organic anion transporters


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

Top Publications

  1. Hollis Moffatt J, Phipps Green A, Chapman B, Jones G, Van Rij A, Gow P, et al. The renal urate transporter SLC17A1 locus: confirmation of association with gout. Arthritis Res Ther. 2012;14:R92 pubmed publisher
    ..70, P = 3.0 × 10-8). Haplotype analysis suggested the presence of a common protective haplotype. We confirm the SLC17A1 locus as the third associated with gout at a genome-wide level of significance. ..
  2. Li N, Hong W, Huang H, Lu H, Lin G, Hong M. Identification of amino acids essential for estrone-3-sulfate transport within transmembrane domain 2 of organic anion transporting polypeptide 1B1. PLoS ONE. 2012;7:e36647 pubmed publisher
  3. Roth M, Obaidat A, Hagenbuch B. OATPs, OATs and OCTs: the organic anion and cation transporters of the SLCO and SLC22A gene superfamilies. Br J Pharmacol. 2012;165:1260-87 pubmed publisher
    ..SLCO (formerly SLC21A) consists of organic anion transporting polypeptides (OATPs), while the organic anion transporters (OATs) and the organic cation transporters (OCTs) are classified in the SLC22A superfamily...
  4. Hagos Y, Wolff N. Assessment of the role of renal organic anion transporters in drug-induced nephrotoxicity. Toxins (Basel). 2010;2:2055-82 pubmed publisher
    In the present review we have attempted to assess the involvement of the organic anion transporters OAT1, OAT2, OAT3, and OAT4, belonging to the SLC22 family of polyspecific carriers, in drug-induced renal damage in humans...
  5. Fenner K, Jones H, Ullah M, Kempshall S, Dickins M, Lai Y, et al. The evolution of the OATP hepatic uptake transport protein family in DMPK sciences: from obscure liver transporters to key determinants of hepatobiliary clearance. Xenobiotica. 2012;42:28-45 pubmed publisher
  6. Iusuf D, van de Steeg E, Schinkel A. Functions of OATP1A and 1B transporters in vivo: insights from mouse models. Trends Pharmacol Sci. 2012;33:100-8 pubmed publisher
  7. Sortica V, Ojopi E, Genro J, Callegari Jacques S, Ribeiro dos Santos A, de Moraes M, et al. Influence of genomic ancestry on the distribution of SLCO1B1, SLCO1B3 and ABCB1 gene polymorphisms among Brazilians. Basic Clin Pharmacol Toxicol. 2012;110:460-8 pubmed publisher
  8. Ramsey L, Bruun G, Yang W, Treviño L, Vattathil S, Scheet P, et al. Rare versus common variants in pharmacogenetics: SLCO1B1 variation and methotrexate disposition. Genome Res. 2012;22:1-8 pubmed publisher
    ..8% of SLCO1B1's effects (1.9% of total variation) and had larger effect sizes than common NS variants. Our results show that rare variants are likely to have an important effect on pharmacogenetic phenotypes. ..
  9. Jin L, Kikuchi R, Saji T, Kusuhara H, Sugiyama Y. Regulation of tissue-specific expression of renal organic anion transporters by hepatocyte nuclear factor 1 ?/? and DNA methylation. J Pharmacol Exp Ther. 2012;340:648-55 pubmed publisher was aimed at investigating the role of this cascade in the transcriptional regulation of renal organic anion transporters (OATs) yet to be characterized in human and mouse...

More Information


  1. Nakanishi T, Tamai I. Genetic polymorphisms of OATP transporters and their impact on intestinal absorption and hepatic disposition of drugs. Drug Metab Pharmacokinet. 2012;27:106-21 pubmed
  2. Kikuchi A, Arai Ichinoi N, Sakamoto O, Matsubara Y, Saheki T, Kobayashi K, et al. Simple and rapid genetic testing for citrin deficiency by screening 11 prevalent mutations in SLC25A13. Mol Genet Metab. 2012;105:553-8 pubmed publisher
    ..Therefore, this assay could be used for newborn screening and for facilitating the genetic diagnosis of citrin deficiency, especially in East Asian populations...
