SLCO1A2

Summary

Gene Symbol: SLCO1A2
Description: solute carrier organic anion transporter family member 1A2
Alias: OATP, OATP-A, OATP1A2, SLC21A3, solute carrier organic anion transporter family member 1A2, OATP-1, organic anion transporting polypeptide A, organic anion-transporting polypeptide 1, sodium-independent organic anion transporter, solute carrier family 21 (organic anion transporter), member 3, solute carrier family 21 member 3
Species: human
Products:     SLCO1A2

Top Publications

  1. Hartkoorn R, Kwan W, Shallcross V, Chaikan A, Liptrott N, Egan D, et al. HIV protease inhibitors are substrates for OATP1A2, OATP1B1 and OATP1B3 and lopinavir plasma concentrations are influenced by SLCO1B1 polymorphisms. Pharmacogenet Genomics. 2010;20:112-20 pubmed publisher
    OATP1B1 and OATP1B3 are major hepatic drug transporters whilst OATP1A2 is mainly located in the brain but is also located in liver and several other organs...
  2. Lee W, Glaeser H, Smith L, Roberts R, Moeckel G, Gervasini G, et al. Polymorphisms in human organic anion-transporting polypeptide 1A2 (OATP1A2): implications for altered drug disposition and central nervous system drug entry. J Biol Chem. 2005;280:9610-7 pubmed
    ..Therefore, genetic variation in SLCO1A2 may have important implications to the disposition and tissue penetration of substrate drugs...
  3. 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
    ..We aimed to determine the influence of the individual human OATP1B1, OATP1B3, and OATP1A2 transporters on the in vivo disposition of the anticancer drugs methotrexate and paclitaxel by using liver-..
  4. Kullak Ublick G, Hagenbuch B, Stieger B, Schteingart C, Hofmann A, Wolkoff A, et al. Molecular and functional characterization of an organic anion transporting polypeptide cloned from human liver. Gastroenterology. 1995;109:1274-82 pubmed
    ..Furthermore, its additional localization in a variety of extrahepatic tissues suggests that it plays a fundamental role in overall transepithelial organic anion transport of the human body. ..
  5. Su Y, Zhang X, Sinko P. Human organic anion-transporting polypeptide OATP-A (SLC21A3) acts in concert with P-glycoprotein and multidrug resistance protein 2 in the vectorial transport of Saquinavir in Hep G2 cells. Mol Pharm. 2004;1:49-56 pubmed
    ..However, the potential role of absorptive influx transporters such as OATP-A (SLC21A3) has not yet been reported for SQV...
  6. Zhou F, Lee A, Krafczyk K, Zhu L, Murray M. Protein kinase C regulates the internalization and function of the human organic anion transporting polypeptide 1A2. Br J Pharmacol. 2011;162:1380-8 pubmed publisher
    The human organic anion transporting polypeptide 1A2 (OATP1A2) is expressed in cells from several regions of the human body, including the kidney, cholangiocytes and the blood-brain barrier, and mediates the cellular flux of various ..
  7. Eechoute K, Franke R, Loos W, Scherkenbach L, Boere I, Verweij J, et al. Environmental and genetic factors affecting transport of imatinib by OATP1A2. Clin Pharmacol Ther. 2011;89:816-20 pubmed publisher
    ..we found that imatinib is transported by the intestinal uptake carrier organic anion transporting polypeptide (OATP1A2) and that this process is sensitive to pH, rosuvastatin, and genetic variants...
  8. Rebello S, Zhao S, Hariry S, Dahlke M, Alexander N, Vapurcuyan A, et al. Intestinal OATP1A2 inhibition as a potential mechanism for the effect of grapefruit juice on aliskiren pharmacokinetics in healthy subjects. Eur J Clin Pharmacol. 2012;68:697-708 pubmed publisher
    ..The uptake of [¹?C]aliskiren and [³H]fexofenadine was linear in OATP1A2-expressing cells and was reduced by naringin, with IC?? values of 75.5 ± 11.6 and 24.2 ± 2.0 ?M, respectively...
  9. Zhou F, Zheng J, Zhu L, Jodal A, Cui P, Wong M, et al. Functional analysis of novel polymorphisms in the human SLCO1A2 gene that encodes the transporter OATP1A2. AAPS J. 2013;15:1099-108 pubmed publisher
    The solute carrier organic anion transporting polypeptide 1A2 (OATP1A2, SLCO1A2) is implicated in the cellular influx of a number of drugs...

More Information

Publications123 found, 100 shown here

  1. Cheng Z, Liu H, Yu N, Wang F, An G, Xu Y, et al. Hydrophilic anti-migraine triptans are substrates for OATP1A2, a transporter expressed at human blood-brain barrier. Xenobiotica. 2012;42:880-90 pubmed publisher
    b>OATP1A2 is expressed in the luminal membrane of human blood-brain barrier (BBB). The human tissue with the highest OATP1A2 mRNA expression is the brain. We have established a robust BacMam2-OATP1A2 transduced HEK293 system...
  2. Chen L, Yang H, Yu C, Yuan M, Li H. High hepatic exposure of furanocoumarins in Radix Angelica dahuricae is associated with transporter mediated active uptake. J Ethnopharmacol. 2018;212:74-85 pubmed publisher
    ..Ritonavir (RTN) and cyclosporine A (CsA), the known inhibitors of organic anion transporting polypeptide (Oatp) significantly inhibited the hepatic uptake of IM and BER, while the inhibitor of the organic anion transporters (..
  3. Kerb R. Implications of genetic polymorphisms in drug transporters for pharmacotherapy. Cancer Lett. 2006;234:4-33 pubmed
    ..organic anion and cation transporters (OAT, OCT, solute carrier family SLC22A), organic anion transport proteins (OATP, solute carrier family SLCO, formerly SLC21A), and MRPs (ABCCs), other members of the ATP-binding cassette family...
