia I. Heterologous expression of a Tpo1 homolog from Arabidopsis thaliana confers resistance to the herbicide 2,4-D and other chemical stresses in yeast. Appl Microbiol Biotechnol. 2009;84:927-36 pubmed publisher
    ..Heterologous expression of At5g13750 in yeast also leads to increased resistance to indole-3-acetic acid (IAA), Al(3+) and Tl(3+). At5g13750 is the first plant putative MFS transporter to be suggested as possibly involved in MDR. ..
  47. Eder K, Ringseis R. The role of peroxisome proliferator-activated receptor alpha in transcriptional regulation of novel organic cation transporters. Eur J Pharmacol. 2010;628:1-5 pubmed publisher
  48. Ohta K, Inoue K, Yasujima T, Ishimaru M, Yuasa H. Functional characteristics of two human MATE transporters: kinetics of cimetidine transport and profiles of inhibition by various compounds. J Pharm Pharm Sci. 2009;12:388-96 pubmed
    ..Cimetidine was demonstrated to be a high affinity substrate of both hMATEs. Subsequent evaluation of the inhibition of hMATEs by various compounds indicated no major difference in function or role between hMATE1 and hMATE2-K. ..
  49. Maeda T, Wakasawa T, Funabashi M, Fukushi A, Fujita M, Motojima K, et al. Regulation of Octn2 transporter (SLC22A5) by peroxisome proliferator activated receptor alpha. Biol Pharm Bull. 2008;31:1230-6 pubmed
    ..In conclusion, our results indicate that the nuclear receptor PPARalpha directly up-regulates the expression of rOctn2 and increases the hepatic uptake of carnitine via rOctn2. ..
  50. Anzai N, Ichida K, Jutabha P, Kimura T, Babu E, Jin C, et al. Plasma urate level is directly regulated by a voltage-driven urate efflux transporter URATv1 (SLC2A9) in humans. J Biol Chem. 2008;283:26834-8 pubmed publisher
  51. Nagano T, Mitchell J, Sanz L, Pauler F, Ferguson Smith A, Feil R, et al. The Air noncoding RNA epigenetically silences transcription by targeting G9a to chromatin. Science. 2008;322:1717-20 pubmed publisher
    ..Our results suggest that Air, and potentially other large ncRNAs, target repressive histone-modifying activities through molecular interaction with specific chromatin domains to epigenetically silence transcription. ..
  52. Inazu T. A case of renal hypouricemia caused by urate transporter 1 gene mutations. Clin Nephrol. 2006;65:370-3 pubmed
    ..Restriction enzyme analysis with HphI was useful to screen the IVS2+1G>A mutation in hURAT1 gene. ..
  53. Hamada T, Ichida K, Hosoyamada M, Mizuta E, Yanagihara K, Sonoyama K, et al. Uricosuric action of losartan via the inhibition of urate transporter 1 (URAT 1) in hypertensive patients. Am J Hypertens. 2008;21:1157-62 pubmed publisher
    ..These findings suggested that losartan inhibited URAT1 and thereby it lowered Sur levels in hypertensive patients. ..
  54. Yokoo S, Masuda S, Yonezawa A, Terada T, Katsura T, Inui K. Significance of organic cation transporter 3 (SLC22A3) expression for the cytotoxic effect of oxaliplatin in colorectal cancer. Drug Metab Dispos. 2008;36:2299-306 pubmed publisher
    ..In conclusion, the hOCT3-mediated uptake of oxaliplatin into the cancers was suggested to be important for its cytotoxicity, and hOCT3 expression may be a marker for cancer chemotherapy including oxaliplatin. ..
  55. Komatsuda A, Iwamoto K, Wakui H, Sawada K, Yamaguchi A. Analysis of mutations in the urate transporter 1 (URAT1) gene of Japanese patients with hypouricemia in northern Japan and review of the literature. Ren Fail. 2006;28:223-7 pubmed
    ..Our study suggests that there is no regional different distribution of the URAT1 genetic mutations in Japanese with renal hypouricemia. ..
  56. Ohnishi S, Okamura N, Sakamoto S, Hasegawa H, Norikura R, Kanaoka E, et al. Role of Na+/L-carnitine transporter (OCTN2) in renal handling of pivaloylcarnitine and valproylcarnitine formed during pivalic acid-containing prodrugs and valproic acid treatment. Drug Metab Pharmacokinet. 2008;23:293-303 pubmed
    ..These results suggest that low renal reabsorption and interaction of hOCTN2 for these acylcarnitines might possibly affect the decrease of L-carnitine concentration in humans. ..
