Research Topics
Genomes and Genes
Species | Ulrich M ZangerSummaryAffiliation: Dr. Margarete Fischer-Bosch Institute of Clinical Pharmacology Country: Germany Publications
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Detail Information
Publications
Functional pharmacogenetics/genomics of human cytochromes P450 involved in drug biotransformationUlrich M Zanger
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstr 112, 70376, Stuttgart, Germany
Anal Bioanal Chem 392:1093-108. 2008..In this review, we provide an up-to-date summary of the functional polymorphisms and aspects of the functional genomics of the major human drug-metabolizing cytochrome P450s, as well as their clinical significance...- Cytochrome P450 enzymes in drug metabolism: regulation of gene expression, enzyme activities, and impact of genetic variationUlrich M Zanger
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstr 112 D, 70376 Stuttgart, Germany
Pharmacol Ther 138:103-41. 2013..Here we review the recent progress on drug metabolism activity profiles, interindividual variability and regulation of expression, and the functional and clinical impact of genetic variation in drug metabolizing P450s... 
A systems biology approach to dynamic modeling and inter-subject variability of statin pharmacokinetics in human hepatocytesJoachim Bucher
Institute of Biochemical Engineering, Allmandring, and Center Systems Biology, Nobelstraße, University of Stuttgart, Germany
BMC Syst Biol 5:66. 2011..Predicting individual drug biotransformation capacity requires quantitative and detailed models...
Cytochrome P450 2D6: overview and update on pharmacology, genetics, biochemistryUlrich M Zanger
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, 70376, Stuttgart, Germany
Naunyn Schmiedebergs Arch Pharmacol 369:23-37. 2004..Whether and how brain functions may be influenced by polymorphic expression are interesting questions for the future...- Polymorphic CYP2B6: molecular mechanisms and emerging clinical significanceUlrich M Zanger
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D 70376 Stuttgart, Germany
Pharmacogenomics 8:743-59. 2007..In this review, we summarize general biomolecular and pharmacological features and present a detailed up-to-date description of genetic polymorphisms, including a discussion of recent clinical applications of CYP2B6 pharmacogenetics... - Aberrant splicing caused by single nucleotide polymorphism c.516G>T [Q172H], a marker of CYP2B6*6, is responsible for decreased expression and activity of CYP2B6 in liverMarco H Hofmann
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany and University of Tübingen, Auerbachstrasse 112, 70376 Stuttgart, Germany
J Pharmacol Exp Ther 325:284-92. 2008..These results establish the single nucleotide polymorphism 516G>Tasthe causal sequence variation for severely decreased expression and function associated with CYP2B6*6... - A natural variant of the heme-binding signature (R441C) resulting in complete loss of function of CYP2D6Kathrin Klein
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart and University of Tuebingen, Auerbachstr 112, D 70376 Stuttgart, Germany
Drug Metab Dispos 35:1247-50. 2007..e., the invariant cysteine 2). This suggests that heme binding in mammalian P450s depends not only on the integrity of the heme-binding signature but also on other family- and subfamily-specific sequence determinants... - Breast cancer treatment outcome with adjuvant tamoxifen relative to patient CYP2D6 and CYP2C19 genotypesWerner Schroth
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D 70376 Stuttgart, Germany
J Clin Oncol 25:5187-93. 2007..We investigated the predictive value of genetic variants of CYP2D6, CYP2C19, and three other cytochrome P450 enzymes for tamoxifen treatment outcome... - A novel intronic mutation, 2988G>A, with high predictivity for impaired function of cytochrome P450 2D6 in white subjectsSebastian Raimundo
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Clin Pharmacol Ther 76:128-38. 2004..Their identification is clinically relevant but remains unsatisfactory because of incomplete characterization of the major allele involved, termed CYP2D6*41 (-1584C, R296C, S486T)... - The induction of cytochrome P450 3A5 (CYP3A5) in the human liver and intestine is mediated by the xenobiotic sensors pregnane X receptor (PXR) and constitutively activated receptor (CAR)Oliver Burk
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D 70376 Stuttgart, Germany
J Biol Chem 279:38379-85. 2004..In this manner, induction of CYP3A5 may contribute to the overall importance of this P450 in drug metabolism and drug interactions... - Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liverAnne T Nies
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Hepatology 50:1227-40. 2009..This indicates consequences for hepatic elimination of and response to OCT substrates such as metformin... - Association between the C3435T MDR1 gene polymorphism and susceptibility for ulcerative colitisMatthias Schwab
