SLCO1B1

Summary

Gene Symbol: SLCO1B1
Description: solute carrier organic anion transporter family member 1B1
Alias: HBLRR, LST-1, LST1, OATP-C, OATP1B1, OATP2, OATPC, SLC21A6, solute carrier organic anion transporter family member 1B1, OATP-2, liver-specific organic anion transporter 1, sodium-independent organic anion-transporting polypeptide 2, solute carrier family 21 (organic anion transporter), member 6
Species: human

Top Publications

  1. ncbi Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European- and African-Americans
    R G Tirona
    Division of Clinical Pharmacology, Departments of Medicine and Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6602, USA
    J Biol Chem 276:35669-75. 2001
  2. ncbi Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier
    Kimio Tohyama
    Department of Molecular Pharmacokinetics, Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo 113 0033, Japan
    Endocrinology 145:4384-91. 2004
  3. doi Interaction of oral antidiabetic drugs with hepatic uptake transporters: focus on organic anion transporting polypeptides and organic cation transporter 1
    Iouri Bachmakov
    Institute of Experimental and Clinical Pharmacology and Toxicology, Friedrich Alexander University Erlangen Nuremberg, Erlangen, Germany
    Diabetes 57:1463-9. 2008
  4. ncbi Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1
    T Abe
    Department of Neurophysiology, Tohoku University School of Medicine, Sendai, 980 8575, Tokyo, 140 8710, Japan
    J Biol Chem 274:17159-63. 1999
  5. ncbi A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane
    J Konig
    Division of Tumor Biochemistry, Deutsches Krebsforschungszentrum, D 69120 Heidelberg, Germany
    Am J Physiol Gastrointest Liver Physiol 278:G156-64. 2000
  6. ncbi Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide
    J Konig
    Division of Tumor Biochemistry, Deutsches Krebsforschungszentrum, D 69120 Heidelberg, Germany
    J Biol Chem 275:23161-8. 2000
  7. ncbi Genetic polymorphisms of human organic anion transporters OATP-C (SLC21A6) and OATP-B (SLC21A9): allele frequencies in the Japanese population and functional analysis
    Takashi Nozawa
    Division of Molecular Biopharmaceutics, Faculty of Pharmaceutical Sciences, Kanazawa University, 13 1 Takara machi, Kanazawa 920 0934, Japan
    J Pharmacol Exp Ther 302:804-13. 2002
  8. ncbi Polymorphisms of OATP-C (SLC21A6) and OAT3 (SLC22A8) genes: consequences for pravastatin pharmacokinetics
    Yohei Nishizato
    Division of Pharmaceutical Sciences, Department of Clinical Pharmacokinetics, Graduate School, Kyushu University, Fukuoka, Japan
    Clin Pharmacol Ther 73:554-65. 2003
  9. ncbi Evidence for inverse effects of OATP-C (SLC21A6) 5 and 1b haplotypes on pravastatin kinetics
    Jessica Mwinyi
    Institute of Clinical Pharmacology, Humboldt University, Berlin, Germany
    Clin Pharmacol Ther 75:415-21. 2004
  10. ncbi High plasma pravastatin concentrations are associated with single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide-C (OATP-C, SLCO1B1)
    Mikko Niemi
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
    Pharmacogenetics 14:429-40. 2004

Research Grants

  1. Wei Yue; Fiscal Year: 2015
  2. HEPATIC DRUG TRANSPORTERS IN DRUG DISPOSITION
    Dan Roden; Fiscal Year: 2006
  3. Bruno Hagenbuch; Fiscal Year: 2016
  4. Swati Nagar; Fiscal Year: 2016
  5. Ivan Csanaky; Fiscal Year: 2014
  6. RICHARD HSINSHIN HO; Fiscal Year: 2016
  7. Bruce M Psaty; Fiscal Year: 2015
  8. Genetic Risk Stratification to Identify Individuals for Early Statin Therapy
    Marc S Sabatine; Fiscal Year: 2010
  9. FUNCTIONS OF THE HEPATIC GAMMA-GLUTAMYL CYCLE
    Nazzareno Ballatori; Fiscal Year: 2007
  10. Genetic and Epigenetic Regulation of Addiction Genes
    Wolfgang Sadee; Fiscal Year: 2010

Detail Information

Publications219 found, 100 shown here

  1. ncbi Polymorphisms in OATP-C: identification of multiple allelic variants associated with altered transport activity among European- and African-Americans
    R G Tirona
    Division of Clinical Pharmacology, Departments of Medicine and Pharmacology, Vanderbilt University School of Medicine, Nashville, Tennessee 37232 6602, USA
    J Biol Chem 276:35669-75. 2001
    The human organic anion transporting polypeptide-C (OATP-C) (gene SLC21A6) is a liver-specific transporter importantly involved in the hepatocellular uptake of a variety of endogenous and foreign chemicals...
  2. ncbi Involvement of multispecific organic anion transporter, Oatp14 (Slc21a14), in the transport of thyroxine across the blood-brain barrier
    Kimio Tohyama
    Department of Molecular Pharmacokinetics, Graduate School of Pharmaceutical Sciences, The University of Tokyo, 7 3 1 Hongo, Bunkyo ku, Tokyo 113 0033, Japan
    Endocrinology 145:4384-91. 2004
    ..probenecid, and estrone-3-sulfate were moderate inhibitors for mOatp14, whereas digoxin (substrate of Oatp2), benzylpenicillin (substrate of Oat3), and large neutral amino acids had no effect...
  3. doi Interaction of oral antidiabetic drugs with hepatic uptake transporters: focus on organic anion transporting polypeptides and organic cation transporter 1
    Iouri Bachmakov
    Institute of Experimental and Clinical Pharmacology and Toxicology, Friedrich Alexander University Erlangen Nuremberg, Erlangen, Germany
    Diabetes 57:1463-9. 2008
    ....
  4. ncbi Identification of a novel gene family encoding human liver-specific organic anion transporter LST-1
    T Abe
    Department of Neurophysiology, Tohoku University School of Medicine, Sendai, 980 8575, Tokyo, 140 8710, Japan
    J Biol Chem 274:17159-63. 1999
    ..This is also the first report of the human molecule that transports thyroid hormones...
  5. ncbi A novel human organic anion transporting polypeptide localized to the basolateral hepatocyte membrane
    J Konig
    Division of Tumor Biochemistry, Deutsches Krebsforschungszentrum, D 69120 Heidelberg, Germany
    Am J Physiol Gastrointest Liver Physiol 278:G156-64. 2000
    ..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...
  6. ncbi Localization and genomic organization of a new hepatocellular organic anion transporting polypeptide
    J Konig
    Division of Tumor Biochemistry, Deutsches Krebsforschungszentrum, D 69120 Heidelberg, Germany
    J Biol Chem 275:23161-8. 2000
    Based on sequence homology to the human organic anion transporting polypeptide 2 (OATP2; SLC21A6), we cloned a new member of the SLC21A superfamily of solute carriers, termed OATP8 (SLC21A8)...
  7. ncbi Genetic polymorphisms of human organic anion transporters OATP-C (SLC21A6) and OATP-B (SLC21A9): allele frequencies in the Japanese population and functional analysis
    Takashi Nozawa
    Division of Molecular Biopharmaceutics, Faculty of Pharmaceutical Sciences, Kanazawa University, 13 1 Takara machi, Kanazawa 920 0934, Japan
    J Pharmacol Exp Ther 302:804-13. 2002
    Genetic polymorphisms of human organic anion transporting polypeptides OATP-C (SLC21A6) and OATP-B (SLC21A9) in the Japanese population were analyzed...
