SLCO1B3

Summary

Gene Symbol: SLCO1B3
Description: solute carrier organic anion transporter family member 1B3
Alias: HBLRR, LST-2, LST-3TM13, LST3, OATP-8, OATP1B3, OATP8, SLC21A8, solute carrier organic anion transporter family member 1B3, liver-specific organic anion transporter 2, liver-specific organic anion transporter 3TM13, organic anion transporter 8, organic anion transporter LST-3c, organic anion-transporting polypeptide 8, solute carrier family 21 (organic anion transporter), member 8
Species: human
Products:     SLCO1B3

Top Publications

  1. 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
    ..Besides common substrates with OATP1B1, OATP1B3 specifically transports cholecystokinin octapeptide (CCK-8)...
  2. Muto M, Onogawa T, Suzuki T, Ishida T, Rikiyama T, Katayose Y, et al. Human liver-specific organic anion transporter-2 is a potent prognostic factor for human breast carcinoma. Cancer Sci. 2007;98:1570-6 pubmed
    Human liver-specific organic anion transporter-2 (LST-2/OATP8/SLCO1B3) has been demonstrated to be expressed in various gastrointestinal carcinomas and also to play pivotal roles in the uptake of a wide variety of both endogenous and ..
  3. Cui Y, Konig J, Nies A, Pfannschmidt M, Hergt M, Franke W, et al. Detection of the human organic anion transporters SLC21A6 (OATP2) and SLC21A8 (OATP8) in liver and hepatocellular carcinoma. Lab Invest. 2003;83:527-38 pubmed
    ..into human hepatocytes include the organic anion transporters SLC21A6 (also termed OATP2, OATP-C, or LST-1) and SLC21A8 (OATP8). Both transporters are localized to the basolateral membrane of human hepatocytes...
  4. Hamada A, Sissung T, Price D, Danesi R, Chau C, Sharifi N, et al. Effect of SLCO1B3 haplotype on testosterone transport and clinical outcome in caucasian patients with androgen-independent prostatic cancer. Clin Cancer Res. 2008;14:3312-8 pubmed publisher
    The organic anion transporter OATP1B3, encoded by SLCO1B3, is involved in the transport of steroid hormones. However, its role in testosterone uptake and clinical outcome of prostatic cancer is unknown...
  5. Konig J, Cui Y, Nies A, Keppler D. Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide. J Biol Chem. 2000;275:23161-8 pubmed
    ..2 (OATP2; SLC21A6), we cloned a new member of the SLC21A superfamily of solute carriers, termed OATP8 (SLC21A8). The protein of 702 amino acids showed an amino acid identity of 80% with human OATP2...
  6. Ulvestad M, Bjorquist P, Molden E, Asberg A, Andersson T. OATP1B1/1B3 activity in plated primary human hepatocytes over time in culture. Biochem Pharmacol. 2011;82:1219-26 pubmed publisher
    ..the present study was to evaluate the activity of organic anion-transporting polypeptide 1B1 (OATP1B1) and 1B3 (OATP1B3) in plated primary human hepatocytes over time in culture...
  7. Abe T, Unno M, Onogawa T, Tokui T, Kondo T, Nakagomi R, et al. LST-2, a human liver-specific organic anion transporter, determines methotrexate sensitivity in gastrointestinal cancers. Gastroenterology. 2001;120:1689-99 pubmed
    ..LST-2 is one of the prime candidate molecules for determining methotrexate sensitivity and may be a good target to deliver anticancer drugs to the gastrointestinal cancers. ..
  8. Lee W, Belkhiri A, Lockhart A, Merchant N, Glaeser H, Harris E, et al. Overexpression of OATP1B3 confers apoptotic resistance in colon cancer. Cancer Res. 2008;68:10315-23 pubmed publisher
    Organic anion transporting polypeptide 1B3 (OATP1B3, SLCO1B3) is normally expressed in hepatocytes. In this study, we showed frequent overexpression of OATP1B3 in colorectal adenocarcinomas...
  9. Nagai M, Furihata T, Matsumoto S, Ishii S, Motohashi S, Yoshino I, et al. Identification of a new organic anion transporting polypeptide 1B3 mRNA isoform primarily expressed in human cancerous tissues and cells. Biochem Biophys Res Commun. 2012;418:818-23 pubmed publisher
    Organic anion transporting polypeptide 1B3 (OATP1B3) is a hepatocyte plasma membrane protein that transports various endogenous and xenobiotic compounds...

More Information

Publications123 found, 100 shown here

  1. Kazmi F, Yerino P, McCoy C, Parkinson A, Buckley D, Ogilvie B. An Assessment of the In Vitro Inhibition of Cytochrome P450 Enzymes, UDP-Glucuronosyltransferases, and Transporters by Phosphodiester- or Phosphorothioate-Linked Oligonucleotides. Drug Metab Dispos. 2018;46:1066-1074 pubmed publisher
    ..observed for the organic anion uptake transporters, including organic anion-transporting polypeptide OATP1B1 and OATP1B3, organic anion transporters OAT1 and OAT3, and organic cation transporter OCT2 (IC50 values of 12-29 <..
  2. Mamidi R, Dallas S, Sensenhauser C, Lim H, Scheers E, Verboven P, et al. In vitro and physiologically-based pharmacokinetic based assessment of drug-drug interaction potential of canagliflozin. Br J Clin Pharmacol. 2017;83:1082-1096 pubmed publisher
    ..but was not a substrate of uptake transporters (organic anion transporter polypeptide isoforms OATP1B1, OATP1B3, organic anion transporters OAT1 and OAT3, and organic cationic transporters OCT1, and OCT2)...
  3. Malinen M, Ito K, Kang H, Honkakoski P, Brouwer K. Protein expression and function of organic anion transporters in short-term and long-term cultures of Huh7 human hepatoma cells. Eur J Pharm Sci. 2019;130:186-195 pubmed publisher
    ..Protein expression of OSTα, OSTβ and OATP1B3 increased over time...