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, 70376 Stuttgart, Germany
Gastroenterology 124:26-33. 2003..Because the MDR1 single nucleotide polymorphism C3435T is associated with lower intestinal P-glycoprotein expression, we tested whether this polymorphism predisposes to development of ulcerative colitis... - The influence of CYP2B6, CYP2C9 and CYP2D6 genotypes on the formation of the potent antioestrogen Z-4-hydroxy-tamoxifen in human liverJanet K Coller
Dr Margarete Fischer Bosch Institut für Klinische Pharmakologie, Auerbachstrasse 112, D 70376 Stuttgart, Germany
Br J Clin Pharmacol 54:157-67. 2002.... - PPARA: a novel genetic determinant of CYP3A4 in vitro and in vivoKathrin Klein
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Clin Pharmacol Ther 91:1044-52. 2012..These findings have implications for variability in response to drug substrates of CYP3A4... - Large interindividual variability in the in vitro formation of tamoxifen metabolites related to the development of genotoxicityJanet K Coller
Dr Margarete Fischer Bosch Institut für Klinische Pharmakologie, Auerbachstr 112, D 70376 Stuttgart, Germany
Br J Clin Pharmacol 57:105-11. 2004..To characterize the interindividual variability and the individual CYP involved in the formation of alpha-hydroxy-, N-desmethyl- and N-didesmethyl-tamoxifen from tamoxifen... - MALDI-TOF mass spectrometry for multiplex genotyping of CYP2B6 single-nucleotide polymorphismsJulia K Blievernicht
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Clin Chem 53:24-33. 2007..Several nonsynonymous and promoter single-nucleotide polymorphisms (SNPs) in the CYP2B6 gene are associated with altered hepatic expression and function, which affect drug plasma concentrations... - Pharmacogenomics of human liver cytochrome P450 oxidoreductase: multifactorial analysis and impact on microsomal drug oxidationAna M Gomes
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Auerbachstrasse 112, 70376 Stuttgart, Germany
Pharmacogenomics 10:579-99. 2009..We investigated genetic and nongenetic POR variability and its impact on drug-oxidation activities in human liver microsomes... - Genetic variability of CYP2B6 in populations of African and Asian origin: allele frequencies, novel functional variants, and possible implications for anti-HIV therapy with efavirenzKathrin Klein
Dr Margarete Fischer-Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Pharmacogenet Genomics 15:861-73. 2005..17 (T26S, D28G, R29T) appeared to be functionally normal. These data extend the CYP2B6 knowledge base and should be particularly relevant for anti-HIV-therapy with efavirenz... - Three novel thiopurine S-methyltransferase allelic variants (TPMT*20, *21, *22) - association with decreased enzyme functionElke Schaeffeler
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Hum Mutat 27:976. 2006..In Caucasians the occurrence of these genetic variants appears to be extremely rare since none of these alleles were identified in a randomly selected control population of 1048 individuals... - Comprehensive analysis of thiopurine S-methyltransferase phenotype-genotype correlation in a large population of German-Caucasians and identification of novel TPMT variantsElke Schaeffeler
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Pharmacogenetics 14:407-17. 2004..Thus, the results of this study provide a solid basis to predict TPMT phenotype in a Northern European Caucasian population by molecular diagnostics... - CYP2D6 genotyping strategy based on gene copy number determination by TaqMan real-time PCRElke Schaeffeler
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Hum Mutat 22:476-85. 2003..The predictability of the new strategy was systematically evaluated. The semiautomatic TaqMan assay allows high sample throughput and will be useful for pharmacogenetic studies and in the clinical setting... - Sex is a major determinant of CYP3A4 expression in human liverRenzo Wolbold
Dr. Margarete Fischer-Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D-70376 Stuttgart, Germany
Hepatology 38:978-88. 2003..John's wort was found. In conclusion, sex, in addition to PXR and drug exposure, is a major factor for CYP3A4 expression in humans, thus explaining many of the previous observations of sex-dependent drug clearance... - Inferring statin-induced gene regulatory relationships in primary human hepatocytesAdrian Schröder
Center for Bioinformatics Tuebingen, University of Tuebingen, Tuebingen, Germany
Bioinformatics 27:2473-7. 2011..However, statins elicit pleitropic responses including beneficial as well as adverse effects in the liver or other organs. Today, the regulatory mechanisms that cause these pleiotropic effects are not sufficiently understood... - A predominate role of CYP1A2 for the metabolism of nabumetone to the active metabolite, 6-methoxy-2-naphthylacetic acid, in human liver microsomesMiia Turpeinen
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D 70376 Stuttgart, Germany