  3. DeGorter M, Ho R, Leake B, Tirona R, Kim R. Interaction of three regiospecific amino acid residues is required for OATP1B1 gain of OATP1B3 substrate specificity. Mol Pharm. 2012;9:986-95 pubmed publisher
    ..Accordingly, our data provide new insight into the molecular determinants of the substrate specificity of these hepatic uptake transporters with relevance to targeted drug design and prediction of drug-drug interactions. ..
  4. Makino T, Okajima K, Uebayashi R, Ohtake N, Inoue K, Mizukami H. 3-Monoglucuronyl-glycyrrhretinic acid is a substrate of organic anion transporters expressed in tubular epithelial cells and plays important roles in licorice-induced pseudoaldosteronism by inhibiting 11?-hydroxysteroid dehydrogenase 2. J Pharmacol Exp Ther. 2012;342:297-304 pubmed publisher
    ..Because the plasma level of 3MGA depends on the function of hepatic transporters, monitoring 3MGA levels in plasma or urine may be useful for preventing pseudoaldosteronism when licorice or GL is prescribed to patients. ..
  5. Wilke R, Ramsey L, Johnson S, Maxwell W, McLeod H, Voora D, et al. The clinical pharmacogenomics implementation consortium: CPIC guideline for SLCO1B1 and simvastatin-induced myopathy. Clin Pharmacol Ther. 2012;92:112-7 pubmed publisher
    ..This guideline explores the relationship between rs4149056 (c.521T>C, p.V174A) and clinical outcome for all statins. The strength of the evidence is high for myopathy with simvastatin. We limit our recommendations accordingly...
  6. de Graan A, Lancaster C, Obaidat A, Hagenbuch B, Elens L, Friberg L, et al. Influence of polymorphic OATP1B-type carriers on the disposition of docetaxel. Clin Cancer Res. 2012;18:4433-40 pubmed
    ..In view of the established exposure-toxicity relationships for docetaxel, we suggest that caution is warranted if docetaxel has to be administered together with agents that potently inhibit both OATP1B1 and OATP1B3. ..
  7. Engel A, Oswald S, Siegmund W, Keiser M. Pharmaceutical excipients influence the function of human uptake transporting proteins. Mol Pharm. 2012;9:2577-81 pubmed publisher
    ..However, the clinical relevance of these findings needs to be evaluated in further in vivo studies. ..
  8. Lancaster C, Bruun G, Peer C, Mikkelsen T, Corydon T, Gibson A, et al. OATP1B1 polymorphism as a determinant of erythromycin disposition. Clin Pharmacol Ther. 2012;92:642-50 pubmed publisher
    ..0072). These results suggest that impairment of OATP1B1 function can alter erythromycin metabolism, independent of changes in CYP3A4 activity. ..
  9. Wang L, Sweet D. Renal organic anion transporters (SLC22 family): expression, regulation, roles in toxicity, and impact on injury and disease. AAPS J. 2013;15:53-69 pubmed publisher
    ..Examples establishing a role for renal OATs in drug clearance, food/drug-drug interactions, and renal injury and pathology are presented. An update of the current information regarding the regulation of OAT expression is also provided. ..
  10. Tapaninen T, Karonen T, Backman J, Neuvonen P, Niemi M. SLCO2B1 c.935G>A single nucleotide polymorphism has no effect on the pharmacokinetics of montelukast and aliskiren. Pharmacogenet Genomics. 2013;23:19-24 pubmed publisher
    ..935GG genotype were 0.98 (0.74, 1.30) or 1.24 (0.85, 1.80), respectively (P=0.576). These data do not support the suggested functional significance of the SLCO2B1 c.935G>A SNP on OATP2B1 activity in vivo. ..
  11. Hagenbuch B, Stieger B. The SLCO (former SLC21) superfamily of transporters. Mol Aspects Med. 2013;34:396-412 pubmed publisher
  12. Alencastro de Azevedo L, Reverbel da Silveira T, Carvalho C, Martins de Castro S, Giugliani R, Matte U. UGT1A1, SLCO1B1, and SLCO1B3 polymorphisms vs. neonatal hyperbilirubinemia: is there an association?. Pediatr Res. 2012;72:169-73 pubmed
    ..Although genetic variation accounts for a good part of this condition, the association between different polymorphisms and environmental factors has yet to be explained. ..