  4. Rizk M, Houle R, Chan G, Hafey M, Rhee E, Chu X. Raltegravir has a low propensity to cause clinical drug interactions through inhibition of major drug transporters: an in vitro evaluation. Antimicrob Agents Chemother. 2014;58:1294-301 pubmed publisher
    ..RAL showed no inhibition of organic anion-transporting polypeptide 1B1 (OATP1B1), weak inhibition of OATP1B3 (40% inhibition at 100 ?M), and no inhibition of organic cation transporter 1 (OCT1)...
  5. Tong Z, Yerramilli U, Surapaneni S, Kumar G. The interactions of lenalidomide with human uptake and efflux transporters and UDP-glucuronosyltransferase 1A1: lack of potential for drug-drug interactions. Cancer Chemother Pharmacol. 2014;73:869-74 pubmed publisher
    ..Lenalidomide was also evaluated as an inhibitor of P-gp, BCRP, MRP2, OCT2, OAT1, OAT3, OATP1B1, OATP1B3 and bile salt export pump (BSEP)...
  6. Nicolaï J, Thevelin L, Bing Q, Stieger B, Chanteux H, Augustijns P, et al. Role of the OATP Transporter Family and a Benzbromarone-SensitiveEfflux Transporter in the Hepatocellular Disposition of Vincristine. Pharm Res. 2017;34:2336-2348 pubmed publisher
    ..OATP1B1-, OATP1B3- and OATP2B1- transfected CHO cells showed significantly increased vincristine uptake as compared to wild-type ..
  7. 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
    ..018 and p FDR = 0.024). ABCB1, ABCC4 and SLCO1B3 were not associated with treatment response...
  8. Chen C, Han Y, Yang Z, Rodrigues A. Effect of interferon-?2b on the expression of various drug-metabolizing enzymes and transporters in co-cultures of freshly prepared human primary hepatocytes. Xenobiotica. 2011;41:476-85 pubmed publisher
    ..05). On the other hand, SULT2A1, carboxylesterase 2, organic anion transporting peptide (OATP1B1, OATP1B3, OATP2B1), organic cation transporter 1, P-glycoprotein and breast cancer resistance protein mRNA expression was ..
  9. Pearson D, Weiss H, Jin Y, Jaap van Lier J, Erpenbeck V, Glaenzel U, et al. Absorption, Distribution, Metabolism, and Excretion of the Oral Prostaglandin D2 Receptor 2 Antagonist Fevipiprant (QAW039) in Healthy Volunteers and In Vitro. Drug Metab Dispos. 2017;45:817-825 pubmed publisher
    ..multidrug resistance gene 1 (MDR1; possible biliary excretion), and organic anion-transporting polypeptide 1B3 (OATP1B3; hepatic uptake)...
  10. 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...
  11. Gao C, Liao M, Han L, Thummel K, Mao Q. Hepatic Transport of 25-Hydroxyvitamin D3 Conjugates: A Mechanism of 25-Hydroxyvitamin D3 Delivery to the Intestinal Tract. Drug Metab Dispos. 2018;46:581-591 pubmed publisher
    ..studies, we showed that 25OHD3-G is a substrate of multidrug resistance proteins 2 and 3, OATP1B1, and OATP1B3, and that 25OHD3-S is probably a substrate of breast cancer resistance protein, OATP2B1, and OATP1B3...
  12. Wang L, Collins C, Kelly E, Chu X, Ray A, Salphati L, et al. Transporter Expression in Liver Tissue from Subjects with Alcoholic or Hepatitis C Cirrhosis Quantified by Targeted Quantitative Proteomics. Drug Metab Dispos. 2016;44:1752-1758 pubmed
    ..of transporters (per gram of liver) was diverse, showing an increase (MATE1), decrease (BSEP, MRP2, NTCP, OATP1B3, OCT1, and P-gp), or no change (BCRP, MRP3, OATP1B1, and 2B1)...
  13. van Dijk R, Beuers U, Bosma P. Gene replacement therapy for genetic hepatocellular jaundice. Clin Rev Allergy Immunol. 2015;48:243-53 pubmed publisher
    ..basolateral/sinusoidal hepatocellular membrane proteins, organic anion-transporting polypeptide 1B1 (OATP1B1) and OATP1B3. Dubin-Johnson syndrome is caused by a defect in the ATP-dependent canalicular transporter, multidrug resistance-..
  14. Schulte R, Ho R. Organic Anion Transporting Polypeptides: Emerging Roles in Cancer Pharmacology. Mol Pharmacol. 2019;: pubmed publisher
    ..In the past decade, OATPs, primarily OATP1A2, OATP1B1, and OATP1B3, have emerged as potential mediators of chemotherapy disposition, including drugs such as methotrexate, ..
  15. Brennan B, Poirier A, Moreira S, Morcos P, Goelzer P, Portmann R, et al. Characterization of the transmembrane transport and absolute bioavailability of the HCV protease inhibitor danoprevir. Clin Pharmacokinet. 2015;54:537-49 pubmed publisher
    ..Danoprevir transport in vitro involved organic anion transporting polypeptide (OATP) 1B1, OATP1B3, P-glycoprotein, and multidrug resistance protein-2, but not breast cancer resistance protein...
  16. Lucero M, Gonzalo A, Ganza A, Leal N, Soengas I, Ioja E, et al. Interactions of bilastine, a new oral H₁ antihistamine, with human transporter systems. Drug Chem Toxicol. 2012;35 Suppl 1:8-17 pubmed publisher
    ..organic cation transporter (OCT)1, organic anion transporter (OAT)1, OAT3, OCT2, OATP2B1, OATP1B1, and OATP1B3)...