  4. Tian J, Keller M, Oler A, Rabaglia M, Schueler K, Stapleton D, et al. Identification of the Bile Acid Transporter Slco1a6 as a Candidate Gene That Broadly Affects Gene Expression in Mouse Pancreatic Islets. Genetics. 2015;201:1253-62 pubmed publisher
    ..When transiently overexpressed in HEK293 cells, BTBR organic anion transporting polypeptide (OATP)1A6-mediated cellular uptake of the bile acid taurocholic acid (TCA) was enhanced compared to B6 OATP1A6...
  5. Clarke J, Dzierlenga A, Arman T, Toth E, Li H, Lynch K, et al. Nonalcoholic fatty liver disease alters microcystin-LR toxicokinetics and acute toxicity. Toxicon. 2019;162:1-8 pubmed publisher
    ..MCLR toxicity is dependent on cellular uptake through the organic anion transporting polypeptide (OATP) transporters...
  6. Mannino G, Sesti G. Individualized therapy for type 2 diabetes: clinical implications of pharmacogenetic data. Mol Diagn Ther. 2012;16:285-302 pubmed publisher
    ..pharmacokinetics (including the cytochrome P450 [CYP] superfamily, the organic anion transporting polypeptide [OATP] family, and the polyspecific organic cation transporter [OCT] family); genes encoding drug targets and receptors (..
  7. Plaza Parrochia F, Poblete C, Gabler F, Carvajal R, Romero C, Valladares L, et al. Expression of steroid sulfated transporters and 3β-HSD activity in endometrium of women having polycystic ovary syndrome. Steroids. 2015;104:189-95 pubmed publisher
    ..and requires transporters for cell intake, that belong to the families of organic anion transporting polypeptides (OATP) and organic anion transporters (OAT)...
  8. Lofthouse E, Cleal J, O Kelly I, Sengers B, Lewis R. Estrone sulphate uptake by the microvillous membrane of placental syncytiotrophoblast is coupled to glutamate efflux. Biochem Biophys Res Commun. 2018;506:237-242 pubmed publisher
    ..OAT and OATP transporter proteins were over expressed in Xenopus oocytes to study their transport characteristics...
  9. Ghersi Egea J, Gazzin S, Strazielle N. Blood-brain interfaces and bilirubin-induced neurological diseases. Curr Pharm Des. 2009;15:2893-907 pubmed
    ..We specifically address the role of ABC and OATP transporters, glutathione-S-transferases, and the potential involvement of glucuronoconjugation and oxidative ..
  10. Groen S, LaPlante E, Alexandre N, Agrawal A, Dobler S, Whiteman N. Multidrug transporters and organic anion transporting polypeptides protect insects against the toxic effects of cardenolides. Insect Biochem Mol Biol. 2017;81:51-61 pubmed publisher
    ..At this concentration, both Mdr and Oatp knockout mutant flies died more rapidly than wildtype flies, and the mutants also experienced more adverse ..
  11. El Kattan A, Varma M, Steyn S, Scott D, Maurer T, Bergman A. Projecting ADME Behavior and Drug-Drug Interactions in Early Discovery and Development: Application of the Extended Clearance Classification System. Pharm Res. 2016;33:3021-3030 pubmed
    ..For class 1B drugs, oral absorption is high and the predominant clearance mechanism is hepatic uptake mediated by OATP transporters...
  12. Petrovic V, Kojovic D, Cressman A, Piquette Miller M. Maternal bacterial infections impact expression of drug transporters in human placenta. Int Immunopharmacol. 2015;26:349-56 pubmed publisher
    ..these data show that maternal infections impact the expression of key drug transporters in placenta, suggesting that materno-fetal drug transport may be altered by changes in placental expression of ABC and OATP transporters.
  13. Zhang H, Liu J, Hu B, Wang L, Yang Z, Han X, et al. Dual-channel fluorescence diagnosis of cancer cells/tissues assisted by OATP transporters and cysteine/glutathione. Chem Sci. 2018;9:3209-3214 pubmed publisher
    ..cancer cell, rather than normal cell, membranes by active transport of the organic-anion transporting polypeptide (OATP) transporters overexpressed in many types of cancer cell, and is then activated by intracellular cysteine (Cys) and ..
  14. Dolberg A, Reichl S. Expression analysis of human solute carrier (SLC) family transporters in nasal mucosa and RPMI 2650 cells. Eur J Pharm Sci. 2018;123:277-294 pubmed publisher
    ..The expression profiles of PEPT2, OATP1A2, OATP4C1, OCT2, OCTN1 and OCTN2 were investigated at the gene and protein levels by performing RT-PCR, western ..
  15. Kusuhara H, Sugiyama Y. Active efflux across the blood-brain barrier: role of the solute carrier family. NeuroRx. 2005;2:73-85 pubmed
    ..role in the efflux transport, especially for organic anions, which include organic anion transporting polypeptides (OATP/SLCO) and organic anion transporters (OAT/SLC22A)...
  16. Pomari E, Dalla Valle L, Pertile P, Colombo L, Thornton M. Intracrine sex steroid synthesis and signaling in human epidermal keratinocytes and dermal fibroblasts. FASEB J. 2015;29:508-24 pubmed publisher
    ..components were present, although only keratinocytes expressed the organic anion organic anion transporter protein (OATP) 2B1 transporter. Both expressed the G-protein-coupled estrogen receptor (GPER1)...
  17. Bodeman C, Dzierlenga A, Tally C, Mulligan R, Lake A, Cherrington N, et al. Differential regulation of hepatic organic cation transporter 1, organic anion-transporting polypeptide 1a4, bile-salt export pump, and multidrug resistance-associated protein 2 transporter expression in lymphocyte-deficient mice associates with inte. J Pharmacol Exp Ther. 2013;347:136-44 pubmed publisher
    ..Branched DNA signal amplification was used to assess mRNA levels of organic anion-transporting polypeptides (Oatp) 1a1, 1a4, and 1b2; organic cation transporter (Oct) 1; canalicular bile-salt export pump (Bsep); multidrug ..