  13. Emami Riedmaier A, Nies A, Schaeffeler E, Schwab M. Organic anion transporters and their implications in pharmacotherapy. Pharmacol Rev. 2012;64:421-49 pubmed publisher
    b>Organic anion transporters play an essential role in the distribution and excretion of numerous endogenous metabolic products and exogenous organic anions, including a host of widely prescribed drugs...
  14. Burckhardt G. Drug transport by Organic Anion Transporters (OATs). Pharmacol Ther. 2012;136:106-30 pubmed publisher
    Common to all so far functionally characterized Organic Anion Transporters (OATs) is their broad substrate specificity and their ability to exchange extracellular against intracellular organic anions...
  15. Wang L, Sweet D. Potential for food-drug interactions by dietary phenolic acids on human organic anion transporters 1 (SLC22A6), 3 (SLC22A8), and 4 (SLC22A11). Biochem Pharmacol. 2012;84:1088-95 pubmed publisher
  16. 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. ..
  17. van de Steeg E, van Esch A, Wagenaar E, Kenworthy K, Schinkel A. Influence of human OATP1B1, OATP1B3, and OATP1A2 on the pharmacokinetics of methotrexate and paclitaxel in humanized transgenic mice. Clin Cancer Res. 2013;19:821-32 pubmed publisher
    ..Humanized transgenic OATP1A/1B mice will provide excellent tools to further study these aspects in vivo for many (anticancer) drugs. ..
  18. Zimmerman E, Hu S, Roberts J, Gibson A, Orwick S, Li L, et al. Contribution of OATP1B1 and OATP1B3 to the disposition of sorafenib and sorafenib-glucuronide. Clin Cancer Res. 2013;19:1458-66 pubmed publisher
    ..These findings signify a unique role for OATP1B1 and OATP1B3 in the elimination of sorafenib-glucuronide and suggest a role for these transporters in the in vivo handling of glucuronic acid conjugates of drugs. ..
  19. Huang J, Li N, Hong W, Zhan K, Yu X, Huang H, et al. Conserved tryptophan residues within putative transmembrane domain 6 affect transport function of organic anion transporting polypeptide 1B1. Mol Pharmacol. 2013;84:521-7 pubmed publisher
    ..Our results suggest that Trp258 and Trp259 may play different roles in the uptake of different substrates by OATP1B1. ..
  20. de Graaf W, Häusler S, Heger M, van Ginhoven T, van Cappellen G, Bennink R, et al. Transporters involved in the hepatic uptake of (99m)Tc-mebrofenin and indocyanine green. J Hepatol. 2011;54:738-45 pubmed publisher
    ..The transporter specificity of (99m)Tc-mebrofenin and ICG partially overlaps as both compounds are transported by OATP1B3. (99m)Tc-mebrofenin is also taken up by OATP1B1, whereas ICG is additionally transported by NTCP. ..
  21. Xiang X, Han Y, Neuvonen M, Pasanen M, Kalliokoski A, Backman J, et al. Effect of SLCO1B1 polymorphism on the plasma concentrations of bile acids and bile acid synthesis marker in humans. Pharmacogenet Genomics. 2009;19:447-57 pubmed publisher
    ..05). SLCO1B1 polymorphism considerably affects the disposition of several endogenous bile acids and bile acid synthesis marker, indicating that OATP1B1 plays an important role in the hepatic uptake of bile acids in vivo in humans. ..
  22. 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
  23. Innocenti F, Kroetz D, Schuetz E, Dolan M, Ramirez J, Relling M, et al. Comprehensive pharmacogenetic analysis of irinotecan neutropenia and pharmacokinetics. J Clin Oncol. 2009;27:2604-14 pubmed publisher
    ..On the basis of this exploratory analysis, common polymorphisms in genes encoding for ABC and SLC transporters may have a significant impact on the pharmacokinetics and pharmacodynamics of CPT-11. Confirmatory studies are required. ..