  17. Weiss J, Theile D, Rüppell M, Speck T, Spalwisz A, Haefeli W. Interaction profile of macitentan, a new non-selective endothelin-1 receptor antagonist, in vitro. Eur J Pharmacol. 2013;701:168-75 pubmed publisher
    ..and revealed that macitentan is an inhibitor of P-gp, breast cancer resistance protein (BCRP), SLCO1B1, and SLCO1B3. Using commercial kits macitentan was demonstrated to be a moderate inhibitor of CYP3A4 and CYP2C19...
  18. Murakami E, Wang T, Park Y, Hao J, Lepist E, Babusis D, et al. Implications of efficient hepatic delivery by tenofovir alafenamide (GS-7340) for hepatitis B virus therapy. Antimicrob Agents Chemother. 2015;59:3563-9 pubmed publisher
    ..hepatic uptake of TAF is also facilitated by the organic anion-transporting polypeptides 1B1 and 1B3 (OATP1B1 and OATP1B3, respectively)...
  19. Shemesh C, Yu R, Warren M, Liu M, Jahic M, Nichols B, et al. Assessment of the Drug Interaction Potential of Unconjugated and GalNAc3-Conjugated 2'-MOE-ASOs. Mol Ther Nucleic Acids. 2017;9:34-47 pubmed publisher
    ..transporters, organic cation transporter 1 (OCT1), organic anion transporting polypeptide 1B1 (OATP1B1), and OATP1B3; three renal uptake transporters, organic anion transporter 1 (OAT1), OAT3, and OCT2; and three efflux ..
  20. Jones A, Freise K, Agarwal S, Humerickhouse R, Wong S, Salem A. Clinical Predictors of Venetoclax Pharmacokinetics in Chronic Lymphocytic Leukemia and Non-Hodgkin's Lymphoma Patients: a Pooled Population Pharmacokinetic Analysis. AAPS J. 2016;18:1192-202 pubmed publisher
    ..race, weak CYP3A inhibitors and inducers as well as OATP1B1 transporter phenotype and P-gp, BCRP, and OATP1B1/OATP1B3 modulators had no impact on venetoclax pharmacokinetics...
  21. Hu D, Marri S, McKinnon R, Mackenzie P, Meech R. Deregulation of the Genes that Are Involved in Drug Absorption, Distribution, Metabolism, and Excretion in Hepatocellular Carcinoma. J Pharmacol Exp Ther. 2019;368:363-381 pubmed publisher
    ..i>CYP2E1, CYP3A4, NAT1, NAT2, UGT2B7, SLC22A1, SLCO1B1, and SLCO1B3) were downregulated...
  22. Wanek T, Halilbasic E, Visentin M, Mairinger S, Römermann K, Stieger B, et al. Influence of 24-Nor-Ursodeoxycholic Acid on Hepatic Disposition of [(18)F]Ciprofloxacin, a Positron Emission Tomography Study in Mice. J Pharm Sci. 2016;105:106-12 pubmed publisher
    ..Transport experiments in organic anion transporting polypeptide (OATP)1B1-, OATP1B3-, and OATP2B1-transfected cells revealed weak transport of [(14)C]ciprofloxacin by OATP1B3 and OATP2B1 and no ..
  23. Krattinger R, Boström A, Schioth H, Thasler W, Mwinyi J, Kullak Ublick G. microRNA-192 suppresses the expression of the farnesoid X receptor. Am J Physiol Gastrointest Liver Physiol. 2016;310:G1044-51 pubmed publisher
    ..mRNA and protein levels as well as the mRNA levels of the FXR-inducible bile acid transporters OST?-OST? and OATP1B3. Significant inverse correlations were detected in colonic adenocarcinoma between NR1H4 mRNA and miR-192-3p ..
  24. Imada S, Kobayashi T, Kitao A, Matsui O, Hashimoto M, Ide K, et al. Central bisectionectomy for hepatocellular carcinoma in a patient with indocyanine green excretory defect associated with reduced expression of the liver transporter. Surg Case Rep. 2016;2:89 pubmed publisher
    ..site of the resected specimen showed very few expression of the organic anion-transporting polypeptide 1B3 (OATP1B3), which is usually expressed on the basolateral membrane of human hepatocytes and mediates the uptake of ICG...
  25. Bleasby K, Fillgrove K, Houle R, Lu B, Palamanda J, Newton D, et al. In Vitro Evaluation of the Drug Interaction Potential of Doravirine. Antimicrob Agents Chemother. 2019;63: pubmed publisher
    ..resistance protein (BCRP) and likely not a substrate of organic anion transporting polypeptide 1B1 (OATP1B1) or OATP1B3. Doravirine was not a reversible inhibitor of major CYP enzymes (CYP1A2, -2B6, -2C8, -2C9, -2C19, -2D6, and -3A4) ..
  26. Zhao Q, Liao R, Sun H, Zhang Z, Wang Q, Yang C, et al. Identifying Genetic Differences Between Dongxiang Blue-Shelled and White Leghorn Chickens Using Sequencing Data. G3 (Bethesda). 2018;8:469-476 pubmed publisher
    ..The most significantly selected genes in Blue-shelled chicken are TMEM141 and CLIC3, while the SLCO1B3 gene, related to eggshell color, was identified via EigenGWAS...
  27. 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
    ..In humans, OATP-B and OATP8 do not appear to transport GSH; however, other members of this family have yet to be characterized in regards to ..
  28. Melchardt T, Hufnagl C, Magnes T, Weiss L, Hutarew G, Neureiter D, et al. CYP39A1 polymorphism is associated with toxicity during intensive induction chemotherapy in patients with advanced head and neck cancer. BMC Cancer. 2015;15:725 pubmed publisher
    ..rs1799793, ERCC1-rs3212986, rs11615, XRCC1-rs25487) or with docetaxel caused toxicity (CYP39A1-rs7761731, SLCO1B3-rs11045585) were evaluated in all patients...