  18. Mason B, Pariante C, Jamel S, Thomas S. Central nervous system (CNS) delivery of glucocorticoids is fine-tuned by saturable transporters at the blood-CNS barriers and nonbarrier regions. Endocrinology. 2010;151:5294-305 pubmed publisher
    ..including the efflux transporter, P-glycoprotein, and members of the organic anion transporter polypeptide (oatp) family, both of which have been found at the blood-CNS barriers...
  19. Huang C, Chen H, Lin T, Lin A, Lii C. Shikonin upregulates the expression of drug-metabolizing enzymes and drug transporters in primary rat hepatocytes. J Ethnopharmacol. 2018;216:18-25 pubmed publisher
    ..e., P-glycoprotein, multidrug resistance-associated protein 2/3, organic anion transporting polypeptide (OATP) 1B1, and OATP2B1...
  20. Garimella T, Tao X, Sims K, Chang Y, Rana J, Myers E, et al. Effects of a Fixed-Dose Co-Formulation of Daclatasvir, Asunaprevir, and Beclabuvir on the Pharmacokinetics of a Cocktail of Cytochrome P450 and Drug Transporter Substrates in Healthy Subjects. Drugs R D. 2018;18:55-65 pubmed publisher
    ..CYP3A4, CYP2D6, and OATP substrates should be co-administered with caution...
  21. Roberts L, Black D, Raman C, Woodford K, Zhou M, Haggerty J, et al. Subcellular localization of transporters along the rat blood-brain barrier and blood-cerebral-spinal fluid barrier by in vivo biotinylation. Neuroscience. 2008;155:423-38 pubmed publisher
    ..Organic anion transporter (Oat) 3 (Slc22a8), organic anion transporter polypeptide (Oatp) 2b1 (Slco2b1, Oatpb), and Mrp5 (Abcc5) were not detected on the luminal surface using either method, while Oatp1a4 ..
  22. Köhrle J. Thyroid Hormones and Derivatives: Endogenous Thyroid Hormones and Their Targets. Methods Mol Biol. 2018;1801:85-104 pubmed publisher
    ..requires a number of cell-membrane transporters or facilitators such as MCT8 or MCT10 and members of the OATP and LAT families of transporters...
  23. Cipriano M, Correia J, Camões S, Oliveira N, Cruz P, Cruz H, et al. The role of epigenetic modifiers in extended cultures of functional hepatocyte-like cells derived from human neonatal mesenchymal stem cells. Arch Toxicol. 2017;91:2469-2489 pubmed publisher
    ..The enhanced hepatic differentiation observed was supported by the presence of the hepatic drug transporters OATP-C and MRP-2 and gene expression of the hepatic markers CK18, TAT, AFP, ALB, HNF4A and CEBPA; and by their ability ..
  24. Bi Y, Scialis R, Lazzaro S, Mathialagan S, Kimoto E, Keefer J, et al. Reliable Rate Measurements for Active and Passive Hepatic Uptake Using Plated Human Hepatocytes. AAPS J. 2017;19:787-796 pubmed publisher
    ..On the basis of inhibition profiles, the contribution of active versus passive and OATP versus non-OATP transport to the PHH uptake was discerned for various endogenous substrates and statins...
  25. Raška J, Čtveráčková L, Dydowiczova A, Sovadinova I, Blaha L, Babica P. Tumor-promoting cyanotoxin microcystin-LR does not induce procarcinogenic events in adult human liver stem cells. Toxicol Appl Pharmacol. 2018;345:103-113 pubmed publisher
    ..OATPs) or multidrug resistance (MDR) proteins, as indicated (a) by a gene expression analysis of 11 human OATP genes and 4 major MDR genes (MDR1/P-glycoprotein, MRP1, MRP2 and BCRP); (b) by non-significant effects of OATP or ..
  26. Sekine T, Miyazaki H, Endou H. Molecular physiology of renal organic anion transporters. Am J Physiol Renal Physiol. 2006;290:F251-61 pubmed
    ..families: the organic anion transporter (OAT) family encoded by SLC22A, the organic anion transporting peptide (OATP) family encoded by SLC21A (SLCO), and the multidrug resistance-associated protein (MRP) family encoded by ABCC...
  27. Furihata T, Morio H, Zhu M, Suzuki Y, Ide H, Tsubota A, et al. Human organic anion transporter 2 is an entecavir, but not tenofovir, transporter. Drug Metab Pharmacokinet. 2017;32:116-119 pubmed publisher
    ..Given these results, ETV and TFV uptake activities in several human OAT/OATP expression systems were examined...
  28. Sortica V, Lindenau J, Cunha M, O Ohnishi M, R Ventura A, Ribeiro Dos Santos Â, et al. SLCO1A2, SLCO1B1 and SLCO2B1 polymorphisms influences chloroquine and primaquine treatment in Plasmodium vivax malaria. Pharmacogenomics. 2017;18:1393-1400 pubmed publisher
    ..002). SLCO1A2 and SLCO1B1 gene treatment over time interactions were associated with gametocytemia clearance rate (p FDR
  29. Wang S, Zeng W, Wu W, Sun L, Yan D. Association between a microRNA binding site polymorphism in SLCO1A2 and the risk of delayed methotrexate elimination in Chinese children with acute lymphoblastic leukemia. Leuk Res. 2018;65:61-66 pubmed publisher
    ..Genetic variation in solute carrier organic anion transporter family member 1A2 (SLCO1A2, the coding gene of OATP1A2) has important implications for the elimination of ..
  30. Hotta K, Ueyama J, Tatsumi Y, Tsukiyama I, Sugiura Y, Saito H, et al. Lack of Contribution of Multidrug Resistance-associated Protein and Organic Anion-transporting Polypeptide to Pharmacokinetics of Regorafenib, a Novel Multi-Kinase Inhibitor, in Rats. Anticancer Res. 2015;35:4681-9 pubmed
    ..The involvement of organic anion-transporting polypeptide 1 (OATP1; OATP in humans) and OATP2 in the hepatic uptake of regorafenib and their protein levels in the liver were also ..