  24. Sai K, Saito Y, Maekawa K, Kim S, Kaniwa N, Nishimaki Mogami T, et al. Additive effects of drug transporter genetic polymorphisms on irinotecan pharmacokinetics/pharmacodynamics in Japanese cancer patients. Cancer Chemother Pharmacol. 2010;66:95-105 pubmed publisher
    ..Certain transporter genotypes additively increased irinotecan-induced neutropenia, but their clinical importance should be further elucidated. ..
  25. Uwai Y, Iwamoto K. Transport of aminopterin by human organic anion transporters hOAT1 and hOAT3: Comparison with methotrexate. Drug Metab Pharmacokinet. 2010;25:163-9 pubmed
    The transport of antifolate aminopterin by human organic anion transporters hOAT1 (SLC22A6) and hOAT3 (SLC22A8) was characterized using Xenopus laevis oocytes and was compared with that of methotrexate...
  26. Laitinen A, Niemi M. Frequencies of single-nucleotide polymorphisms of SLCO1A2, SLCO1B3 and SLCO2B1 genes in a Finnish population. Basic Clin Pharmacol Toxicol. 2011;108:9-13 pubmed publisher
    ..99, D'?=?1.00), all other SNP pairs showed only a weak correlation. In conclusion, non-synonymous sequence variations of SLCO1A2, SLCO1B3 and SLCO2B1 occur at high frequencies in the Finnish population. ..
  27. Leuthold S, Hagenbuch B, Mohebbi N, Wagner C, Meier P, Stieger B. Mechanisms of pH-gradient driven transport mediated by organic anion polypeptide transporters. Am J Physiol Cell Physiol. 2009;296:C570-82 pubmed publisher
  28. Shirasaka Y, Kuraoka E, Spahn Langguth H, Nakanishi T, Langguth P, Tamai I. Species difference in the effect of grapefruit juice on intestinal absorption of talinolol between human and rat. J Pharmacol Exp Ther. 2010;332:181-9 pubmed publisher
  29. Karlgren M, Ahlin G, Bergström C, Svensson R, Palm J, Artursson P. In vitro and in silico strategies to identify OATP1B1 inhibitors and predict clinical drug-drug interactions. Pharm Res. 2012;29:411-26 pubmed publisher
    ..Twenty-two new OATP1B1 inhibitors were identified, a predictive OATP1B1 inhibition in silico model was developed, and successful predictions of clinical DDIs were obtained with OATP1B1. ..
  30. Gui C, Hagenbuch B. Amino acid residues in transmembrane domain 10 of organic anion transporting polypeptide 1B3 are critical for cholecystokinin octapeptide transport. Biochemistry. 2008;47:9090-7 pubmed publisher
    ..In conclusion, we have identified three amino acid residues (Y537, S545, and T550) in TM10 of OATP1B3 that are important for CCK-8 transport. ..
  31. Mougey E, Feng H, Castro M, Irvin C, Lima J. Absorption of montelukast is transporter mediated: a common variant of OATP2B1 is associated with reduced plasma concentrations and poor response. Pharmacogenet Genomics. 2009;19:129-38 pubmed publisher
    ..02+/-0.01, P=1.0; c.[935G]+[935G]=1.0+/-0.3, P<0.0001). Altogether, these observations suggest that the genetics of SLCO2B1 may be an important variable in determining the pharmacokinetics and the pharmacodynamics of montelukast. ..
  32. 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. ..
  33. Shiraya K, Hirata T, Hatano R, Nagamori S, Wiriyasermkul P, Jutabha P, et al. A novel transporter of SLC22 family specifically transports prostaglandins and co-localizes with 15-hydroxyprostaglandin dehydrogenase in renal proximal tubules. J Biol Chem. 2010;285:22141-51 pubmed publisher
    ..By removing extracellular PGE(2), OAT-PG is proposed to be involved in the local PGE(2) clearance and metabolism for the inactivation of PG signals in the kidney cortex. ..
  34. 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. ..