  8. ncbi Polymorphisms of OATP-C (SLC21A6) and OAT3 (SLC22A8) genes: consequences for pravastatin pharmacokinetics
    Yohei Nishizato
    Division of Pharmaceutical Sciences, Department of Clinical Pharmacokinetics, Graduate School, Kyushu University, Fukuoka, Japan
    Clin Pharmacol Ther 73:554-65. 2003
    ....
  9. ncbi Evidence for inverse effects of OATP-C (SLC21A6) 5 and 1b haplotypes on pravastatin kinetics
    Jessica Mwinyi
    Institute of Clinical Pharmacology, Humboldt University, Berlin, Germany
    Clin Pharmacol Ther 75:415-21. 2004
    ..We compared the pharmacogenetic effects of OATP-C (organic anion transporting polypeptide C) *1a, *1b (A388G), and *5 (T521C) haplotypes on single-dose pharmacokinetics of pravastatin in white subjects...
  10. ncbi High plasma pravastatin concentrations are associated with single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide-C (OATP-C, SLCO1B1)
    Mikko Niemi
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
    Pharmacogenetics 14:429-40. 2004
    ..between polymorphisms in the drug transporter genes organic anion transporting polypeptide-C (OATP-C, SLCO1B1), OATP-B (SLCO2B1), multidrug resistance-associated protein 2 (MRP2, ABCC2) and multidrug resistance transporter (..
  11. ncbi Effect of OATP1B1 (SLCO1B1) variant alleles on the pharmacokinetics of pitavastatin in healthy volunteers
    Jae Yong Chung
    Department of Pharmacology and Clinical Pharmacology Unit, Seoul National University College of Medicine and Hospital, and Choongwae Pharma
    Clin Pharmacol Ther 78:342-50. 2005
    ..We characterized the effects of organic anion transporting polypeptide 1 B 1 (OATP 1 B 1) alleles *1a, *1b, and *15 on the pharmacokinetics of pitavastatin...
  12. ncbi Influence of the SLCO1B1*1b and *5 haplotypes on pravastatin's cholesterol lowering capabilities and basal sterol serum levels
    Thomas Gerloff
    Institute of Clinical Pharmacology, Charite University Medical Center, Humboldt University of Berlin, Schumannstrasse 20 21, 10098, Berlin, Germany
    Naunyn Schmiedebergs Arch Pharmacol 373:45-50. 2006
    We previously showed that variant SLCO1B1 haplotype *1b (A388G) accelerates and that *5 (T521C) delays hepatocellular uptake of the HMG-CoA reductase inhibitor pravastatin [Mwinyi et al. (2004): Clin Pharmacol Ther 75:415-421]...
  13. ncbi Impact of the SLCO1B1 polymorphism on the pharmacokinetics and lipid-lowering efficacy of multiple-dose pravastatin
    Michael Igel
    Department of Clinical Pharmacology, University of Bonn, Bonn, Germany
    Clin Pharmacol Ther 79:419-26. 2006
    The polymorphism of SLCO1B1 (solute carrier organic anion transporter family, member 1B1), encoding the hepatic uptake transporter organic anion transporting polypeptide 1B1, has been associated with increased pravastatin concentrations ..
  14. ncbi SLCO1B1 polymorphism markedly affects the pharmacokinetics of simvastatin acid
    Marja K Pasanen
    Department of Clinical Pharmacology, University of Helsinki and Helsinki University Central Hospital, Helsinki, Finland
    Pharmacogenet Genomics 16:873-9. 2006
    ..This study aimed to investigate the effects of genetic polymorphism in the SLCO1B1 gene encoding OATP1B1 on the pharmacokinetics of simvastatin.
  15. ncbi Pharmacogenetics of SLCO1B1: haplotypes, htSNPs and hepatic expression in three distinct Asian populations
    Srinivasa Rao Jada
    Laboratory of Clinical Pharmacology, Division of Medical Sciences, National Cancer Centre, 11 Hospital Drive, Singapore, 169610, Singapore
    Eur J Clin Pharmacol 63:555-63. 2007
    The aim of this study was to characterize the population frequency of SLCO1B1 polymorphic variants in three distinct healthy Asian populations, namely Chinese (n = 100), Malay (n = 100) and Indian (n = 100), and to explore the ..
  16. pmc SLCO1B1 521T-->C functional genetic polymorphism and lipid-lowering efficacy of multiple-dose pravastatin in Chinese coronary heart disease patients
    Wei Zhang
    Pharmacogenetics Research Institute, Institute of Clinical Pharmacology, Central South University, Changsha, Hunan, China
    Br J Clin Pharmacol 64:346-52. 2007
    ..g. hepatocytes in the liver) by the organic anion transporting polypeptide 1B1 (OATP1B1), encoded by SLCO1B1...
  17. ncbi SLCO1B1 (OATP1B1, an uptake transporter) and ABCG2 (BCRP, an efflux transporter) variant alleles and pharmacokinetics of pitavastatin in healthy volunteers
    I Ieiri
    Department of Clinical Pharmacokinetics, Graduate School of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan
    Clin Pharmacol Ther 82:541-7. 2007
    To investigate the contribution of genetic polymorphisms of SLCO1B1 and ABCG2 to the pharmacokinetics of a dual substrate, pitavastatin, 2 mg of pitavastatin was administered to 38 healthy volunteers and pharmacokinetic parameters were ..
  18. ncbi Influence of OATP1B1 genotype on the pharmacokinetics of rosuvastatin in Koreans
    J H Choi
    Department of Pharmacology, Yonsei University College of Medicine, Seoul, Korea
    Clin Pharmacol Ther 83:251-7. 2008
    This study was carried out to determine whether polymorphisms of organic anion-transporting polypeptide 1B1 (OATP1B1) have an effect on rosuvastatin pharmacokinetics in Koreans. Among 200 subjects genotyped for OATP1B1 c.388A>G, and c...
  19. pmc Effect of drug transporter genotypes on pravastatin disposition in European- and African-American participants
    Richard H Ho
    Department of Pediatrics and Pharmacology, Vanderbilt University School of Medicine, Nashville, TN, USA
    Pharmacogenet Genomics 17:647-56. 2007
    ..the effects of polymorphisms in the hepatic drug uptake transporter organic anion transporting polypeptide 1B1 (OATP1B1, SLCO1B1) and efflux transporters multidrug resistance-associated protein 2 (MRP2, ABCC2), bile salt export pump (..
  20. ncbi Characterization of novel CYP2C8 haplotypes and their contribution to paclitaxel and repaglinide metabolism
    C Rodriguez-Antona
    Section of Pharmacogenetics, Department of Physiology and Pharmacology, Karolinska Institute, Stockholm, Sweden
    Pharmacogenomics J 8:268-77. 2008
    ..In conclusion, two novel common CYP2C8 haplotypes were identified and significantly associated with altered rate of CYP2C8-dependent drug metabolism in vitro and in vivo...
  21. ncbi Non-synonymous polymorphisms in the human SLCO1B1 gene: an in vitro analysis of SNP c.1929A>C
    Annick Seithel
    Institute of Experimental and Clinical Pharmacology and Toxicology, Friedrich Alexander University Erlangen Nuremberg, Fahrstrasse 17, Erlangen, Germany
    Mol Genet Genomics 279:149-57. 2008
    Polymorphisms in the SLCO1B1 gene encoding the human hepatocellular uptake transporter OATP1B1 can be associated with alterations in transporter properties and may affect the pharmacokinetics of drugs transported by OATP1B1...