  29. Edwards J, Eliot L, Parkinson A, Karan S, MacConell L. Assessment of Pharmacokinetic Interactions Between Obeticholic Acid and Caffeine, Midazolam, Warfarin, Dextromethorphan, Omeprazole, Rosuvastatin, and Digoxin in Phase 1 Studies in Healthy Subjects. Adv Ther. 2017;34:2120-2138 pubmed publisher
    ..CYP2C9 (S-warfarin), CYP2D6 (dextromethorphan), CYP2C19 (omeprazole), and drug transporters, BCRP/OATP1B1/OATP1B3 (rosuvastatin), and P-gp (digoxin)...
  30. Briz O, Romero M, Martinez Becerra P, Macias R, Perez M, Jimenez F, et al. OATP8/1B3-mediated cotransport of bile acids and glutathione: an export pathway for organic anions from hepatocytes?. J Biol Chem. 2006;281:30326-35 pubmed
    ..Expression of OATP8/1B3 enhanced CA efflux, which was trans-activated by taurocholate but trans-inhibited by reduced (GSH) and ..
  31. Ieiri I, Higuchi S, Sugiyama Y. Genetic polymorphisms of uptake (OATP1B1, 1B3) and efflux (MRP2, BCRP) transporters: implications for inter-individual differences in the pharmacokinetics and pharmacodynamics of statins and other clinically relevant drugs. Expert Opin Drug Metab Toxicol. 2009;5:703-29 pubmed publisher
    ..Organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 are uptake transporters, specifically expressed in the liver, and considered important for drugs, particularly as ..
  32. Suga T, Yamaguchi H, Sato T, Maekawa M, Goto J, Mano N. Preference of Conjugated Bile Acids over Unconjugated Bile Acids as Substrates for OATP1B1 and OATP1B3. PLoS ONE. 2017;12:e0169719 pubmed publisher
    ..Human organic anion-transporting polypeptides (OATP) 1B1 and OATP1B3 contribute to hepatic uptake of bile acids such as taurocholic acid...
  33. Shitara Y, Sugiyama Y. Preincubation-dependent and long-lasting inhibition of organic anion transporting polypeptide (OATP) and its impact on drug-drug interactions. Pharmacol Ther. 2017;177:67-80 pubmed publisher
    ..with cyclosporin A (CsA), a potent inhibitor of organic anion transporting polypeptide 1B1 (OATP1B1) and OATP1B3, enhanced its inhibitory effects on these transporters in vitro...
  34. Walker A, Franke R, Sparreboom A, Ware R. Transcellular movement of hydroxyurea is mediated by specific solute carrier transporters. Exp Hematol. 2011;39:446-56 pubmed publisher
    ..Further characterization of hydroxyurea transport revealed that cellular uptake by OATP1B3 is time- and temperature-dependent and inhibited by known substrates of OATP1B3...
  35. Sticova E, Lodererova A, van de Steeg E, Frankova S, Kollar M, Lanska V, et al. Down-regulation of OATP1B proteins correlates with hyperbilirubinemia in advanced cholestasis. Int J Clin Exp Pathol. 2015;8:5252-62 pubmed
    Organic anion-transporting polypeptides OATP1B1 and OATP1B3 are sinusoidal membrane transporters mediating liver uptake of a wide range of substrates including conjugated and unconjugated bilirubin, xenobiotics and drugs...
  36. 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
    ..The objective of this study was to define the distribution of SNPs of three SLCO genes, SLCO1B1, SLCO1B3, and SLCO2B1, in a Korean population and other ethnic groups...
  37. Brännström M, Nordell P, Bonn B, Davis A, Palmgren A, Hilgendorf C, et al. Montelukast Disposition: No Indication of Transporter-Mediated Uptake in OATP2B1 and OATP1B1 Expressing HEK293 Cells. Pharmaceutics. 2015;7:554-64 pubmed publisher
    ..Montelukast is a carboxylic acid, a relatively potent inhibitor of OATP1B1, OATP1B3, and OATP2B1, and has previously been postulated to be actively transported into human hepatocytes...
  38. Arita Y, Allen S, Chen G, Zhang W, Wang Y, Owen A, et al. Rapid isolation of peptidic inhibitors of the solute carrier family transporters OATP1B1 and OATP1B3 by cell-based phage display selections. Biochem Biophys Res Commun. 2016;473:370-6 pubmed publisher
    OATP1B1 and OATP1B3 (1B3) are members of organic anion-transporting polypeptides (OATPs), a family of sodium-independent organic anion membrane transporters that contribute to transport of various drugs...
  39. Tan S, Wong M, Tiew A, Choo Y, Lim S, Ooi I, et al. Sunitinib DDI with paracetamol, diclofenac, mefenamic acid and ibuprofen shows sex-divergent effects on the tissue uptake and distribution pattern of sunitinib in mice. Cancer Chemother Pharmacol. 2016;78:709-18 pubmed publisher
    ..paracetamol, mefenamic acid and ibuprofen was evaluated due to their P450 mediated metabolism and OATP1B1, OATP1B3, ABCB1, ABCG2 transporters overlapping features...
  40. Santana Machado T, Poitevin S, Paul P, McKay N, Jourde Chiche N, Legris T, et al. Indoxyl Sulfate Upregulates Liver P-Glycoprotein Expression and Activity through Aryl Hydrocarbon Receptor Signaling. J Am Soc Nephrol. 2018;29:906-918 pubmed publisher
    ..involved in drug clearance: SLC10A1, SLC22A1, SLC22A7, SLC47A1, SLCO1B1, SLCO1B3, SLCO2B1, ABCB1, ABCB11, ABCC2, ABCC3, ABCC4, ABCC6, and ..
  41. 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
    ..The polymorphisms from UGT1A1 (rs8175347), SLCO1B1 (rs4149056 and rs2306283), and SLCO1B3 (rs17680137 and rs2117032) were analyzed by capillary electrophoresis and hydrolysis probes...
  42. Riha J, Brenner S, Srovnalova A, Klameth L, Dvorak Z, Jäger W, et al. Effects of anthocyans on the expression of organic anion transporting polypeptides (SLCOs/OATPs) in primary human hepatocytes. Food Funct. 2015;6:772-9 pubmed publisher
    ..of widely used drugs such as statins and some anticancer drugs is mediated by the liver-specific OATP1B1 and OATP1B3, thus any interference with expression of these particular transporters might influence therapeutic outcomes...