  35. Huppertz A, Breuer J, Fels L, Schultze Mosgau M, Sutter G, Klein S, et al. Evaluation of possible drug-drug interaction between gadoxetic acid and erythromycin as an inhibitor of organic anion transporting peptides (OATP). J Magn Reson Imaging. 2011;33:409-16 pubmed publisher
    ..6 (SD 17.9%) after placebo. Ratio of relative enhancements was 0.951 (95% confidence interval, 0.833; 1.061; statistically not significant). Coadministration of erythromycin has no effect on gadoxetic acid enhanced liver MR imaging. ..
  36. Takane H, Kawamoto K, Sasaki T, Moriki K, Moriki K, Kitano H, et al. Life-threatening toxicities in a patient with UGT1A1*6/*28 and SLCO1B1*15/*15 genotypes after irinotecan-based chemotherapy. Cancer Chemother Pharmacol. 2009;63:1165-9 pubmed publisher
    ..The severe toxicities in this patient are attributable to the extensive accumulation of SN-38, which may result from a synergistic or additive effect of low metabolic (UGT1A1*6/*28) and transport (SLCO1B1*15/*15) capabilities. ..
  37. Ahn S, Nigam S. Toward a systems level understanding of organic anion and other multispecific drug transporters: a remote sensing and signaling hypothesis. Mol Pharmacol. 2009;76:481-90 pubmed publisher
    b>Organic anion transporters (Oats) are located in the barrier epithelia of diverse organs, where they mediate the absorption and excretion of a wide range of metabolites, signaling molecules, and xenobiotics...
  38. Lin R, Wang X, Wang Y, Zhang F, Wang Y, Fu W, et al. Association of polymorphisms in four bilirubin metabolism genes with serum bilirubin in three Asian populations. Hum Mutat. 2009;30:609-15 pubmed publisher
    ..Finally, we observed that significant differences of TBIL levels existed among the three populations; however, this could not be completely explained by the differences at the (TA)n repeat polymorphism and SNP rs4148323:G>A. ..
  39. Jindal C, Kumar S, Choudhari G, Goel H, Mittal B. Organic anion transporter protein (OATP1B1) encoded by SLCO1B1 gene polymorphism (388A>G) & susceptibility in gallstone disease. Indian J Med Res. 2009;129:170-5 pubmed
    ..Although the prevalence of SLCO1B1 gene 388A>G polymorphism in north Indian population in high, yet this polymorphism does not appear to play a significant role in susceptibility to gallstone formation. ..
  40. Gui C, Hagenbuch B. Role of transmembrane domain 10 for the function of organic anion transporting polypeptide 1B1. Protein Sci. 2009;18:2298-306 pubmed publisher
    ..In conclusion, our results show that TM10 is critical for the function of OATP1B1. ..
  41. VanWert A, Gionfriddo M, Sweet D. Organic anion transporters: discovery, pharmacology, regulation and roles in pathophysiology. Biopharm Drug Dispos. 2010;31:1-71 pubmed publisher
    ..Many drugs bear anionic functional groups, and thus interact with organic anion transporters (OATs). Collectively, these transporters are nearly ubiquitously expressed in barrier epithelia...
  42. Saito H. Pathophysiological regulation of renal SLC22A organic ion transporters in acute kidney injury: pharmacological and toxicological implications. Pharmacol Ther. 2010;125:79-91 pubmed publisher
    ..Such analysis will provide a better understanding of the pathophysiological implications of SLC22A transporters. ..
  43. Picard N, Yee S, Woillard J, Lebranchu Y, Le Meur Y, Giacomini K, et al. The role of organic anion-transporting polypeptides and their common genetic variants in mycophenolic acid pharmacokinetics. Clin Pharmacol Ther. 2010;87:100-8 pubmed publisher
    ..Further studies demonstrated that this variant of OATP1B3 exhibited a reduced maximal velocity (V(max)) in transfected HEK cells, thereby providing functional evidence to support our clinical findings. ..