  22. ncbi Global analysis of genetic variation in SLCO1B1
    Marja K Pasanen
    University of Helsinki, Department of Clinical Pharmacology, Helsinki University Central Hospital, PO Box 340, FIN 00029 HUS, Helsinki, Finland
    Pharmacogenomics 9:19-33. 2008
    Organic anion transporting polypeptide 1B1 (OATP1B1), encoded by the SLCO1B1 gene, mediates the hepatic uptake of endogenous compounds and xenobiotics, including drugs...
  23. doi Comparison of SLCO1B1 sequence variability among German, Turkish, and African populations
    Jessica Mwinyi
    Institute of Clinical Pharmacology, Charite Universitatsmedizin Berlin, Humboldt University of Berlin, Schumannstrasse 20 21, 10098 Berlin, Germany
    Eur J Clin Pharmacol 64:257-66. 2008
    ..Polymorphisms of the SLCO1B1 gene have been demonstrated to influence in vitro transport function and the pharmacokinetic profile of compounds.
  24. doi Different effects of SLCO1B1 polymorphism on the pharmacokinetics and pharmacodynamics of repaglinide and nateglinide
    Annikka Kalliokoski
    Department of Clinical Pharmacology, Helsinki University Central Hospital, FIN 00029 HUS, Finland
    J Clin Pharmacol 48:311-21. 2008
    Thirty-two healthy volunteers with different SLCO1B1 genotypes ingested a 0.5-mg dose of repaglinide and 60-mg dose of nateglinide with a washout period of 1 week. Participants with SLCO1B1 c.521CC genotype (n = 4) had a 59% (P = 0...
  25. pmc Effect of pregnane X receptor ligands on transport mediated by human OATP1B1 and OATP1B3
    Chunshan Gui
    Department of Pharmacology, Toxicology and Therapeutics, The University of Kansas Medical Center, Kansas City, Kansas, USA
    Eur J Pharmacol 584:57-65. 2008
    ..Organic anion transporting polypeptides 1B1 and 1B3 (OATP1B1 and OATP1B3) are polyspecific transporters expressed at the sinusoidal membrane of human hepatocytes...
  26. doi SLCO1B1 variants and statin-induced myopathy--a genomewide study
    E Link
    N Engl J Med 359:789-99. 2008
    ..In rare cases, myopathy occurs in association with statin therapy, especially when the statins are administered at higher doses and with certain other medications...
  27. doi Association between a frequent allele of the gene encoding OATP1B1 and enhanced LDL-lowering response to fluvastatin therapy
    Philippe Couvert
    INSERM, UMR S551, Dyslipoproteinemia and Atherosclerosis Research Unit, Hopital de la Pitie, F 75013, Paris, France
    Pharmacogenomics 9:1217-27. 2008
    ..The organic anion transporting polypeptide-1B1 encoded by the SLCO1B1 gene is implicated as a major transporter in cellular uptake of statins, and notably fluvastatin...
  28. pmc Comprehensive pharmacogenetic analysis of irinotecan neutropenia and pharmacokinetics
    Federico Innocenti
    The University of Chicago, Chicago, IL 60637, USA
    J Clin Oncol 27:2604-14. 2009
    ..We aim to identify genetic variation, in addition to the UGT1A1*28 polymorphism, that can explain the variability in irinotecan (CPT-11) pharmacokinetics and neutropenia in cancer patients...
  29. pmc Germline genetic variation in an organic anion transporter polypeptide associated with methotrexate pharmacokinetics and clinical effects
    Lisa R Treviño
    St Jude Children s Research Hospital, Memphis, TN 38105 2794, USA
    J Clin Oncol 27:5972-8. 2009
    ..Our aim was to identify the genetic basis of interindividual variability in methotrexate pharmacokinetics in children with newly diagnosed acute lymphoblastic leukemia (ALL)...
  30. ncbi Effects of SLCO1B1 and ABCB1 genotypes on the pharmacokinetics of atorvastatin and 2-hydroxyatorvastatin in healthy Korean subjects
    Y J Lee
    Department of Pharmacology, College of Medicine, Yonsei University, Seoul, Korea
    Int J Clin Pharmacol Ther 48:36-45. 2010
    This study aimed to evaluate the effect of genetic polymorphisms of SLCO1B1 and ABCB1 on the pharmacokinetics of atorvastatin and its metabolites.
  31. doi SLCO1B1 polymorphism and oral antidiabetic drugs
    Annikka Kalliokoski
    Research Department, Social Insurance Institution, Helsinki, Finland
    Basic Clin Pharmacol Toxicol 107:775-81. 2010
    Organic anion-transporting polypeptide 1B1 (OATP1B1; gene: SLCO1B1) is an influx transporter expressed on the sinusoidal membrane of human hepatocytes, where it mediates the uptake of its substrates from blood into liver...
  32. doi 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
    Christina Justenhoven
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
    Breast Cancer Res Treat 125:563-9. 2011
    ..We investigated 31 variants located in PXR, SLCO1A2, SLCO1B1, SLCO1B3, and SLCO2B1 for an association with breast cancer risk and/or histo-pathological tumor characteristics...
  33. doi Loci from a genome-wide analysis of bilirubin levels are associated with gallstone risk and composition
    Stephan Buch
    Department of Internal Medicine I, University Hospital Schleswig Holstein, Kiel, Germany
    Gastroenterology 139:1942-1951.e2. 2010
    ..Bilirubin is a major component of gallstones so we investigated whether these variants predict gallstone bilirubin content and overall risk for gallstones...
  34. doi Differential effect of the rs4149056 variant in SLCO1B1 on myopathy associated with simvastatin and atorvastatin
    L R Brunham
    Centre for Molecular Medicine and Therapeutics, Child and Family Research Institute, University of British Columbia, Vancouver, British Columbia, Canada
    Pharmacogenomics J 12:233-7. 2012
    ..Recently, variation in the SLCO1B1 gene was reported to predict simvastatin-associated myopathy...
  35. pmc Mayo Genome Consortia: a genotype-phenotype resource for genome-wide association studies with an application to the analysis of circulating bilirubin levels
    Suzette J Bielinski
    Division of Epidemiology, Mayo Clinic, 200 First Street SW, Rochester, MN 55905, USA
    Mayo Clin Proc 86:606-14. 2011
    ....
  36. doi OATP1B1/1B3 activity in plated primary human hepatocytes over time in culture
    Maria Ulvestad
    DMPK Innovative Medicines, AstraZeneca R and D Molndal, Pepparedsleden 1, SE 431 83 Molndal, Sweden
    Biochem Pharmacol 82:1219-26. 2011
    ..The aim of 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...
  37. doi Influence of genomic ancestry on the distribution of SLCO1B1, SLCO1B3 and ABCB1 gene polymorphisms among Brazilians
    Vinicius de A Sortica
    Genetics Department, Federal University of Rio Grande do Sul, Porto Alegre, Brazil
    Basic Clin Pharmacol Toxicol 110:460-8. 2012
    The frequency distribution of SNPs and haplotypes in the ABCB1, SLCO1B1 and SLCO1B3 genes varies largely among continental populations...