  43. Burt H, Riedmaier A, Harwood M, Crewe H, Gill K, Neuhoff S. Abundance of Hepatic Transporters in Caucasians: A Meta-Analysis. Drug Metab Dispos. 2016;44:1550-61 pubmed publisher
    ..Organic anion transporting polypeptides OATP1B1 and OATP1B3 showed the highest population abundance in healthy adult Caucasians...
  44. Hagenbuch B, Meier P. Organic anion transporting polypeptides of the OATP/ SLC21 family: phylogenetic classification as OATP/ SLCO superfamily, new nomenclature and molecular/functional properties. Pflugers Arch. 2004;447:653-65 pubmed
  45. Leskela S, Jara C, Leandro García L, Martinez A, Garcia Donas J, Hernando S, et al. Polymorphisms in cytochromes P450 2C8 and 3A5 are associated with paclitaxel neurotoxicity. Pharmacogenomics J. 2011;11:121-9 pubmed publisher
    ..enzymes (CYP2C8, CYP3A4 and CYP3A5) and transporters (organic anion transporting polypeptide (OATP) 1B1, OATP1B3 and P-glycoprotein) and genotyped them in 118 Spanish cancer patients treated with paclitaxel...
  46. Svoboda M, Wlcek K, Taferner B, Hering S, Stieger B, Tong D, et al. Expression of organic anion-transporting polypeptides 1B1 and 1B3 in ovarian cancer cells: relevance for paclitaxel transport. Biomed Pharmacother. 2011;65:417-26 pubmed publisher
    ..Cytotoxicity of paclitaxel in OVCAR-3, SK-OV-3 and OATP1B1- and OATP1B3-transfected SK-OV-3 cells was performed using the CellTiter-Glo assay...
  47. Yoneda N, Matsui O, Ikeno H, Inoue D, Yoshida K, Kitao A, et al. Correlation between Gd-EOB-DTPA-enhanced MR imaging findings and OATP1B3 expression in chemotherapy-associated sinusoidal obstruction syndrome. Abdom Imaging. 2015;40:3099-103 pubmed publisher
    ..on the findings of gadoxetic acid-enhanced MRI (EOB-MRI) and the organic anion transporting polypeptide 1B3 (OATP1B3) expression of in the liver. The patient was a 75-year-old female...
  48. Gruetz M, Sticht H, Glaeser H, Fromm M, Konig J. Analysis of amino acid residues in the predicted transmembrane pore influencing transport kinetics of the hepatic drug transporter organic anion transporting polypeptide 1B1 (OATP1B1). Biochim Biophys Acta. 2016;1858:2894-2902 pubmed publisher
    The hepatic uptake transporters OATP1B1 (SLCO1B1) and OATP1B3 (SLCO1B3) mediate the uptake of endogenous metabolites and drugs from blood into hepatocytes...
  49. Alam K, Farasyn T, Crowe A, Ding K, Yue W. Treatment with proteasome inhibitor bortezomib decreases organic anion transporting polypeptide (OATP) 1B3-mediated transport in a substrate-dependent manner. PLoS ONE. 2017;12:e0186924 pubmed publisher
    OATP1B1 and OATP1B3 mediate hepatic uptake of many drugs (e.g., statins) and can mediate transporter-mediated drug-drug-interactions (DDIs). Bortezomib is the first-in-class proteasome inhibitor drug approved by the U. S...
  50. Kellick K. Organic Ion Transporters and Statin Drug Interactions. Curr Atheroscler Rep. 2017;19:65 pubmed publisher
    ..to one drug transport system, the organic anion-transporting polypeptides (OATPs) specifically OATP1B1 and OATP1B3. Since the publication of the discovery of OATPs, there have been various pharmacokinetic models that have been ..
  51. Vavricka S, Jung D, Fried M, Grutzner U, Meier P, Kullak Ublick G. The human organic anion transporting polypeptide 8 (SLCO1B3) gene is transcriptionally repressed by hepatocyte nuclear factor 3beta in hepatocellular carcinoma. J Hepatol. 2004;40:212-8 pubmed
    ..Our aim was to study the expression and regulation of OATP8 (OATP1B3, SLC21A8/SLCO1B3) and OATP-C (OATP1B1, SLC21A6/SLCO1B1) in hepatocellular carcinomas (HCC)...
  52. Ohtsuka H, Abe T, Onogawa T, Kondo N, Sato T, Oshio H, et al. Farnesoid X receptor, hepatocyte nuclear factors 1alpha and 3beta are essential for transcriptional activation of the liver-specific organic anion transporter-2 gene. J Gastroenterol. 2006;41:369-77 pubmed
    We isolated the human liver-specific organic anion transporter gene, LST-2 (OATP8/SLCO1B3), which is exclusively expressed in the basolateral membrane of the hepatocytes...
  53. Eng H, Scialis R, Rotter C, Lin J, Lazzaro S, Varma M, et al. The Antimicrobial Agent Fusidic Acid Inhibits Organic Anion Transporting Polypeptide-Mediated Hepatic Clearance and May Potentiate Statin-Induced Myopathy. Drug Metab Dispos. 2016;44:692-9 pubmed publisher
    ..CYP3A4 and clinically relevant drug transporters such as organic anion transporting polypeptides OATP1B1 and OATP1B3, multidrug resistant protein 1, and breast cancer resistance protein, which are involved in the oral absorption ..
  54. Cai L, Huang W, Su Z, Ye H, Wang L, Wu Y, et al. Identification of two novel genes SLC15A2 and SLCO1B3 associated with maintenance dose variability of warfarin in a Chinese population. Sci Rep. 2017;7:17379 pubmed publisher
    ..confirmed that the common variant rs9923231 in VKORC1 and two novel genes, SLC15A2 (rs1143671 and rs1143672) and SLCO1B3 (rs4149117 and rs7311358), are associated with the warfarin maintenance dose...