  44. Watchko J, Lin Z. Exploring the genetic architecture of neonatal hyperbilirubinemia. Semin Fetal Neonatal Med. 2010;15:169-75 pubmed publisher
    ..Variant gene co-expression including compound and synergistic heterozygosity enhances hyperbilirubinemia risk, contributing to the etiologic heterogeneity and complex nature of neonatal jaundice. ..
  45. Johnson A, Kavousi M, Smith A, Chen M, Dehghan A, Aspelund T, et al. Genome-wide association meta-analysis for total serum bilirubin levels. Hum Mol Genet. 2009;18:2700-10 pubmed publisher
    ..In analyses for association with gallbladder disease or gallstones, top bilirubin SNPs in UGT1A1 and SLCO1B1 were not associated. ..
  46. Bahat H, Dinour D, Ganon L, Feldman L, Holtzman E, Goldman M. Non-urate transporter 1-related renal hypouricemia and acute renal failure in an Israeli-Arab family. Pediatr Nephrol. 2009;24:999-1003 pubmed publisher
    ..A non-URAT1 genetic defect that causes decreased reabsorption or, more probably, increased secretion of uric acid, induces IRHU. Further studies are required in order to elucidate the genetic defect. ..
  47. Holla V, Backlund M, Yang P, Newman R, DuBois R. Regulation of prostaglandin transporters in colorectal neoplasia. Cancer Prev Res (Phila). 2008;1:93-9 pubmed publisher
    ..Our collective data suggest that the existing model to explain increased PGE(2) in colorectal neoplasia should be modified to include the novel mechanism of coordinated up- and down-regulation of genes involved in PGE(2) transport. ..
  48. Kalliokoski A, Backman J, Neuvonen P, Niemi M. Effects of the SLCO1B1*1B haplotype on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide. Pharmacogenet Genomics. 2008;18:937-42 pubmed publisher
    ..The SLCO1B1*1B/*1B genotype is associated with reduced plasma concentrations of repaglinide, consistent with an enhanced hepatic uptake by OATP1B1, but has limited effects on the pharmacokinetics of nateglinide. ..
  49. Ahn S, Bhatnagar V. Update on the molecular physiology of organic anion transporters. Curr Opin Nephrol Hypertens. 2008;17:499-505 pubmed publisher
    b>Organic anion transporters (OATs) mediate the renal absorption and excretion of a wide range of metabolites and xenobiotics...
  50. Yamaguchi H, Sugie M, Okada M, Mikkaichi T, Toyohara T, Abe T, et al. Transport of estrone 3-sulfate mediated by organic anion transporter OATP4C1: estrone 3-sulfate binds to the different recognition site for digoxin in OATP4C1. Drug Metab Pharmacokinet. 2010;25:314-7 pubmed
    ..1)) In conclusion, we found that estrone 3-sulfate is a novel substrate for OATP4C1. Moreover, our results indicate that estrone 3-sulfate does not bind to the recognition site for digoxin in OATP4C1. ..
  51. Obaidat A, Roth M, Hagenbuch B. The expression and function of organic anion transporting polypeptides in normal tissues and in cancer. Annu Rev Pharmacol Toxicol. 2012;52:135-51 pubmed publisher
    ..On the basis of the findings summarized in this review, we propose that OATPs could be valuable targets for anticancer therapy. ..
  52. Wright A, Rudan I, Hastie N, Campbell H. A 'complexity' of urate transporters. Kidney Int. 2010;78:446-52 pubmed publisher
  53. Harrison B, Magee M, Mandagere A, Walker G, Dufton C, Henderson L, et al. Effects of rifampicin (rifampin) on the pharmacokinetics and safety of ambrisentan in healthy subjects: a single-sequence, open-label study. Clin Drug Investig. 2010;30:875-885 pubmed publisher
    ..No dose adjustment of ambrisentan should be required when it is co-administered with rifampicin, a strong inducer of CYP3A4 activity and inhibitor of OATPs. ..
  54. Svoboda M, Riha J, Wlcek K, Jaeger W, Thalhammer T. Organic anion transporting polypeptides (OATPs): regulation of expression and function. Curr Drug Metab. 2011;12:139-53 pubmed
    ..For drugs, this may result in increased toxicity and adverse drug reactions. Therefore, it is important to improve the knowledge on the regulation and function of individual OATPs, and to apply it for therapeutic considerations. ..