  31. Teneva I, Klaczkowska D, Batsalova T, Kostova Z, Dzhambazov B. Influence of captopril on the cellular uptake and toxic potential of microcystin-LR in non-hepatic adhesive cell lines. Toxicon. 2016;111:50-7 pubmed publisher
    ..through the plasma membrane, MC-LR needs specific transporters such the organic anion-transporting polypeptides (OATP) that are highly expressed on the hepatocytes...
  32. Kim S, Yoshikado T, Ieiri I, Maeda K, Kimura M, Irie S, et al. Clarification of the Mechanism of Clopidogrel-Mediated Drug-Drug Interaction in a Clinical Cassette Small-dose Study and Its Prediction Based on In Vitro Information. Drug Metab Dispos. 2016;44:1622-32 pubmed publisher
    ..with cerivastatin-induced rhabdomyolysis, and clopidogrel and its metabolites are capable of inhibiting CYP2C8 and OATP 1B1 in vitro...
  33. Liu Y, Luo X, Yang C, Yang T, Zhou J, Shi S. Impact of quercetin?induced changes in drug?metabolizing enzyme and transporter expression on the pharmacokinetics of cyclosporine in rats. Mol Med Rep. 2016;14:3073-85 pubmed publisher
    ..CYP3A2, UDP glucuronosyltransferase family 1 member A complex locus, organic anion?transporting polypeptide (OATP)2B1, OATP1B2, P?glycoprotein, breast cancer resistance protein, and multidrug resistance?associated protein 2 in ..
  34. Johnson E, Won C, Köck K, Paine M. Prioritizing pharmacokinetic drug interaction precipitants in natural products: application to OATP inhibitors in grapefruit juice. Biopharm Drug Dispos. 2017;38:251-259 pubmed publisher
    ..in the model natural product, grapefruit juice, as inhibitors of intestinal organic anion-transporting peptide (OATP)-mediated uptake...
  35. Yim C, Jeong Y, Lee S, Pyeon W, Ryu H, Lee J, et al. Specific Inhibition of the Distribution of Lobeglitazone to the Liver by Atorvastatin in Rats: Evidence for a Rat Organic Anion Transporting Polypeptide 1B2-Mediated Interaction in Hepatic Transport. Drug Metab Dispos. 2017;45:246-259 pubmed publisher
    Cytochrome P450 enzymes and human organic anion transporting polypeptide (OATP) 1B1 are reported to be involved in the pharmacokinetics of lobeglitazone (LB), a new peroxisome proliferator-activated receptor γ agonist...
  36. Miura T, Tachikawa M, Ohtsuka H, Fukase K, Nakayama S, Sakata N, et al. Application of Quantitative Targeted Absolute Proteomics to Profile Protein Expression Changes of Hepatic Transporters and Metabolizing Enzymes During Cholic Acid-Promoted Liver Regeneration. J Pharm Sci. 2017;106:2499-2508 pubmed publisher
    ..bile acid transporters Na+-taurocholate cotransporting polypeptide, anion transporting polypeptide (oatp) 1a1, and oatp1b2, bile acid synthesis-related enzymes cyp7a1 and cyp8b1, and drug transporters breast cancer ..
  37. Riccardi K, Lin J, Li Z, Niosi M, Ryu S, Hua W, et al. Novel Method to Predict In Vivo Liver-to-Plasma Kpuu for OATP Substrates Using Suspension Hepatocytes. Drug Metab Dispos. 2017;45:576-580 pubmed publisher
    ..Validation was performed using six OATP substrates with rat in vivo Kpuu data from i.v. infusion studies where a steady state was achieved...
  38. Koo T, Lee J, Yan J, Jang J, Ju K, Han M, et al. The P2X7 receptor antagonist, oxidized adenosine triphosphate, ameliorates renal ischemia-reperfusion injury by expansion of regulatory T cells. Kidney Int. 2017;92:415-431 pubmed publisher
    ..Here we tested whether periodate-oxidized ATP (oATP), a P2X7 receptor (P2X7R) antagonist can attenuate renal ischemia-reperfusion injury and clarify the related ..
  39. Edginton A, Zimmerman E, Vasilyeva A, Baker S, Panetta J. Sorafenib metabolism, transport, and enterohepatic recycling: physiologically based modeling and simulation in mice. Cancer Chemother Pharmacol. 2016;77:1039-52 pubmed publisher
    ..It included relevant influx (Oatp) and efflux (Abcc2 and Abcc3) transporters, hepatic metabolic enzymes (CYP3A4 and UGT1A9), and intestinal ?-..
  40. Nishizawa K, Nakanishi T, Tamai I. Comparative Evaluation of Dehydroepiandrosterone Sulfate Potential to Predict Hepatic Organic Anion Transporting Polypeptide Transporter-Based Drug-Drug Interactions. Drug Metab Dispos. 2017;45:224-227 pubmed publisher
    ..we reported that plasma dehydroepiandrosterone sulfate (DHEAS) could serve as an endogenous probe to predict OATP-based DDIs in monkeys using rifampicin as an OATP inhibitor...
  41. Shen H, Chen W, Drexler D, Mandlekar S, Holenarsipur V, Shields E, et al. Comparative Evaluation of Plasma Bile Acids, Dehydroepiandrosterone Sulfate, Hexadecanedioate, and Tetradecanedioate with Coproporphyrins I and III as Markers of OATP Inhibition in Healthy Subjects. Drug Metab Dispos. 2017;45:908-919 pubmed publisher
    ..endogenous compounds have been proposed as candidate biomarkers to monitor organic anion transporting polypeptide (OATP) function in preclinical species or humans...
  42. Ingelido A, Abballe A, Gemma S, Dellatte E, Iacovella N, De Angelis G, et al. Biomonitoring of perfluorinated compounds in adults exposed to contaminated drinking water in the Veneto Region, Italy. Environ Int. 2018;110:149-159 pubmed publisher
    ..The enrolled population was also genotyped for the OATP1A2*3 allelic variant, possibly affecting PFAS excretion and hence the internal dose...