  55. You H, Lee K, Lee S, Hwang S, Kim K, Cho K, et al. Computational classification models for predicting the interaction of compounds with hepatic organic ion importers. Drug Metab Pharmacokinet. 2015;30:347-51 pubmed publisher
    ..a hepatic transporter with experimental data of 284 compounds for four representative hepatic importers, OATP1B1, OATP1B3, OAT2, and OCT1...
  56. Sayyed K, Vee M, Abdel Razzak Z, Jouan E, Stieger B, Denizot C, et al. Alteration of human hepatic drug transporter activity and expression by cigarette smoke condensate. Toxicology. 2016;363-364:58-71 pubmed publisher
    ..CSC thus directly inhibited activities of sinusoidal transporters such as OATP1B1, OATP1B3, OCT1 and NTCP as well as those of canalicular transporters like P-glycoprotein, MRP2, BCRP and MATE1, in hepatic ..
  57. Lee H, Leake B, Kim R, Ho R. Contribution of Organic Anion-Transporting Polypeptides 1A/1B to Doxorubicin Uptake and Clearance. Mol Pharmacol. 2017;91:14-24 pubmed
    ..vaccinia-based method for expressing uptake transporters in HeLa cells revealed that OATP1A2, but not OATP1B1 or OATP1B3, and the rat ortholog Oatp1a4 were capable of significant doxorubicin uptake...
  58. Zhang Y, Boxberger K, Hagenbuch B. Organic anion transporting polypeptide 1B3 can form homo- and hetero-oligomers. PLoS ONE. 2017;12:e0180257 pubmed publisher
    b>OATP1B3 is a 12 transmembrane domain protein expressed at the basolateral membrane of human hepatocytes where it mediates the uptake of numerous drugs and endogenous compounds...
  59. Oh Y, Jeong Y, Kim M, Min J, Ryoo G, Park J, et al. Inhibition of Organic Anion Transporting Polypeptide 1B1 and 1B3 by Betulinic Acid: Effects of Preincubation and Albumin in the Media. J Pharm Sci. 2018;107:1713-1723 pubmed publisher
    ..Preincubation (incubation with inhibitors, followed by washout) with BA led to a sustained inhibition of OATP1B3, which recovered rapidly in the media containing 10% fetal bovine serum...
  60. Sharifi N, Hamada A, Sissung T, Danesi R, Venzon D, Baum C, et al. A polymorphism in a transporter of testosterone is a determinant of androgen independence in prostate cancer. BJU Int. 2008;102:617-21 pubmed publisher
  61. Woo S, Gardner E, Chen X, Ockers S, Baum C, Sissung T, et al. Population pharmacokinetics of romidepsin in patients with cutaneous T-cell lymphoma and relapsed peripheral T-cell lymphoma. Clin Cancer Res. 2009;15:1496-503 pubmed publisher
    ..a nonlinear mixed effects modeling approach to explore the effects of polymorphic variations in CYP3A4, CYP3A5, SLCO1B3, and ABCB1, all of which encode genes thought to be involved in romidepsin disposition...
  62. Wang M, Qi H, Li J, Xu Y, Zhang H. Transmembrane transport of steviol glucuronide and its potential interaction with selected drugs and natural compounds. Food Chem Toxicol. 2015;86:217-24 pubmed publisher
    ..In contrast, OAT3 played a predominant role in the uptake of SVG in comparison to OATP1B1, OATP1B3, or OATP2B1...
  63. Johnson M, Patel D, Matheny C, Ho M, Chen L, Ellens H. Inhibition of Intestinal OATP2B1 by the Calcium Receptor Antagonist Ronacaleret Results in a Significant Drug-Drug Interaction by Causing a 2-Fold Decrease in Exposure of Rosuvastatin. Drug Metab Dispos. 2017;45:27-34 pubmed
    ..but is an in vitro substrate of multiple transporters [organic anion transporting polypeptide 1B1 (OATP1B1), OATP1B3, OATP1A2, OATP2B1, sodium-taurocholate cotransporting polypeptide, breast cancer resistance protein (BCRP), ..
  64. Ellens H, Johnson M, Lawrence S, Watson C, Chen L, Richards Peterson L. Prediction of the Transporter-Mediated Drug-Drug Interaction Potential of Dabrafenib and Its Major Circulating Metabolites. Drug Metab Dispos. 2017;45:646-656 pubmed publisher
    ..were investigated as inhibitors of the clinically relevant transporters P-gp, BCRP, OATP1B1, OATP1B3, OCT2, OAT1, and OAT3...
  65. Yamaguchi H, Kobayashi M, Okada M, Takeuchi T, Unno M, Abe T, et al. Rapid screening of antineoplastic candidates for the human organic anion transporter OATP1B3 substrates using fluorescent probes. Cancer Lett. 2008;260:163-9 pubmed
    ..b>OATP1B3 is abundantly expressed in solid digestive organ cancers...
  66. Hirano M, Maeda K, Shitara Y, Sugiyama Y. Contribution of OATP2 (OATP1B1) and OATP8 (OATP1B3) to the hepatic uptake of pitavastatin in humans. J Pharmacol Exp Ther. 2004;311:139-46 pubmed
    ..study, we investigated the contribution of organic anion transporting polypeptide 2 (OATP2/OATP1B1) and OATP8 (OATP1B3) to pitavastatin uptake using transporter-expressing HEK293 cells and human cryopreserved hepatocytes...
  67. Fujino H, Saito T, Ogawa S, Kojima J. Transporter-mediated influx and efflux mechanisms of pitavastatin, a new inhibitor of HMG-CoA reductase. J Pharm Pharmacol. 2005;57:1305-11 pubmed
    ..The acid form of pitavastatin was shown to be a substrate for human OATP1, OATP2, OATP8, OAT3 and NTCP, and for rat Oatp1 and Oatp4 with relatively low K(m) values...