  38. doi Conserved tryptophan residues within putative transmembrane domain 6 affect transport function of organic anion transporting polypeptide 1B1
    Jiujiu Huang
    College of Life Science, South China Agricultural University, Guangzhou, China J H, N L, w h, K Z, X Y, M H and School of Information, University of South Florida, Tampa, Florida H H
    Mol Pharmacol 84:521-7. 2013
    ..residues (Trp258 and Trp259) within TM6 were identified as critical amino acids for the transport function of OATP1B1. Kinetic studies showed that substitution of Trp258 with alanine resulted in monophasic kinetics for estrone-3-..
  39. ncbi Genetic factors related to unconjugated hyperbilirubinemia amongst adults
    Ching Shan Huang
    Department of Medical Technology, Fooyin University, Kaohsiung, Taiwan
    Pharmacogenet Genomics 15:43-50. 2005
    ..were analysed for UGT1A1, glucose-6-phosphate dehydrogenase (G6PD) and organic anion transporter polypeptide 2 (OATP2) genotypes using polymerase chain reaction-restriction fragment length polymorphism...
  40. ncbi Acute effects of pravastatin on cholesterol synthesis are associated with SLCO1B1 (encoding OATP1B1) haplotype *17
    Mikko Niemi
    Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
    Pharmacogenet Genomics 15:303-9. 2005
    The aim was to investigate whether polymorphisms in the SLCO1B1 gene, encoding the hepatic uptake transporter OATP1B1, influence the short-term effects of pravastatin on cholesterol synthesis.
  41. pmc Pharmacokinetics and response to pravastatin in paediatric patients with familial hypercholesterolaemia and in paediatric cardiac transplant recipients in relation to polymorphisms of the SLCO1B1 and ABCB1 genes
    Mia Hedman
    Hospital for Children and Adolescents, University of Helsinki, Helsinki, Finland
    Br J Clin Pharmacol 61:706-15. 2006
    Our aim was to investigate associations between the single nucleotide polymorphisms (SNPs) in the SLCO1B1 (encoding OATP1B1) and ABCB1 (encoding P-glycoprotein) genes with the pharmacokinetics and efficacy of pravastatin in children with ..
  42. ncbi Frequencies of single nucleotide polymorphisms and haplotypes of organic anion transporting polypeptide 1B1 SLCO1B1 gene in a Finnish population
    Marja K Pasanen
    Department of Clinical Pharmacology, University of Helsinki and Helsinki University Central Hospital, PO Box 340, Helsinki, 00029 HUS, Finland
    Eur J Clin Pharmacol 62:409-15. 2006
    ..to establish high-throughput genotyping assays for the major known single nucleotide polymorphisms (SNP) in the SLCO1B1 gene encoding OATP1B1 and to investigate the frequencies of SNPs and haplotypes of SLCO1B1 in a large Caucasian ..
  43. pmc No significant effect of SLCO1B1 polymorphism on the pharmacokinetics of rosiglitazone and pioglitazone
    Annikka Kalliokoski
    Department of Clinical Pharmacology, University of Helsinki and Helsinki University Central Hospital, Helsinki, Finland
    Br J Clin Pharmacol 65:78-86. 2008
    To examine possible effects of polymorphism in the SLCO1B1 gene, encoding the hepatic uptake transporter organic anion transporting polypeptide (OATP) 1B1, on the pharmacokinetics of rosiglitazone and pioglitazone in a prospective ..
  44. ncbi Organic anion transporting polypeptide-1B1 haplotypes in Chinese patients
    Lin Yong Xu
    Department of Epidemic and Health Statistics, School of Public Health, Central South University, Changsha 410078, China
    Acta Pharmacol Sin 28:1693-7. 2007
    To detect 388G>A and 521T>C variant alleles in the organic anion transporting polypeptide-1B1 (OATP1B1, encoding gene SLCO1B1) gene.
  45. doi Organic anion transporter 1B1: an important factor in hepatic thyroid hormone and estrogen transport and metabolism
    Wendy M van der Deure
    Department of Internal Medicine, Erasmus University Medical Center, Room Ee 502, Dr Molewaterplein 50, 3015 GE Rotterdam, The Netherlands
    Endocrinology 149:4695-701. 2008
    ..A possible candidate is OATP1B1 because model substrates for this transporter include the bilirubin mimic bromosulfophthalein (BSP) and E1S, and ..
  46. ncbi Genetic variations of the SLCO1B1 gene in the Chinese, Malay and Indian populations of Singapore
    Woon Fei Ho
    Department of Pharmacology, Yong Loo Lin School of Medicine, National University of Singapore
    Drug Metab Pharmacokinet 23:476-82. 2008
    ..This study aims to identify genetic variations of SLCO1B1 gene in three distinct ethnic groups of the Singaporean population (n=288)...
  47. doi Association of polymorphisms in four bilirubin metabolism genes with serum bilirubin in three Asian populations
    Rong Lin
    Ministry of Education Key Laboratory of Contemporary Anthropology, School of Life Sciences and Institutes of Biomedical Sciences, Fudan University, Shanghai, China
    Hum Mutat 30:609-15. 2009
    ..11 genetic polymorphisms in heme oxygenase-1 (HMOX1); biliverdin reductase A (BLVRA); solute carrier organic anion transporter family member 1B1 (SLCO1B1); and UGT1A1...
  48. doi The eighth and ninth transmembrane domains in organic anion transporting polypeptide 1B1 affect the transport kinetics of estrone-3-sulfate and estradiol-17beta-D-glucuronide
    Mayuko Miyagawa
    Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan
    J Pharmacol Exp Ther 329:551-7. 2009
    ..Because the homology of the amino acid sequence in the latter part of OATP1B1 and OATP1B3 is relatively low, to determine which TMs in the latter part of OATP1B1 are important for its ..
  49. pmc Genome-wide association meta-analysis for total serum bilirubin levels
    Andrew D Johnson
    National Heart Lung and Blood Institute s The Framingham Heart Study, 73 Mt Wayte Avenue, Suite 2, Framingham, MA 01702, USA
    Hum Mol Genet 18:2700-10. 2009
    ..2 locus. The peak signal in the 12p12.2 region was a non-synonymous SNP in SLCO1B1 (rs4149056, P = 6...
  50. doi 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
    Ichiro Ieiri
    Kyushu University, Graduate School of Pharmaceutical Sciences, Department of Clinical Pharmacokinetics, Fukuoka, Japan
    Expert Opin Drug Metab Toxicol 5:703-29. 2009
    ..All 3-hydroxyl-3-methylglutaryl-CoA reductase inhibitors (statins) except fluvastatin are substrates for OATP1B1, but hepatobiliary (canalicular) efflux transporters differ among statins...
  51. pmc Role of transmembrane domain 10 for the function of organic anion transporting polypeptide 1B1
    Chunshan Gui
    Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, Kansas City, Kansas 66160, USA
    Protein Sci 18:2298-306. 2009
    The liver-specific organic anion transporting polypeptides OATP1B1 and OATP1B3 are highly homologous and share numerous substrates. However, at low concentrations OATP1B1 shows substrate selectivity for estrone-3-sulfate...
  52. pmc The SLCO1B1*5 genetic variant is associated with statin-induced side effects
    Deepak Voora
    Division of Cardiovascular Medicine, Duke University Medical Center, Durham, North Carolina 27708, USA
    J Am Coll Cardiol 54:1609-16. 2009
    ..We sought to identify single nucleotide polymorphisms associated with mild statin-induced side effects...