  43. Chan S, Martin Santos A, Loubière L, Gonzalez A, Stieger B, Logan A, et al. The expression of thyroid hormone transporters in the human fetal cerebral cortex during early development and in N-Tera-2 neurodifferentiation. J Physiol. 2011;589:2827-45 pubmed publisher
    ..Compared with adult cortex, mRNAs encoding OATP1A2, OATP1C1, OATP3A1 variant 2, OATP4A1, LAT2 and CD98 were reduced in fetal cortex at different gestational ages, ..
  44. Bednarczyk D, Boiselle C. Organic anion transporting polypeptide (OATP)-mediated transport of coproporphyrins I and III. Xenobiotica. 2016;46:457-66 pubmed publisher
    ..4. The identification of coproporphyrins as OATP substrates in vitro more clearly defines the role of OATPs in the hepatic disposition and renal excretion of ..
  45. Keiser M, Kaltheuner L, Wildberg C, Müller J, Grube M, Partecke L, et al. The Organic Anion-Transporting Peptide 2B1 Is Localized in the Basolateral Membrane of the Human Jejunum and Caco-2 Monolayers. J Pharm Sci. 2017;106:2657-2663 pubmed publisher
    The organic anion-transporting polypeptide (OATP) 2B1 which is ubiquitously expressed in the human body is assumed to play an important role in the cellular uptake of many drugs...
  46. Patik I, Székely V, Német O, Szepesi Ã, Kucsma N, Várady G, et al. Identification of novel cell-impermeant fluorescent substrates for testing the function and drug interaction of Organic Anion-Transporting Polypeptides, OATP1B1/1B3 and 2B1. Sci Rep. 2018;8:2630 pubmed publisher
    ..Inhibition of Cascade Blue or Alexa Fluor 405 uptake by known OATP substrates/inhibitors yielded IC50 values in agreement with gold-standard radioligand assays...
  47. Meyer zu Schwabedissen H, Tirona R, Yip C, Ho R, Kim R. Interplay between the nuclear receptor pregnane X receptor and the uptake transporter organic anion transporter polypeptide 1A2 selectively enhances estrogen effects in breast cancer. Cancer Res. 2008;68:9338-47 pubmed publisher
    ..In this study, we show that mRNA expression of organic anion transporter polypeptide 1A2 (OATP1A2), a transporter capable of mediating the cellular uptake of estrogen metabolites, is nearly 10-fold greater in ..
  48. Chan T, Zhu L, Madigan M, Wang K, Shen W, Gillies M, et al. Human organic anion transporting polypeptide 1A2 (OATP1A2) mediates cellular uptake of all-trans-retinol in human retinal pigmented epithelial cells. Br J Pharmacol. 2015;172:2343-53 pubmed publisher
    ..This study investigated the role of human organic anion transporting polypeptide 1A2 (OATP1A2) in atROL uptake in human RPE...
  49. Steiner K, Zimmermann L, Hagenbuch B, Dietrich D. Zebrafish Oatp-mediated transport of microcystin congeners. Arch Toxicol. 2016;90:1129-39 pubmed publisher
    ..Differences in observed MC toxicity in various fish species suggest differential expression of Oatp subtypes leading to varying tissue distribution of the very same MC congener within different species...
  50. Namgoong S, Cheong H, Kim J, Kim L, Na H, Koh I, et al. Comparison of genetic variations of the SLCO1B1, SLCO1B3, and SLCO2B1 genes among five ethnic groups. Environ Toxicol Pharmacol. 2015;40:692-7 pubmed publisher
    Organic anion-transporting polypeptide (OATP; gene symbol, SLCO) transporters are generally involved in the uptake of multiple drugs and their metabolites at most epithelial barriers...
  51. Moj D, Hanke N, Britz H, Frechen S, Kanacher T, Wendl T, et al. Clarithromycin, Midazolam, and Digoxin: Application of PBPK Modeling to Gain New Insights into Drug-Drug Interactions and Co-medication Regimens. AAPS J. 2017;19:298-312 pubmed publisher
    ..well as a substrate and competitive inhibitor of P-glycoprotein (P-gp) and organic anion-transporting polypeptides (OATP) 1B1 and 1B3...
  52. Bulc Rozman K, Juric D, Suput D. Selective cytotoxicity of microcystins LR, LW and LF in rat astrocytes. Toxicol Lett. 2017;265:1-8 pubmed publisher
    ..The cultured astrocytes expressed organic anion-transporting polypeptides (Oatp) Oatp1a4, Oatp1c1 and Oatp1a5, but not Oatp1b2...
  53. Yamakawa Y, Hamada A, Shuto T, Yuki M, Uchida T, Kai H, et al. Pharmacokinetic impact of SLCO1A2 polymorphisms on imatinib disposition in patients with chronic myeloid leukemia. Clin Pharmacol Ther. 2011;90:157-63 pubmed publisher
    ..this study was to explore the role of the organic anion-transporting polypeptide (OATP) 1A2, which is encoded by SLCO1A2, in the cellular uptake of the Bcr-Abl tyrosine kinase inhibitor imatinib, and the relationship between SLCO1A2 ..
  54. Fujita D, Saito Y, Nakanishi T, Tamai I. Organic Anion Transporting Polypeptide (OATP)2B1 Contributes to Gastrointestinal Toxicity of Anticancer Drug SN-38, Active Metabolite of Irinotecan Hydrochloride. Drug Metab Dispos. 2016;44:1-7 pubmed publisher
    ..Based on the fact that liver-specific organic anion transporting polypeptide (OATP)1B1, a member of the same family as OATP2B1, is known to be involved in hepatic transport of SN-38, we hypothesized ..