  55. Sissung T, Baum C, Kirkland C, Gao R, Gardner E, Figg W. Pharmacogenetics of membrane transporters: an update on current approaches. Mol Biotechnol. 2010;44:152-67 pubmed publisher
    ..A comprehensive list of substrates for the major drug transporters is included. Finally, studies linking transporter genotype with clinical outcomes are discussed...
  56. Leonhardt M, Keiser M, Oswald S, Kuhn J, Jia J, Grube M, et al. Hepatic uptake of the magnetic resonance imaging contrast agent Gd-EOB-DTPA: role of human organic anion transporters. Drug Metab Dispos. 2010;38:1024-8 pubmed publisher
    ..There is evidence from preclinical studies that multidrug organic anion transporters are involved in hepatic uptake of Gd-EOB-DTPA...
  57. Mima A, Ichida K, Matsubara T, Kanamori H, Inui E, Tanaka M, et al. Acute renal failure after exercise in a Japanese sumo wrestler with renal hypouricemia. Am J Med Sci. 2008;336:512-4 pubmed publisher
    ..Thus, we describe a Japanese sumo wrestler of familial renal hypouricemia complicated with anaerobic exercise-induced ARF, with definite demonstration of genetic abnormality in the responsible gene, URAT1. ..
  58. 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. ..
  59. Bailey D. Fruit juice inhibition of uptake transport: a new type of food-drug interaction. Br J Clin Pharmacol. 2010;70:645-55 pubmed publisher
    ..The interaction between grapefruit juice and etoposide also seemed relevant. Knowledge of both affected uptake transporter and drug hydrophilicity assisted prediction of the clinical interaction with grapefruit or orange juice. ..
  60. Donnelly L, Doney A, Tavendale R, Lang C, Pearson E, Colhoun H, et al. Common nonsynonymous substitutions in SLCO1B1 predispose to statin intolerance in routinely treated individuals with type 2 diabetes: a go-DARTS study. Clin Pharmacol Ther. 2011;89:210-6 pubmed publisher
    ..This study suggests that common genetic variants selected for an extreme phenotype of statin-induced myopathy also predispose to more common milder statin intolerance and may, for this reason, impact lipid-lowering efficacy. ..
  61. Brunham L, Lansberg P, Zhang L, Miao F, Carter C, Hovingh G, et al. Differential effect of the rs4149056 variant in SLCO1B1 on myopathy associated with simvastatin and atorvastatin. Pharmacogenomics J. 2012;12:233-7 pubmed publisher
    ..Our findings provide further support for a role for SLCO1B1 genotype in simvastatin-associated myopathy, and suggest that this association may be stronger for simvastatin compared with atorvastatin...
  62. 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. ..
  63. He J, Qiu Z, Li N, Yu Y, Lu Y, Han D, et al. Effects of SLCO1B1 polymorphisms on the pharmacokinetics and pharmacodynamics of repaglinide in healthy Chinese volunteers. Eur J Clin Pharmacol. 2011;67:701-7 pubmed publisher
    ..Moreover, this polymorphism of SLCO1B1 has significant influence on the pharmacokinetics of repaglinide, but no effects on its pharmacodynamics. ..
  64. He Y, Zhang W, Chen Y, Guo D, Tu J, Xu L, et al. Rifampicin alters atorvastatin plasma concentration on the basis of SLCO1B1 521T>C polymorphism. Clin Chim Acta. 2009;405:49-52 pubmed publisher
    ..05). These results suggested that rifampicin elevated the plasma concentration of atorvastatin depending on SLCO1B1 genotype and rifampicin pharmacokinetics were not altered by SLCO1B1 genotype. ..
  65. Marciante K, Durda J, Heckbert S, Lumley T, Rice K, McKnight B, et al. Cerivastatin, genetic variants, and the risk of rhabdomyolysis. Pharmacogenet Genomics. 2011;21:280-8 pubmed publisher
    ..48; 95% confidence interval: 0.36-0.63). We identified modest genetic risk factors for an extreme response to cerivastatin. Disabling genetic variants in the candidate genes were not responsible for the bimodal response to cerivastatin. ..