  53. doi OATP1B1 388A>G polymorphism and pharmacokinetics of pitavastatin in Chinese healthy volunteers
    J Wen
    Institute of Clinical Pharmacology, College of Medicine, Nanchang University, Nanchang, Jiangxi, China
    J Clin Pharm Ther 35:99-104. 2010
    To investigate the contribution of the most frequent single nucleotide polymorphism (SNPs) of the organic anion transporting polypeptide 1B1 (OATP1B1) 388A>G to the pharmacokinetics of pitavastatin in Chinese healthy volunteers.
  54. pmc Identification of amino acids essential for estrone-3-sulfate transport within transmembrane domain 2 of organic anion transporting polypeptide 1B1
    Nan Li
    College of Life Science, South China Agricultural University, Guangzhou, China
    PLoS ONE 7:e36647. 2012
    ..we identify four amino acids (Asp70, Phe73, Glu74, and Gly76) that are essential for the transport function of OATP1B1, an OATP member that is specifically expressed in the human liver...
  55. doi Influence of human OATP1B1, OATP1B3, and OATP1A2 on the pharmacokinetics of methotrexate and paclitaxel in humanized transgenic mice
    Evita van de Steeg
    Division of Molecular Oncology, The Netherlands Cancer Institute, Amsterdam, The Netherlands
    Clin Cancer Res 19:821-32. 2013
    ..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 ..
  56. ncbi Polymorphic organic anion transporting polypeptide 1B1 is a major determinant of repaglinide pharmacokinetics
    Mikko Niemi
    Department of Clinical Pharmacology, University of Helsinki University Central Hospital, Helsinki
    Clin Pharmacol Ther 77:468-78. 2005
    ..SNPs) in the genes encoding for the drug transporters organic anion transporting polypeptide 1B1 (OATP1B1) (SLCO1B1 ) and P-glycoprotein ( MDR1 , ABCB1 ) and the drug-metabolizing enzymes cytochrome P450 (CYP) 2C8 and CYP3A5.
  57. ncbi Different effects of SLCO1B1 polymorphism on the pharmacokinetics of atorvastatin and rosuvastatin
    M K Pasanen
    Department of Clinical Pharmacology, University of Helsinki and Helsinki University Central Hospital, Helsinki, Finland
    Clin Pharmacol Ther 82:726-33. 2007
    Thirty-two healthy volunteers with different SLCO1B1 genotypes ingested a 20 mg dose of atorvastatin and 10 mg dose of rosuvastatin with a washout period of 1 week. Subjects with the SLCO1B1 c.521CC genotype (n=4) had a 144% (P<0...
  58. doi Association between ABCC2 polymorphism and lopinavir accumulation in peripheral blood mononuclear cells of HIV-infected patients
    Laure Elens
    Louvain Center for Toxicology and Applied Pharmacology LTAP, Universite Catholique de Louvain, 53 02 Avenue E Mounier, 1200 Bruxelles, Belgium
    Pharmacogenomics 10:1589-97. 2009
    ....
  59. ncbi Characterization of the efflux transport of 17beta-estradiol-D-17beta-glucuronide from the brain across the blood-brain barrier
    D Sugiyama
    Department of Biopharmaceutics, Graduate School of Pharmaceutical Sciences, The University of Tokyo, Tokyo, Japan
    J Pharmacol Exp Ther 298:316-22. 2001
    ..by examining their inhibitory effects on the transport via organic anion transporting polypeptide 1 (Oatp1), Oatp2, organic anion transporter 1 (Oat1), and Oat3 transfectants using LLC-PK1 cells as hosts...
  60. ncbi Down-regulation of organic anion transporter expression in human hepatocytes exposed to the proinflammatory cytokine interleukin 1beta
    Marc Le Vee
    Institut National de la Santé et de la Recherche Médicale U620, Faculty of Pharmacy, Rennes, France
    Drug Metab Dispos 36:217-22. 2008
    ..Such IL-1beta effects may likely participate in both cholestasis and alterations of hepatic detoxification pathways caused by inflammation in humans...
  61. ncbi Detection of the human organic anion transporters SLC21A6 (OATP2) and SLC21A8 (OATP8) in liver and hepatocellular carcinoma
    Yunhai Cui
    Deutsches Krebsforschungszentrum, Division of Tumor Biochemistry, Heidelberg, Germany
    Lab Invest 83:527-38. 2003
    ..mediating the selective uptake of organic anions into human hepatocytes include the organic anion transporters SLC21A6 (also termed OATP2, OATP-C, or LST-1) and SLC21A8 (OATP8)...
  62. ncbi Molecular identification of a rat novel organic anion transporter moat1, which transports prostaglandin D(2), leukotriene C(4), and taurocholate
    T Nishio
    Department of Neurophysiology, Tohoku University School of Medicine, Sendai, 980 8575, Japan
    Biochem Biophys Res Commun 275:831-8. 2000
    ....
  63. doi Hepatic uptake of the magnetic resonance imaging contrast agent Gd-EOB-DTPA: role of human organic anion transporters
    Mirko Leonhardt
    Department of Pharmacy, Ernst Moritz Arndt University of Greifswald, Greifswald, Germany
    Drug Metab Dispos 38:1024-8. 2010
    ..Therefore, we evaluated affinity of the contrast agent to human organic anion-transporting polypeptides (OATP1B1, OATP1B3, OATP2B1) and to the Na(+)/taurocholate cotransporting polypeptide (NTCP) using stable transfected human ..
  64. ncbi Regulation of rat organic anion transporters in bile salt-induced cholestatic hepatitis: effect of ursodeoxycholate
    Daniel Rost
    Department of Gastroenterology, University Hospital, Heidelberg, Germany
    Hepatology 38:187-95. 2003
    ..In rat liver, Oatp1 (Slc21a1), Oatp2 (Slc21a5), and Oatp4 (Slca10) are expressed at the basolateral membrane of hepatocytes and may be differentially ..
  65. pmc Mechanism of polybrominated diphenyl ether uptake into the liver: PBDE congeners are substrates of human hepatic OATP transporters
    Erik Pacyniak
    Department of Pharmacology, Toxicology and Therapeutics, University of Kansas Medical Center, Kansas City, Kansas 66160, USA
    Toxicol Sci 115:344-53. 2010
    ..Therefore, in the present study, Chinese hamster ovary cell lines expressing OATP1B1, OATP1B3, and OATP2B1 were used to test the hypothesis that OATPs expressed in human hepatocytes would be ..
  66. ncbi Increased hepatic and renal expressions of multidrug resistance-associated protein 3 in Eisai hyperbilirubinuria rats
    Makoto Kuroda
    Third Department of Internal Medicine, Mie University School of Medicine, Tsu, Mie, Japan
    J Gastroenterol Hepatol 19:146-53. 2004
    ..The aim of the present study was to investigate adaptive expressions of mrp1, mrp3, mrp6, organic anion transporting polypeptide 1 (oatp1) and oatp2 in liver and kidney of EHBR.
  67. pmc Targeted disruption of murine organic anion-transporting polypeptide 1b2 (Oatp1b2/Slco1b2) significantly alters disposition of prototypical drug substrates pravastatin and rifampin
    Hani Zaher
    Pfizer Global Research and Development, Ann Arbor, Michigan, USA
    Mol Pharmacol 74:320-9. 2008
    ..Pharmacological characterization was carried out using two prototypical substrates of human OATP1B1 and -1B3, rifampin and pravastatin. After a single intravenous dose of rifampin (1 mg/kg), a 1...