  55. Duan P, Zhao P, Zhang L. Physiologically Based Pharmacokinetic (PBPK) Modeling of Pitavastatin and Atorvastatin to Predict Drug-Drug Interactions (DDIs). Eur J Drug Metab Pharmacokinet. 2017;42:689-705 pubmed publisher
    ..The statin models reasonably predicted the observed exposure change due to Organic Anion Transporting Polypeptide (OATP) 1B1 polymorphism or clinical DDIs with itraconazole, erythromycin, and gemfibrozil, while under-predicted the ..
  56. Ni C, Yu X, Fang Z, Huang J, Hong M. Oligomerization Study of Human Organic Anion Transporting Polypeptide 1B1. Mol Pharm. 2017;14:359-367 pubmed publisher
    ..It has been proposed that OATP family members, as membrane proteins, may form oligomers...
  57. Li X, Zhong K, Guo Z, Zhong D, Chen X. Fasiglifam (TAK-875) Inhibits Hepatobiliary Transporters: A Possible Factor Contributing to Fasiglifam-Induced Liver Injury. Drug Metab Dispos. 2015;43:1751-9 pubmed publisher
    ..9 μM. TAK-875 significantly inhibited atorvastatin uptake in organic anion transporter protein (OATP) 1B1 and OATP1B3 cells with IC₅₀ values of 2.28 and 3.98 μM, respectively...
  58. Mikkaichi T, Nakai D, Yoshigae Y, Imaoka T, Okudaira N, Izumi T. Liver-selective distribution in rats supports the importance of active uptake into the liver via organic anion transporting polypeptides (OATPs) in humans. Drug Metab Pharmacokinet. 2015;30:334-40 pubmed publisher
    Organic anion transporting polypeptide (OATP) 1B1 and 1B3 are key molecules that are involved in hepatic uptake related to drug elimination, and OATP-mediated drug interactions are of clinical concern...
  59. Iparraguirre L, Gutierrez Camino A, Umerez M, Martin Guerrero I, Astigarraga I, Navajas A, et al. MiR-pharmacogenetics of methotrexate in childhood B-cell acute lymphoblastic leukemia. Pharmacogenet Genomics. 2016;26:517-525 pubmed
    ..These miRNAs were predicted, in silico, to regulate genes involved in MTX uptake: SLC46A1, SLC19A1, and SLCO1A2. In this study, we detected three SNPs in miR-5189, miR-595, and miR-6083 that might affect SLC46A1, SLC19A1, and ..
  60. Konig J, Cui Y, Nies A, Keppler D. A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane. Am J Physiol Gastrointest Liver Physiol. 2000;278:G156-64 pubmed
    We cloned and expressed a new organic anion transporting polypeptide (OATP), termed human OATP2, (OATP-C, LST-1; symbol SLC21A6), involved in the uptake of various lipophilic anions into human liver...
  61. Ballatori N, Hammond C, Cunningham J, Krance S, Marchan R. Molecular mechanisms of reduced glutathione transport: role of the MRP/CFTR/ABCC and OATP/SLC21A families of membrane proteins. Toxicol Appl Pharmacol. 2005;204:238-55 pubmed
    ..of ATP-binding cassette (ABC) proteins, as well as some members of the organic anion transporting polypeptide (OATP or SLC21A) family of transporters contribute to this process...
  62. Yoshikado T, Yoshida K, Kotani N, Nakada T, Asaumi R, Toshimoto K, et al. Quantitative Analyses of Hepatic OATP-Mediated Interactions Between Statins and Inhibitors Using PBPK Modeling With a Parameter Optimization Method. Clin Pharmacol Ther. 2016;100:513-523 pubmed publisher
    ..In conclusion, this study proposes a method to optimize in vivo PBPK parameters in hepatic uptake transporter-mediated DDIs. ..
  63. Kondo A, Narumi K, Ogura J, Sasaki A, Yabe K, Kobayashi T, et al. Organic anion-transporting polypeptide (OATP) 2B1 contributes to the cellular uptake of theaflavin. Drug Metab Pharmacokinet. 2017;32:145-150 pubmed publisher
    Organic anion-transporting polypeptide (OATP) 2B1 has been reported in the apical membranes of the human small intestinal epithelium, where it contributes to the intestinal absorption of pharmacologically active drugs...
  64. Shebley M, Liu J, Kavetskaia O, Sydor J, de Morais S, Fischer V, et al. Mechanisms and Predictions of Drug-Drug Interactions of the Hepatitis C Virus Three Direct-Acting Antiviral Regimen: Paritaprevir/Ritonavir, Ombitasvir, and Dasabuvir. Drug Metab Dispos. 2017;45:755-764 pubmed publisher
    ..was predicted for CYP3A, CYP2C8, UDP-glucuronosyltransferase (UGT) 1A1, organic anion-transporting polypeptide (OATP) 1B1/1B3, breast cancer resistance protein (BCRP), and P-glycoprotein (P-gp)...
  65. Traber M, Labut E, Leonard S, Lebold K. ?-Tocopherol injections in rats up-regulate hepatic ABC transporters, but not cytochrome P450 enzymes. Free Radic Biol Med. 2011;51:2031-40 pubmed publisher
    ..Two liver efflux transporter genes, ABCB1b and ABCG2, were up-regulated after ?-tocopherol injections, whereas OATP, a liver influx transporter, was down-regulated...
  66. Tournier N, Saba W, Cisternino S, Peyronneau M, Damont A, Goutal S, et al. Effects of selected OATP and/or ABC transporter inhibitors on the brain and whole-body distribution of glyburide. AAPS J. 2013;15:1082-90 pubmed publisher
    ..In vitro studies show that GLB is a substrate of organic anion transporting polypeptide (OATP) and ATP-binding cassette (ABC) transporter families, which may influence GLB distribution and pharmacokinetics in ..
  67. Kawase A, Ito A, Yamada A, Iwaki M. Age-related changes in mRNA levels of hepatic transporters, cytochrome P450 and UDP-glucuronosyltransferase in female rats. Eur J Drug Metab Pharmacokinet. 2015;40:239-44 pubmed publisher
    ..protein (Mrp)2, breast cancer resistance protein (Bcrp) and organic anion-transporting polypeptide (Oatp)1a1, and the metabolic enzymes cytochrome P450 (CYP)3A1, CYP3A2 and UDP-glucuronosyltransferase (UGT)1A1 were ..