  68. Sekine S, Ogawa R, Ojima H, Kanai Y. Expression of SLCO1B3 is associated with intratumoral cholestasis and CTNNB1 mutations in hepatocellular carcinoma. Cancer Sci. 2011;102:1742-7 pubmed publisher
    ..Among the genes involved in bile acid and bilirubin transport, the expression of SLCO1B3 was significantly elevated in HCC with CTNNB1 mutations, whereas the expression of ABCC4 was elevated in HCC with ..
  69. Chew S, Sandanaraj E, Singh O, Chen X, Tan E, Lim W, et al. Influence of SLCO1B3 haplotype-tag SNPs on docetaxel disposition in Chinese nasopharyngeal cancer patients. Br J Clin Pharmacol. 2012;73:606-18 pubmed publisher
    b>SLCO1B3 is an influx transporter located at the hepatocyte basolateral membrane and it is involved in the uptake of a broad range of drug substrates including docetaxel...
  70. Testa A, Dall Angelo S, Mingarelli M, Augello A, Schweiger L, Welch A, et al. Design, synthesis, in vitro characterization and preliminary imaging studies on fluorinated bile acid derivatives as PET tracers to study hepatic transporters. Bioorg Med Chem. 2017;25:963-976 pubmed publisher
    ..In addition, the lead compound, LCATD (4c), was tested as a substrate of other liver uptake transporters OATP1B3, NTCP and efflux transporter BSEP to evaluate its specificity of liver transport...
  71. Kullak Ublick G, Ismair M, Stieger B, Landmann L, Huber R, Pizzagalli F, et al. Organic anion-transporting polypeptide B (OATP-B) and its functional comparison with three other OATPs of human liver. Gastroenterology. 2001;120:525-33 pubmed
    ..and hepatocellular localization and to compare its substrate specificity with those of OATP-A, OATP-C, and OATP8. Tissue distribution and hepatocellular localization of OATP-B were analyzed by Northern blotting and ..
  72. 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
    ..h L g, respectively (P = 0.03004 in multivariate analysis). The median dose-adjusted AUC0-12 of MPAG in SLCO1B3 334T/T+T/G (699G/G+G/A, n = 46) and 334G/G (699A/A, n = 34) was 1191 and 1580 mg.h L g, respectively (P = 0...
  73. Wright J, Kwon E, Ostrander E, Montgomery R, Lin D, Vessella R, et al. Expression of SLCO transport genes in castration-resistant prostate cancer and impact of genetic variation in SLCO1B3 and SLCO2B1 on prostate cancer outcomes. Cancer Epidemiol Biomarkers Prev. 2011;20:619-27 pubmed publisher
    ..whether prostate cancer outcomes are associated with single nucleotide polymorphisms (SNP) in SLCO2B1 and SLCO1B3, transporters previously shown to mediate androgen uptake...
  74. Endo S, Fukahori A, Tokuhiro S, Shinagawa A, Walker J, Yoshihara K, et al. Association study of genetic polymorphisms of drug transporters, SLCO1B1, SLCO1B3 and ABCC2, in African-Americans, Hispanics and Caucasians and olmesartan exposure. J Hum Genet. 2012;57:531-44 pubmed publisher
    ..We investigated the association of SLCO1B1, SLCO1B3 and ABCC2 polymorphisms with the pharmacokinetics of olmesartan...
  75. Ren Q, Han X, Ren J, Liu X, Ji L. Influence of the SLCO1B3 Gene on Sulfonylurea Failure in Patients with Type 2 Diabetes in China. Exp Clin Endocrinol Diabetes. 2017;125:449-453 pubmed publisher
    ..Recent research has demonstrated that SLCO1B3 functions as a determinant of the insulinotropic effect of glibenclamide at the tissue level...
  76. Jiang P, Zhang X, Huang Y, Cheng N, Ma Y. Hepatotoxicity Induced by Sophora flavescens and Hepatic Accumulation of Kurarinone, a Major Hepatotoxic Constituent of Sophora flavescens in Rats. Molecules. 2017;22: pubmed publisher
    ..5 g/kg). Active uptake of kurarinone and kurarinone glucuronides was studied in OAT2-, OATP1B1-, OATP2B1-, and OATP1B3-transfected HEK293 cells...
  77. Takanohashi T, Kubo S, Arisaka H, Shinkai K, Ubukata K. Contribution of organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 to hepatic uptake of nateglinide, and the prediction of drug-drug interactions via these transporters. J Pharm Pharmacol. 2012;64:199-206 pubmed publisher
    We have investigated the contributions of organic anion transporting polypeptide (OATP) 1B1 and OATP1B3 to the hepatic uptake of nateglinide, and the possibility of drug-drug interactions via these transporters...
  78. Zhao W, Zitzow J, Weaver Y, Ehresman D, Chang S, Butenhoff J, et al. Organic Anion Transporting Polypeptides Contribute to the Disposition of Perfluoroalkyl Acids in Humans and Rats. Toxicol Sci. 2017;156:84-95 pubmed publisher
    ..We used CHO and HEK293 cells to demonstrate that human OATP1B1, OATP1B3, and OATP2B1 can transport PFBS, PFHxS, PFOS, and the 2 PFCAs (C8 and C9)...
  79. Anderson M, Cote J, Liu Y, Stypinski D, Auger P, Hohnstein A, et al. Effects of Rifampin, a potent inducer of drug-metabolizing enzymes and an inhibitor of OATP1B1/3 transport, on the single dose pharmacokinetics of anacetrapib. J Clin Pharmacol. 2013;53:746-52 pubmed publisher
  80. Miura M, Satoh S, Inoue K, Kagaya H, Saito M, Inoue T, et al. Influence of SLCO1B1, 1B3, 2B1 and ABCC2 genetic polymorphisms on mycophenolic acid pharmacokinetics in Japanese renal transplant recipients. Eur J Clin Pharmacol. 2007;63:1161-9 pubmed
    ..dose-adjusted area under the cuve (AUC)(6-12) of MPA, an estimate of enterohepatic recirculation, was greater in SLCO1B3 T334G GG (or G699A AA) carriers than in TT carriers (or G699A GG) (40 vs...