  68. ncbi Identification and species similarity of OATP transporters responsible for hepatic uptake of beta-lactam antibiotics
    Masanori Nakakariya
    Faculty of Pharmaceutical Sciences, Tokyo University of Science RIKADAI, Chiba, Japan
    Drug Metab Pharmacokinet 23:347-55. 2008
    ..In vitro uptake studies revealed that OATP1B3 and OATP1B1 transported nafcillin with Km values of 74 microM and 11 mM, respectively...
  69. pmc Impact of OATP transporters on pharmacokinetics
    A Kalliokoski
    Department of Clinical Pharmacology, University of Helsinki, Helsinki, Finland
    Br J Pharmacol 158:693-705. 2009
    ..For example, a single nucleotide polymorphism (c.521T > C, p.Val174Ala) in the SLCO1B1 gene encoding OATP1B1 decreases the ability of OATP1B1 to transport active simvastatin acid from portal ..
  70. ncbi Effect of phenobarbital on the expression of bile salt and organic anion transporters of rat liver
    N Hagenbuch
    Department of Medicine, University Hospital, Zurich, Switzerland
    J Hepatol 34:881-7. 2001
    ..The hepatic clearance of drugs and cholephilic organic anions is stimulated by phenobarbital (PB). Our aim was to analyze the effects of PB on the expression of hepatocellular bile salt and organic anion transporters...
  71. ncbi Effects of proinflammatory cytokines on rat organic anion transporters during toxic liver injury and cholestasis
    Andreas Geier
    Department of Internal Medicine III, University of Technology Aachen, Aachen, Germany
    Hepatology 38:345-54. 2003
    ..Thus, we studied the molecular mechanisms by which Ntcp, Oatp1, Oatp2, and Mrp2 are regulated by proinflammatory cytokines during liver injury...
  72. ncbi Differential expression of organic anion transporters in rats subjected to 70% or 90% hepatectomy
    Koichiro Sano
    Department of Surgical Oncology and Regulation of Organ Function, Miyazaki University School of Medicine, Miyazaki, Japan
    Hepatogastroenterology 56:176-80. 2009
    ..Differences in hepatic organic anion transporters were compared in rats to identify a causative factor for early stage acute hepatic failure after 70% or 90% hepatectomy (Hx)...
  73. ncbi Molecular characterization and functional regulation of a novel rat liver-specific organic anion transporter rlst-1
    M Kakyo
    Department of Neurophysiology, Tohoku University School of Medicine, Sendai, Ltd, Tokyo, Japan
    Gastroenterology 117:770-5. 1999
    ..The aim of this study was to isolate a rat counterpart of human LST-1 and examine the expression regulation of its messenger RNA (mRNA) to clarify the molecular basis of cholestasis...
  74. ncbi Characterization of organic anion transporter regulation, glutathione metabolism and bile formation in the obese Zucker rat
    Andreas Geier
    Department of Gastroenterology, Aachen University RWTH, Aachen, Germany
    J Hepatol 43:1021-30. 2005
    ..Alterations in hepatobiliary transporters may render fatty livers more vulnerable against various toxic insults...
  75. ncbi Effects of fibrates on human organic anion-transporting polypeptide 1B1-, multidrug resistance protein 2- and P-glycoprotein-mediated transport
    M Yamazaki
    Department of Drug Metabolism, Merck Research Laboratories, West Point, PA 19846, USA
    Xenobiotica 35:737-53. 2005
    ..fenofibrate, fenofibric acid and gemfibrozil) on human organic anion transporting-polypeptide 1B1 (OATP2, OATP-C, SLC21A6), multidrug resistance protein 2 (MRP2/ABCC2) and MDR1-type P-glycoprotein (P-gp/ABCB1) were examined in vitro...
  76. ncbi Bile salt transporters
    Peter J Meier
    Division of Clinical Pharmacology and Toxicology, Department of Medicine, University Hospital, Zurich, 8091 Switzerland
    Annu Rev Physiol 64:635-61. 2002
    ..Ntcp (rodents) and NTCP (humans) and by the Na(+)-independent organic anion-transporting polypeptides Oatp1, Oatp2, and Oatp4 (rodents) and OATP-C (humans)...
  77. ncbi Gemfibrozil and its glucuronide inhibit the hepatic uptake of pravastatin mediated by OATP1B1
    R Nakagomi-Hagihara
    Drug Metabolism and Pharmacokinetics Research Laboratories, Sankyo Co, Ltd, Tokyo, Japan
    Xenobiotica 37:474-86. 2007
    ..i.d., 3 days) to man, the AUC of pravastatin increased approximately 2-fold. We have clarified that OATP1B1 is a key determinant of the hepatic uptake of pravastatin in humans...
  78. ncbi Coordinate regulation of xenobiotic and bile acid homeostasis by pregnane X receptor
    J Staudinger
    Department of Pharmacology and Toxicology, University of Kansas Medical Center, Breidenthal Building, Kansas City, KS 66160 7417, USA
    Drug Metab Dispos 29:1467-72. 2001
    ..of PXR in regulating hepatomegaly and regulating the activity of CYP3A, organic anion transporting polypeptide-2 (Oatp2), and Cyp7a1 (cholesterol 7alpha-hydroxylase) gene products in vivo...
  79. ncbi Influence of drug transporter polymorphisms on pravastatin pharmacokinetics in humans
    Kari T Kivistö
    Department of Pharmacological Sciences, Medical School, University of Tampere, Tampere 33014, Finland
    Pharm Res 24:239-47. 2007
    ..The organic anion transporting polypeptide 1B1 (OATP1B1), encoded by SLCO1B1, and multidrug resistance-associated protein 2 [MRP2 (ABCC2)], are thought to be the major transporters involved ..
  80. ncbi Predominant contribution of rat organic anion transporting polypeptide-2 (Oatp2) to hepatic uptake of beta-lactam antibiotics
    Masanori Nakakariya
    Department of Membrane Transport and Pharmacokinetics, Faculty of Pharmaceutical Sciences, Tokyo University of Science, 2641 Yamasaki, Noda, Chiba 278 8510, Japan
    Pharm Res 25:578-85. 2008
    ..To identify the rat hepatic basolateral transporters involved in the hepatic uptake of beta-lactam antibiotics using nafcillin as a model beta-lactam antibiotic that undergoes extensive biliary excretion...
  81. doi Interaction of porphyrins with human organic anion transporting polypeptide 1B1
    Scott D Campbell
    Division of Clinical and Translational Research, Department of Anesthesiology, Washington University School of Medicine, St Louis, MO 63110, USA
    Chem Biol Interact 182:45-51. 2009
    ..tetrapyrrole bilirubin has been shown to be a substrate for the organic anion transporting polypeptide 1B1 (OATP1B1), similar studies have not been conducted for the cyclic tetrapyrroles (porphyrins)...
  82. ncbi The disposition of pravastatin in a rat model of streptozotocin-induced diabetes and organic anion transporting polypeptide 2 and multidrug resistance-associated protein 2 expression in the liver
    Yoshitaka Hasegawa
    Laboratory of Clinical Pharmaceutics, Faculty of Pharmaceutical Sciences, Kobe Gakuin University, Kobe, Japan
    Biol Pharm Bull 33:153-6. 2010
    ..mRNA expressions of multidrug resistance-associated protein 2 (MRP2) and organic anion transporting polypeptide 2 (OATP2) in the liver were also estimated using reverse transcriptase-polymerase chain reaction (RT-PCR)...
  83. ncbi Molecular evidence of organic ion transporters in the rat adrenal cortex with adrenocorticotropin-regulated zonal expression
    E Beery
    Abteilung Nephrologie und Rheumatologie, Universitat Gottingen, 37073 Gottingen, Germany
    Endocrinology 144:4519-26. 2003
    ..PCR revealed the presence of OAT1, oatp1, oatp2, and oatp3...