  57. Terada T, Inui K. Gene expression and regulation of drug transporters in the intestine and kidney. Biochem Pharmacol. 2007;73:440-9 pubmed
    ..The purpose of this research updates is to review the recent progress in the study of the gene expression and regulation of intestinal and renal drug transporters. ..
  58. Ali A, Bajaj V, Gopinath K, Kumar A. Characterization of the human SLC22A18 gene promoter and its regulation by the transcription factor Sp1. Gene. 2009;429:37-43 pubmed publisher
    ..A COBRA-based assay has been developed to look for promoter methylation in different cancers. The present data will help to understand the regulation of this gene and its role in tumorigenesis. ..
  59. Zolk O, Solbach T, Konig J, Fromm M. Structural determinants of inhibitor interaction with the human organic cation transporter OCT2 (SLC22A2). Naunyn Schmiedebergs Arch Pharmacol. 2009;379:337-48 pubmed publisher
    ..0 A. Taken together, our data identify structural determinants for inhibitor interactions with OCT2. ..
  60. Wang T, Li J, Chen F, Zhao Y, He X, Wan D, et al. Choline transporters in human lung adenocarcinoma: expression and functional implications. Acta Biochim Biophys Sin (Shanghai). 2007;39:668-74 pubmed
  61. Omote H, Hiasa M, Matsumoto T, Otsuka M, Moriyama Y. The MATE proteins as fundamental transporters of metabolic and xenobiotic organic cations. Trends Pharmacol Sci. 2006;27:587-93 pubmed
    ..Thus, we propose that members of the MATE family are organic cation exporters that excrete metabolic or xenobiotic organic cations from the body. ..
  62. Meyer zu Schwabedissen H, Verstuyft C, Kroemer H, Becquemont L, Kim R. Human multidrug and toxin extrusion 1 (MATE1/SLC47A1) transporter: functional characterization, interaction with OCT2 (SLC22A2), and single nucleotide polymorphisms. Am J Physiol Renal Physiol. 2010;298:F997-F1005 pubmed publisher
  63. Tzovaras V, Chatzikyriakidou A, Bairaktari E, Liberopoulos E, Georgiou I, Elisaf M. Absence of SLC22A12 gene mutations in Greek Caucasian patients with primary renal hypouricaemia. Scand J Clin Lab Invest. 2007;67:589-95 pubmed
    ..No mutation was found--only the previously reported silent polymorphism 1246T > C (His 42His) in exon 2 of the SLC22A12 gene. No previously reported mutation of URAT1 was associated with primary renal hypouricaemia in Greek subjects. ..
  64. Nies A, Koepsell H, Winter S, Burk O, Klein K, Kerb R, et al. Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver. Hepatology. 2009;50:1227-40 pubmed publisher
    ..0001), and four variants in OCT3 (rs2292334, rs2048327, rs1810126, rs3088442) were associated with reduced OCT3 mRNA levels (P = 0.03)...
  65. Machová E, O Regan S, Newcombe J, Meunier F, Prentice J, Dove R, et al. Detection of choline transporter-like 1 protein CTL1 in neuroblastoma x glioma cells and in the CNS, and its role in choline uptake. J Neurochem. 2009;110:1297-309 pubmed publisher
  66. Shnitsar V, Eckardt R, Gupta S, Grottker J, Müller G, Koepsell H, et al. Expression of human organic cation transporter 3 in kidney carcinoma cell lines increases chemosensitivity to melphalan, irinotecan, and vincristine. Cancer Res. 2009;69:1494-501 pubmed publisher
    ..Thus, our data support the hypothesis that the sensitivity of tumor cells to chemotherapeutic treatment depends on the expression of transporter proteins mediating specific drug accumulation into target cells. ..
  67. Kitada N, Takara K, Minegaki T, Itoh C, Tsujimoto M, Sakaeda T, et al. Factors affecting sensitivity to antitumor platinum derivatives of human colorectal tumor cell lines. Cancer Chemother Pharmacol. 2008;62:577-84 pubmed
    ..Some factors affecting the sensitivity of tumor cells to platinum derivatives were proposed, and will provide useful information for cancer chemotherapy with platinum derivatives. ..