  68. Jain L, Abraham S, Shord S. The interactions of anti-cancer drugs approved in the last decade in the United States with membrane transporters. Anticancer Agents Med Chem. 2010;10:601-16 pubmed
    ..anticancer drugs approved in the last decade with the more common membranes transporters, such as ABCB1, ABCG2, and OATP. The drugs were divided into three categories: targeted therapies, cytotoxic agents and hormonal therapies...
  69. Arakawa H, Nakanishi T, Yanagihara C, Nishimoto T, Wakayama T, Mizokami A, et al. Enhanced expression of organic anion transporting polypeptides (OATPs) in androgen receptor-positive prostate cancer cells: possible role of OATP1A2 in adaptive cell growth under androgen-depleted conditions. Biochem Pharmacol. 2012;84:1070-7 pubmed publisher
    ..The stimulatory effect of DHEAS on cell growth was investigated in LNCaP cells in which OATP1A2 had been silenced...
  70. Chino Y, Hasegawa M, Fukasawa Y, Mano Y, Bando K, Miyata A, et al. In vitro evaluation of potential drug interactions mediated by cytochrome P450 and transporters for luseogliflozin, an SGLT2 inhibitor. Xenobiotica. 2017;47:314-323 pubmed publisher
    ..P-glycoprotein (P-gp), but not for breast cancer resistance protein (BCRP), organic anion transporting polypeptide (OATP) 1B1 and OATP1B3, organic anion transporter (OAT) 1 and OAT3, or organic cation transporter (OCT) 2...
  71. Ishida K, Ullah M, Tóth B, Juhász V, Unadkat J. Successful Prediction of In Vivo Hepatobiliary Clearances and Hepatic Concentrations of Rosuvastatin Using Sandwich-Cultured Rat Hepatocytes, Transporter-Expressing Cell Lines, and Quantitative Proteomics. Drug Metab Dispos. 2018;46:66-74 pubmed publisher
    ..b> [Formula: see text] of RSV into cells expressing organic anion transporting polypeptide (Oatp) 1a1, 1a4, and 1b2 was also determined...
  72. Barnett S, Ogungbenro K, Menochet K, Shen H, Lai Y, Humphreys W, et al. Gaining mechanistic insight into coproporphyrin I as endogenous biomarker for OATP1B-mediated drug-drug interactions using population pharmacokinetic modelling and simulation. Clin Pharmacol Ther. 2017;: pubmed publisher
    ..of rifampicin were modelled to describe CPI synthesis, elimination clearances and obtain rifampicin in vivo OATP Ki...
  73. Kullak Ublick G, Beuers U, Meier P, Domdey H, Paumgartner G. Assignment of the human organic anion transporting polypeptide (OATP) gene to chromosome 12p12 by fluorescence in situ hybridization. J Hepatol. 1996;25:985-7 pubmed
    The organic anion transporting polypeptide (OATP) of human liver mediates the basolateral hepatocellular uptake of numerous cholephilic anions and steroidal compounds...
  74. Speek M. Antisense promoter of human L1 retrotransposon drives transcription of adjacent cellular genes. Mol Cell Biol. 2001;21:1973-85 pubmed
    ..These results indicate that many L1Hs contain active ASPs which are capable of interfering with normal gene expression, and this type of transcriptional control may be widespread. ..
  75. Miura M, Kagaya H, Satoh S, Inoue K, Saito M, Habuchi T, et al. Influence of drug transporters and UGT polymorphisms on pharmacokinetics of phenolic glucuronide metabolite of mycophenolic acid in Japanese renal transplant recipients. Ther Drug Monit. 2008;30:559-64 pubmed publisher
    ..BCRP rather than multidrug resistance protein 2 seems to be the transporter associated with biliary excretion of MPAG...
  76. Akamine Y, Miura M, Sunagawa S, Kagaya H, Yasui Furukori N, Uno T. Influence of drug-transporter polymorphisms on the pharmacokinetics of fexofenadine enantiomers. Xenobiotica. 2010;40:782-9 pubmed publisher
    This study investigated an association of SLCO (encoding organic anion-transporting polypeptides (OATP), 1B1, 1B3, and 2B1), ABCB1 (P-glycoprotein (P-gp)), ABCC2 multidrug resistance protein 2 (MRP2), and ABCG2 (breast cancer resistance ..
  77. Zhang A, Jia Y, Xu Q, Wang C, Liu Q, Meng Q, et al. Dioscin protects against ANIT-induced cholestasis via regulating Oatps, Mrp2 and Bsep expression in rats. Toxicol Appl Pharmacol. 2016;305:127-135 pubmed publisher
    ..The uptakes of organic anion transporting polypeptide (Oatp) substrates were altered in liver uptake index in vivo, perfused rat liver in situ and isolated rat hepatocytes in ..
  78. Tan M, Yoshida K, Zhao P, Zhang L, Nolin T, Piquette Miller M, et al. Effect of Chronic Kidney Disease on Nonrenal Elimination Pathways: A Systematic Assessment of CYP1A2, CYP2C8, CYP2C9, CYP2C19, and OATP. Clin Pharmacol Ther. 2017;: pubmed publisher
    ..CYP2C8-metabolized, CYP2C9-metabolized, CYP2C19-metabolized, and organic anion-transporting polypeptide (OATP)-transported drugs was investigated...
  79. Navrátilová L, Ramos Mandíková J, Pávek P, Mladěnka P, Trejtnar F. Honey flavonoids inhibit hOATP2B1 and hOATP1A2 transporters and hOATP-mediated rosuvastatin cell uptake in vitro. Xenobiotica. 2018;48:745-755 pubmed publisher
    ..OATP2B1 and OATP1A2 expressed in the apical membrane of human enterocytes may significantly contribute to the intestinal absorption ..