  84. doi Organic anion transporting polypeptide 2-mediated uptake of paclitaxel and 2'-ethylcarbonate-linked paclitaxel in freshly isolated rat hepatocytes
    Tadatoshi Tanino
    School of Pharmacy, Kinki University, Higashi Osaka, Osaka, Japan
    J Pharm Pharmacol 61:1029-35. 2009
    ....
  85. ncbi OATP8/1B3-mediated cotransport of bile acids and glutathione: an export pathway for organic anions from hepatocytes?
    Oscar Briz
    Research Unit, University Hospital, Salamanca, Spain
    J Biol Chem 281:30326-35. 2006
    ....
  86. ncbi Endogenous drug transporters in in vitro and in vivo models for the prediction of drug disposition in man
    Lay Beng Goh
    Biomedical Research Centre, University of Dundee, Ninewells Hospital and Medical School, DD1 9SY, Dundee, UK
    Biochem Pharmacol 64:1569-78. 2002
    ..The findings presented are relevant to the use of porcine and canine models for drug disposition...
  87. ncbi Substrate-dependent drug-drug interactions between gemfibrozil, fluvastatin and other organic anion-transporting peptide (OATP) substrates on OATP1B1, OATP2B1, and OATP1B3
    Johannes Noe
    F Hoffmann La Roche Ltd, Non Clinical Development Drug Safety, Basel, Switzerland
    Drug Metab Dispos 35:1308-14. 2007
    ..Multiple transporters are involved in this uptake as Chinese hamster ovary or HEK293 cells expressing either OATP1B1 (K(m) = 1.4-3.5 microM), OATP2B1 (K(m) = 0.7-0...
  88. ncbi Active influx transport is mediated by members of the organic anion transporting polypeptide family in human epidermal keratinocytes
    Ruth Schiffer
    Department of Dermatology, University Clinic, RWTH Aachen, Germany
    J Invest Dermatol 120:285-91. 2003
    ....
  89. ncbi Interactions of cationic drugs and cardiac glycosides at the hepatic uptake level: studies in the rat in vivo, isolated perfused rat liver, isolated rat hepatocytes and oocytes expressing oatp2
    Dirk K F Meijer
    Department of Pharmacokinetics and Drug Delivery, Groningen University Institute of Drug Exploration, The Netherlands
    Arch Pharm Res 25:397-415. 2002
    ..It is shown that the so called organic anion transporting peptide 2 (oatp2) is the likely interaction site: differential inhibition patterns as observed in oocytes expressing oatp2, could ..
  90. ncbi Differential interaction of 3-hydroxy-3-methylglutaryl-coa reductase inhibitors with ABCB1, ABCC2, and OATP1B1
    Cuiping Chen
    Pharmacokinetics, Dynamics and Metabolism, Pfizer Global Research and Development, MS4044, Eastern Point Rd, Groton, CT 06340, USA
    Drug Metab Dispos 33:537-46. 2005
    ..multidrug resistance-associated protein 2 (MRP2, ABCC2), and organic anion-transporting polypeptide 1B1 (OATP1B1, SLCO21A6)...
  91. ncbi Extrahepatic cholestasis downregulates Oatp1 by TNF-alpha signalling without affecting Oatp2 and Oatp4 expression and sodium-independent bile salt uptake in rat liver
    Andreas Geier
    Department of Medicine III, University Hospital Aachen UKA, Aachen University RWTH, Aachen, Germany
    Liver Int 27:1056-65. 2007
    ..In contrast, Oatp2/Oatp1a4 and Oatp4/Oatp1b2 protein expression was not affected by CBDL as compared with controls...
  92. doi In vitro inhibition of OATP-mediated uptake of phalloidin using bile acid derivatives
    Elisa Herraez
    CIBERehd, University of Salamanca, Spain
    Toxicol Appl Pharmacol 239:13-20. 2009
    Hepatocyte uptake of phalloidin is carried out mainly by OATP1B1. We have used this compound as a prototypic substrate and assayed the ability to inhibit OATP-mediated phalloidin transport of four bile acid derivatives (BALU-1, BALU-2, ..
  93. ncbi Conditionally immortalized cell lines as a new in vitro model for the study of barrier functions
    T Terasaki
    Department of Molecular Biopharmacy and Genetics, Graduate School of Pharmaceutical Sciences and New Industry Creation Hatchery Center, Sendai, Japan
    Biol Pharm Bull 24:111-8. 2001
    ..They may also express oatp2 and exhibit dehydroepiandrosterone sulfate and digoxin uptake activity...
  94. ncbi Localization of organic anion transporting polypeptide 4 (Oatp4) in rat liver and comparison of its substrate specificity with Oatp1, Oatp2 and Oatp3
    V Cattori
    Division of Clinical Pharmacology and Toxicology, Department of Internal Medicine, University Hospital, 8091 Zurich, Switzerland
    Pflugers Arch 443:188-95. 2001
    ..In contrast to the well-characterized Oatp1 and Oatp2, the localization and substrate specificity of the recently cloned Oatp4 have not been investigated in detail...
  95. ncbi The organic anion transport polypeptide 1d1 (Oatp1d1) mediates hepatocellular uptake of phalloidin and microcystin into skate liver
    F Meier-Abt
    Mount Desert Island Biological Laboratories MDIBL, Salsbury Cove, Maine 04672, USA
    Toxicol Appl Pharmacol 218:274-9. 2007
    ..sOatp) has been identified and suggested to represent an evolutionarily ancient precursor of the mammalian liver OATP1B1 (human), Oatp1b2 (rat), and OATP1B3 (human)...
  96. ncbi Expression of hepatic UDP-glucuronosyltransferase 1A1 and 1A6 correlated with increased expression of the nuclear constitutive androstane receptor and peroxisome proliferator-activated receptor alpha in male rats fed a high-fat and high-sucrose diet
    Makoto Osabe
    Department of Pharmaco Biochemistry, School of Pharmaceutical Sciences, University of Shizuoka, 52 1 Yada, Shizuoka 422 8526, Japan
    Drug Metab Dispos 36:294-302. 2008
    ..No significant difference in the organic anion transporter polypeptide (Oatp) 1, Oatp2, multidrug resistance-associated protein (Mrp) 2, or Mrp3 protein levels was found between the standard and HF1 ..
  97. doi Influence of drug transporters and UGT polymorphisms on pharmacokinetics of phenolic glucuronide metabolite of mycophenolic acid in Japanese renal transplant recipients
    Masatomo Miura
    Department of Pharmacy, Akita University Hospital, 1 1 1 Hondo, Akita, Japan
    Ther Drug Monit 30:559-64. 2008
    ..On the other hand, the median dose-adjusted AUC0-12 of MPAG in SLCO1B1 1a/1a+1a/1b+1b+1b (n = 53) and 1a/*15 + 1b/*15+*15/*15 (n = 27) were 1549 and 1134 mg.h L g, respectively (P = 0...
  98. ncbi Different expression patterns of organic anion transporting polypeptides in osteosarcomas, bone metastases and aneurysmal bone cysts
    Richard Liedauer
    Department of Pathophysiology, Center for Physiology and Pathophysiology, Medical University of Vienna, Vienna, Austria
    Oncol Rep 22:1485-92. 2009
    ..Transcriptional expression of OATP1A2, 1C1, 2A1, 2B1, 3A1, 4A1, 4C1 and 5A1, but not of OATP1B1, 1B3 and 6A1 was observed in malignant and non-malignant tumor specimens at varying level...