  66. Lopez Lopez E, Martin Guerrero I, Ballesteros J, Piñan M, García Miguel P, Navajas A, et al. Polymorphisms of the SLCO1B1 gene predict methotrexate-related toxicity in childhood acute lymphoblastic leukemia. Pediatr Blood Cancer. 2011;57:612-9 pubmed publisher
    ..Identification of the rs4149081 and rs11045879 SLCO1B1 polymorphisms in children with ALL could be a useful tool for monitoring patients at risk of low-MTX clearance in order to avoid MTX-related toxicity. ..
  67. Kindla J, Fromm M, Konig J. In vitro evidence for the role of OATP and OCT uptake transporters in drug-drug interactions. Expert Opin Drug Metab Toxicol. 2009;5:489-500 pubmed
  68. Zlender V, Breljak D, Ljubojevic M, Flajs D, Balen D, Brzica H, et al. Low doses of ochratoxin A upregulate the protein expression of organic anion transporters Oat1, Oat2, Oat3 and Oat5 in rat kidney cortex. Toxicol Appl Pharmacol. 2009;239:284-96 pubmed publisher
  69. Bakhiya N, Arlt V, Bahn A, Burckhardt G, Phillips D, Glatt H. Molecular evidence for an involvement of organic anion transporters (OATs) in aristolochic acid nephropathy. Toxicology. 2009;264:74-9 pubmed publisher
    ..Epithelial cells of the proximal tubule are the primary cellular target of AA. To study whether organic anion transporters (OATs) expressed in proximal tubule cells are involved in uptake of AA, we used human epithelial kidney (..
  70. 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. ..
  71. Pressler H, Sissung T, Venzon D, Price D, Figg W. Expression of OATP family members in hormone-related cancers: potential markers of progression. PLoS ONE. 2011;6:e20372 pubmed publisher
    ..OATPs correlate to differentiation in certain hormone-dependent cancers, thus may be useful as biomarkers for assessing clinical treatment and stage of disease. ..
  72. Aklillu E, Mugusi S, Ngaimisi E, Hoffmann M, König S, Ziesenitz V, et al. Frequency of the SLCO1B1 388A>G and the 521T>C polymorphism in Tanzania genotyped by a new LightCycler®-based method. Eur J Clin Pharmacol. 2011;67:1139-45 pubmed publisher
    ..The clinical relevance of SLCO1B1 genetic variation in the African population remains to be investigated. ..
  73. Ose A, Kusuhara H, Endo C, Tohyama K, Miyajima M, Kitamura S, et al. Functional characterization of mouse organic anion transporting peptide 1a4 in the uptake and efflux of drugs across the blood-brain barrier. Drug Metab Dispos. 2010;38:168-76 pubmed publisher
    ..Whether Oatp1a4 can deliver drugs from the blood to the brain remains controversial...
  74. Hollis Moffatt J, Xu X, Dalbeth N, Merriman M, Topless R, Waddell C, et al. Role of the urate transporter SLC2A9 gene in susceptibility to gout in New Zealand M?ori, Pacific Island, and Caucasian case-control sample sets. Arthritis Rheum. 2009;60:3485-92 pubmed publisher
    ..More extensive linkage disequilibrium in M?ori and Pacific Island samples suggests that Caucasian samples may be more useful for fine-mapping. ..
  75. Treviño L, Shimasaki N, Yang W, Panetta J, Cheng C, Pei D, et al. Germline genetic variation in an organic anion transporter polypeptide associated with methotrexate pharmacokinetics and clinical effects. J Clin Oncol. 2009;27:5972-8 pubmed publisher
    ..4; P = .03 to .004). A genome-wide interrogation identified inherited variations in a plausible, yet heretofore low-priority candidate gene, SLCO1B1, as important determinants of methotrexate's pharmacokinetics and clinical effects. ..
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    ..We demonstrated that the conserved positively charged amino acids Lys41 and Arg580 are pivotal to the transport activity of OATP1B3. ..