  81. Wlcek K, Koller F, Ferenci P, Stieger B. Hepatocellular organic anion-transporting polypeptides (OATPs) and multidrug resistance-associated protein 2 (MRP2) are inhibited by silibinin. Drug Metab Dispos. 2013;41:1522-8 pubmed publisher
    ..activity of the hepatocellular uptake transporters organic anion-transporting polypeptides (OATPs) OATP1B1, OATP1B3, and OATP2B1, as well as Na(+)-taurocholate cotransporting polypeptide (NTCP) and of the efflux transporters ..
  82. Nambu T, Hamada A, Nakashima R, Yuki M, Kawaguchi T, Mitsuya H, et al. Association of SLCO1B3 polymorphism with intracellular accumulation of imatinib in leukocytes in patients with chronic myeloid leukemia. Biol Pharm Bull. 2011;34:114-9 pubmed
    ..ABCG2, solute carrier 22A1 (SLC22A1), solute carrier organic anion transporter family members 1B1 (SLCO1B1) and SLCO1B3. The imatinib levels in leukocytes were determined using HPLC in 15 patients with chronic phase CML...
  83. Geng F, Jiao Z, Dao Y, Qiu X, Ding J, Shi X, et al. The association of the UGT1A8, SLCO1B3 and ABCC2/ABCG2 genetic polymorphisms with the pharmacokinetics of mycophenolic acid and its phenolic glucuronide metabolite in Chinese individuals. Clin Chim Acta. 2012;413:683-90 pubmed publisher
    This study aimed to evaluate the effect of UGT1A8*2, SLCO1B3 T334G, ABCC2 C-24T and ABCG2 C421A polymorphisms on the pharmacokinetics (PKs) of mycophenolic acid (MPA) and its phenolic glucuronide (MPAG) in healthy Chinese volunteers and ..
  84. Chun S, Thakkar N, Oh Y, Park J, Han S, Ryoo G, et al. The N-terminal region of organic anion transporting polypeptide 1B3 (OATP1B3) plays an essential role in regulating its plasma membrane trafficking. Biochem Pharmacol. 2017;131:98-105 pubmed publisher
    Organic anion transporting polypeptide 1B3 (OATP1B3) is a major influx transporter mediating the hepatic uptake of various endogenous substrates as well as clinically important drugs such as statins and anticancer drugs...
  85. Kumar V, Nguyen T, Tóth B, Juhász V, Unadkat J. Optimization and Application of a Biotinylation Method for Quantification of Plasma Membrane Expression of Transporters in Cells. AAPS J. 2017;19:1377-1386 pubmed publisher
    ..7% (±12.2%), and 65.3% (±6.8%) of total cell OATP1B1 expression. Mean (±SD) plasma membrane expression of OATP1B3 in plated OATP1B3-expressing HEK293 cells, OATP2B1 in plated OATP2B1-expressing MDCKII cells, and sodium/..
  86. Yamakawa Y, Hamada A, Nakashima R, Yuki M, Hirayama C, Kawaguchi T, et al. Association of genetic polymorphisms in the influx transporter SLCO1B3 and the efflux transporter ABCB1 with imatinib pharmacokinetics in patients with chronic myeloid leukemia. Ther Drug Monit. 2011;33:244-50 pubmed publisher
    ..of 14 single nucleotide polymorphisms in three genes coding for influx transporters (SLC22A1, SLCO1B1, and SLCO1B3), two genes coding for efflux transporters (ABCB1 and ABCG2), and four genes coding for enzymes (CYP2C9, CYP2C19, ..
  87. Sissung T, Ley A, Strope J, McCrea E, Beedie S, Peer C, et al. Differential Expression of OATP1B3 Mediates Unconjugated Testosterone Influx. Mol Cancer Res. 2017;15:1096-1105 pubmed publisher
    ..functional, and clinical relevance of de novo expression of the steroid hormone transporter OATP1B3 (SLCO1B3)...
  88. Shitara Y, Takeuchi K, Nagamatsu Y, Wada S, Sugiyama Y, Horie T. Long-lasting inhibitory effects of cyclosporin A, but not tacrolimus, on OATP1B1- and OATP1B3-mediated uptake. Drug Metab Pharmacokinet. 2012;27:368-78 pubmed
    Cyclosporin A (CsA) causes a number of clinically relevant drug-drug interactions (DDIs) by inhibiting OATP1B1 and OATP1B3. In the present study, long-lasting inhibitory effects of CsA on these transporters were examined in comparison to ..
  89. 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
    The human organic anion-transporting polypeptides OATP1B1 (SLCO1B1) and OATP1B3 (SLCO1B3) are liver-enriched membrane transporters of major importance to hepatic uptake of numerous endogenous compounds, including bile acids, steroid ..
  90. Imai S, Kikuchi R, Tsuruya Y, Naoi S, Nishida S, Kusuhara H, et al. Epigenetic regulation of organic anion transporting polypeptide 1B3 in cancer cell lines. Pharm Res. 2013;30:2880-90 pubmed publisher
    The expression of a multispecific organic anion transporter, OATP1B3/SLCO1B3, is associated with clinical prognosis and survival of cancer cells...
  91. Bachmakov I, Glaeser H, Fromm M, Konig J. Interaction of oral antidiabetic drugs with hepatic uptake transporters: focus on organic anion transporting polypeptides and organic cation transporter 1. Diabetes. 2008;57:1463-9 pubmed publisher
    ..Using stably transfected cell systems recombinantly expressing the uptake transporters OATP1B1, OATP1B3, OATP2B1, or OCT1, we analyzed whether the antidiabetic drugs repaglinide, rosiglitazone, or metformin influence ..