  99. doi Clinical implications of pharmacogenetic variation on the effects of statins
    Simran D S Maggo
    Department of Pharmacology and Toxicology, School of Medical Sciences, University of Otago, Dunedin, New Zealand
    Drug Saf 34:1-19. 2011
    ..genes, CYP2D6, CYP3A4 and CYP3A5, and also a hepatic transporter, solute carrier organic anion transporter (SLCO1B1), which is a single nucleotide polymorphism discovered to be associated with statin-induced myopathy through a ..
  100. ncbi Pvu II polymorphism in the primate homologue of the mouse B144 (LST-1). A novel marker gene within the tumor necrosis factor region
    A de Baey
    Department of Anthropology and Human Genetics, University of Munich, Germany
    Hum Immunol 42:9-14. 1995
    ..LST-1 and its polymorphism may be used as an additional marker of the TNF region, where genes responsible for autoimmune diseases are suspected to be localized...
  101. doi Hepatic uptake and excretion of (-)-N-{2-[(R)-3-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline-2-carbonyl)piperidino]ethyl}-4-fluorobenzamide (YM758), a novel if channel inhibitor, in rats and humans
    Ken ichi Umehara
    Drug Metabolism Research Laboratories, Drug Discovery Research, Astellas Pharma Inc, 1 8, Azusawa 1 chome, Itabashi ku, Tokyo 174 8511, Japan
    Drug Metab Dispos 36:1030-8. 2008
    ..In addition, the uptake of 17beta-estradiol-d-17beta-glucuronide via OATP1B1 was inhibited in the presence of YM758, whereas that via OATP1B3 was not...

Research Grants23

  1. Wei Yue; Fiscal Year: 2015
    ..Therefore, OATP proteins have significant relevance to human health. Dysfunction of OATP1B1 and OATP1B3 is closely related with altered drug pharmacokinetics and toxicity...
  2. HEPATIC DRUG TRANSPORTERS IN DRUG DISPOSITION
    Dan Roden; Fiscal Year: 2006
    ..Moreover, variability in the extent of rifampin-mediated induction of the drug metabolizing enzyme, CYP3A, among subjects with variant OATP-C alleles, will also be tested. [unreadable] [unreadable]..
  3. Bruno Hagenbuch; Fiscal Year: 2016
    DESCRIPTION (provided by applicant): The organic anion transporting polypeptides OATP1B1 and OATP1B3 are two major drug transporters expressed in human hepatocytes...
  4. Swati Nagar; Fiscal Year: 2016
    ..These drugs are substrates for P-gp, BCRP, MRP2, and OATP1B1. 2) Characterize the in situ and in vivo disposition properties of a diverse set of 30 drugs...
  5. Ivan Csanaky; Fiscal Year: 2014
    ..The liver-specific transporter Oatp1b2 (in rodents) has hum an orthologs OATP1B1 and OATP1B3, which are responsible for hepatic uptake of a large number of chemicals...
  6. RICHARD HSINSHIN HO; Fiscal Year: 2016
    ..Our preliminary data strongly supports a role for the hepatic OATPs, OATP1B1 and -1B3, to the disposition of the widely used chemotherapeutic agent docetaxel...
  7. Bruce M Psaty; Fiscal Year: 2015
    ..A non-synonymous variant (V174A, SLCO1B1*5 allele) in the hepatic transporter increased the rhabdomyolysis risk, a finding that we validated in functional ..
  8. Genetic Risk Stratification to Identify Individuals for Early Statin Therapy
    Marc S Sabatine; Fiscal Year: 2010
    ..g., SLCO1B1 and myopathy)...
  9. FUNCTIONS OF THE HEPATIC GAMMA-GLUTAMYL CYCLE
    Nazzareno Ballatori; Fiscal Year: 2007
    ....
  10. Genetic and Epigenetic Regulation of Addiction Genes
    Wolfgang Sadee; Fiscal Year: 2010
    ....
  11. Serotonin-related genes in human brain
    Wolfgang Sadee; Fiscal Year: 2008
    ..Identifying genetic variants that regulate key serotonin-related genes will be a significant step toward developing new methods for the diagnosis, treatment and, possibly, prevention of these disorders. [unreadable] [unreadable]..
  12. Beta-adrenoceptor genetic polymorphisms and obesity
    Julie Johnson; Fiscal Year: 2002
    ..Additionally, genotyping individuals early in age may help to identify those at increased risk of obesity prior to them becoming obese so that they may take appropriate preventive measures. ..
  13. NEONATAL BILIRUBIN NEUROTOXICITY AND P-GLYCOPROTEIN
    Jon Watchko; Fiscal Year: 2007
    ..abstract_text> ..
  14. Hypertension Pharmacogenetics
    Julie Johnson; Fiscal Year: 2006
    ..The proposed studies should add substantial new information about antihypertensive pharmacogenetics, and could influence how antihypertensive medications are prescribed in the future. ..
  15. Beta-receptors and cardiovascular pharmacogenomics
    Julie Johnson; Fiscal Year: 2006
    ..abstract_text> ..
  16. Polymorphisms in Regulatory Regions of Addiction Genes
    Wolfgang Sadee; Fiscal Year: 2005
    ..The results will permit us to assign functional significance to cis-regulatory polymorphisms as a guide in clinical association studies of drug addiction. ..
  17. METHYLMERCURY TRANSPORT ACROSS CELL MEMBRANES
    Nazzareno Ballatori; Fiscal Year: 2005
    ..Evaluate the molecular mechanism by which NAC stimulates renal excretion of MeHg. IV. Test the hypothesis that urinary excretion of MeHg following an NAC oral challenge may be used as a new biomarker of MeHg exposure. ..
  18. OPIOID RECEPTOR REGULATION
    Wolfgang Sadee; Fiscal Year: 2003
    ..Considered together, these hypotheses may yield important insights into the mechanisms underlying tolerance and dependence, providing the opportunity to develop effective therapies of narcotic addiction. ..
  19. Identification of Measles Class II-Restricted Peptides
    INNA OVSYANNIKOVA; Fiscal Year: 2003
    ..The basis from which this proposal will build on is outlined in the background, significance, and preliminary data sections below. ..
  20. BETA-ADRENERGIC RECEPTOR POLYMORPHISMS AND HYPERTENSION
    Julie Johnson; Fiscal Year: 2003
    ..the BAR genotype significantly impacts the BP response to B-blockers could lead to improved patient outcomes, as patients could be genotyped prior to institution of B-blocker therapy, thus avoiding this therapy in those likely to respond ..
  21. MUTATIONS OF MUSCARINIC CHOLINERGIC RECEPTOR GENES
    Wolfgang Sadee; Fiscal Year: 2001
    ..The expected insights from the studies outlined in this proposal should assist in the design of cholinergic therapy for cognitive disorders. ..
  22. Genetic Determinants of C-Reactive Protein
    JACQUELINE DANIK; Fiscal Year: 2008
    ..At the end of the proposed research program, Dr. Suk will have attained advanced skills in genetics and epidemiology which can then be applied to independent research in genetic epidemiology and cardiovascular disease. ..
  23. Cell Signaling, PXR Phosphorylation & Drug Disposition
    Jeffrey Staudinger; Fiscal Year: 2009
    ..These studies will provide additional insight into the regulation of drug disposition and drug-drug interaction. ..