  80. Njumbe Ediage E, Dillen L, Vroman A, Diels L, Kunze A, Snoeys J, et al. Development of an LC-MS method to quantify coproporphyrin I and III as endogenous biomarkers for drug transporter-mediated drug-drug interactions. J Chromatogr B Analyt Technol Biomed Life Sci. 2018;1073:80-89 pubmed publisher
    Coproporphyrins are proposed as endogenous biomarkers of hepatic Organic Anion Transporting Polypeptide (OATP)1B functional activity...
  81. Petrovic V, Wang J, Piquette Miller M. Effect of endotoxin on the expression of placental drug transporters and glyburide disposition in pregnant rats. Drug Metab Dispos. 2008;36:1944-50 pubmed publisher
    ..biodistribution study was carried out with glyburide, a hypoglycemic sulfonylurea substrate of both ABC efflux and Oatp uptake transporters...
  82. Justenhoven C, Schaeffeler E, Winter S, Baisch C, Hamann U, Harth V, et al. Polymorphisms of the nuclear receptor pregnane X receptor and organic anion transporter polypeptides 1A2, 1B1, 1B3, and 2B1 are not associated with breast cancer risk. Breast Cancer Res Treat. 2011;125:563-9 pubmed publisher
    ..The nuclear receptor pregnane X receptor (PXR) is involved in the regulation of SLCO1A2 expression...
  83. Vaidyanathan J, Yoshida K, Arya V, Zhang L. Comparing Various In Vitro Prediction Criteria to Assess the Potential of a New Molecular Entity to Inhibit Organic Anion Transporting Polypeptide 1B1. J Clin Pharmacol. 2016;56 Suppl 7:S59-72 pubmed publisher
    Evaluation of organic anion transporting polypeptide (OATP) 1B1-mediated drug-drug interactions (DDIs) is an integral part of drug development and is recommended by regulatory agencies...
  84. Kullak Ublick G, Beuers U, Fahney C, Hagenbuch B, Meier P, Paumgartner G. Identification and functional characterization of the promoter region of the human organic anion transporting polypeptide gene. Hepatology. 1997;26:991-7 pubmed
    The organic anion transporting polypeptide (OATP) of the basolateral hepatocyte membrane mediates multispecific uptake of anionic and other amphipathic substrates from sinusoidal blood plasma...
  85. Kato Y, Yoshida K, Watanabe C, Sai Y, Tsuji A. Screening of the interaction between xenobiotic transporters and PDZ proteins. Pharm Res. 2004;21:1886-94 pubmed
    ..PDZ proteins was identified for several xenobiotic transporters including PEPT1, PEPT2, OCT3, OCTN1, OCTN2, OAT4, OATP-A, OATP-D, and OATP-F...
  86. Hashimoto Y, Tatsumi S, Takeda R, Naka A, Ogane N, Kameda Y, et al. Expression of organic anion-transporting polypeptide 1A2 and organic cation transporter 6 as a predictor of pathologic response to neoadjuvant chemotherapy in triple negative breast cancer. Breast Cancer Res Treat. 2014;145:101-11 pubmed publisher
    Organic anion-transporting polypeptide 1A2 (OATP1A2) and organic cation transporter 6 (OCT6) are involved in the uptake of taxanes and anthracyclines, respectively...
  87. Zhou Y, Yuan J, Li Z, Wang Z, Cheng D, Du Y, et al. Genetic polymorphisms and function of the organic anion-transporting polypeptide 1A2 and its clinical relevance in drug disposition. Pharmacology. 2015;95:201-8 pubmed publisher
    ..Human OATP1A2 is a drug uptake transporter known for its broad substrate specificity, including many drugs in clinical use...
  88. Li J, Wu J, Bao X, Honea N, Xie Y, Kim S, et al. Quantitative and Mechanistic Understanding of AZD1775 Penetration across Human Blood-Brain Barrier in Glioblastoma Patients Using an IVIVE-PBPK Modeling Approach. Clin Cancer Res. 2017;23:7454-7466 pubmed publisher
    ..3 to 24.4 (median, 3.2). It was a substrate for ABCB1, ABCG2, and OATP1A2, but not for OATP2B1 or OAT3...
  89. Buch S, Schafmayer C, Volzke H, Seeger M, Miquel J, Sookoian S, et al. Loci from a genome-wide analysis of bilirubin levels are associated with gallstone risk and composition. Gastroenterology. 2010;139:1942-1951.e2 pubmed publisher
    ..Bilirubin is a major component of gallstones so we investigated whether these variants predict gallstone bilirubin content and overall risk for gallstones...
  90. Hartman J, Brouwer K, Mandagere A, Melvin L, GORCZYNSKI R. Evaluation of the endothelin receptor antagonists ambrisentan, darusentan, bosentan, and sitaxsentan as substrates and inhibitors of hepatobiliary transporters in sandwich-cultured human hepatocytes. Can J Physiol Pharmacol. 2010;88:682-91 pubmed publisher
    ..The 4 transporters studied were sodium-dependent taurocholate cotransporter (NTCP), organic anion transporter (OATP), bile salt export pump (BSEP), and multidrug resistance-associated protein 2 (MRP2)...
  91. Kimura N, Hakamada K, Ikenaga S, Umehara Y, Toyoki Y, Sasaki M. Gene expression of ATP-binding cassette transporters during liver regeneration after 90% hepatectomy in rats. Int J Mol Med. 2012;30:28-34 pubmed publisher
    ..Among 20 ABC transporter genes, multidrug resistance protein (MRP) 2 and organic anion transporting polypeptide (OATP) 1 were significantly downregulated, while MRP1 and MRP3 tended to be expressed...
  92. Chahine S, Campos A, O Donnell M. Genetic knockdown of a single organic anion transporter alters the expression of functionally related genes in Malpighian tubules of Drosophila melanogaster. J Exp Biol. 2012;215:2601-10 pubmed publisher
    ..Knockdown of dMRP is associated with a decrease in MET expression but an increase in OATP expression when flies are reared on MTX-enriched diet...