Drug Metab Dispos 37:1017-24. 2009..Taken together, these studies indicate that the formation of the active metabolite of nabumetone, 6-MNA, is predominantly catalyzed by CYP1A2 in HLMs with only minor contribution of other P450s... - Genetic polymorphisms of glutathione S-transferase A1, the major glutathione S-transferase in human liver: consequences for enzyme expression and busulfan conjugationMonika Bredschneider
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Clin Pharmacol Ther 71:479-87. 2002.... - A natural CYP2B6 TATA box polymorphism (-82T--> C) leading to enhanced transcription and relocation of the transcriptional start siteJörg Zukunft
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Mol Pharmacol 67:1772-82. 2005..Furthermore, a detailed interspecies comparison of CYP2B promoters and transcriptional start sites provided novel insights into evolutionary relationships... - Highly multiplexed genotyping of thiopurine s-methyltransferase variants using MALD-TOF mass spectrometry: reliable genotyping in different ethnic groupsElke Schaeffeler
Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany, and University of Tuebingen, Tuebingen, Germany
Clin Chem 54:1637-47. 2008..To avoid severe hematotoxicity in patients, determination of the TPMT (thiopurine S-methyltransferase) genotype before commencing thiopurine therapy has become accepted... - Molecular mechanisms of polymorphic CYP3A7 expression in adult human liver and intestineOliver Burk
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D 70376 Stuttgart, Germany
J Biol Chem 277:24280-8. 2002..We conclude that the presence of the ER6 motif of CYP3A4 mediates the high expression of CYP3A7 in subjects carrying CYP3A7*1C... - Inhibition of human CYP2B6 by N,N',N''-triethylenethiophosphoramide is irreversible and mechanism-basedTanja Richter
Dr. Margarete Fischer-Bosch Institute of Clinical Pharmacology, Auerbachstr. 112, 70376 Stuttgart, Germany
Biochem Pharmacol 69:517-24. 2005..These findings contribute to better understanding of drug interactions with thioTEPA... - Molecular mechanism of basal CYP3A4 regulation by hepatocyte nuclear factor 4alpha: evidence for direct regulation in the intestineHeike Tegude
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D 70376 Stuttgart, Germany
Drug Metab Dispos 35:946-54. 2007..In summary, we here have elucidated a molecular mechanism of direct regulation of CYP3A4 by HNF4alpha, which is probably specific for the intestine... - Role of genetic and nongenetic factors for fluorouracil treatment-related severe toxicity: a prospective clinical trial by the German 5-FU Toxicity Study GroupMatthias Schwab
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, University of Stuttgart, Stuttgart, Germany
J Clin Oncol 26:2131-8. 2008.... - Azathioprine therapy and adverse drug reactions in patients with inflammatory bowel disease: impact of thiopurine S-methyltransferase polymorphismMatthias Schwab
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
Pharmacogenetics 12:429-36. 2002.... - DNA methylation is associated with downregulation of the organic cation transporter OCT1 (SLC22A1) in human hepatocellular carcinomaElke Schaeffeler
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, 70376 Stuttgart, Germany
Genome Med 3:82. 2011..Therefore, we investigated the role of DNA methylation in the transcriptional regulation of the family members SLC22A1/OCT1, SLC22A2/OCT2 and SLC22A3/OCT3 in HCC... - Discriminative quantification of cytochrome P4502D6 and 2D7/8 pseudogene expression by TaqMan real-time reverse transcriptase polymerase chain reactionKarin Endrizzi
Dr. Margarete Fischer-Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, 70376 Stuttgart, Germany
Anal Biochem 300:121-31. 2002..46, P < 0.0001) but did not depend on CYP2D6 genotype. These data demonstrate genotype-dependent mRNA expression for CYP2D6 and they emphasize the necessity of differentiating between the functional CYP2D6 and the CYP2D pseudogenes... - Potent mechanism-based inhibition of human CYP2B6 by clopidogrel and ticlopidineTanja Richter
Dr. Margarete Fischer-Bosch Institute of Clinical Pharmacology, Stuttgart, Germany
J Pharmacol Exp Ther 308:189-97. 2004..These results suggest the possibility of drug interactions between thienopyridine derivates and drug substrates of CYP2B6 and CYP2C19... - Direct transcriptional regulation of human hepatic cytochrome P450 3A4 (CYP3A4) by peroxisome proliferator-activated receptor alpha (PPARα)Maria Thomas
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstr 112, 70376 Stuttgart, Germany
Mol Pharmacol 83:709-18. 2013..Furthermore, our data suggest that nutritional status can influence drug biotransformation capacity via endogenous phospholipid signaling... - Influence of omeprazole on multidrug resistance protein 3 expression in human liverMonika Hitzl
Dr. Margarete Fischer-Bosch-Institute of Clinical Pharmacology, Stuttgart, Germany
J Pharmacol Exp Ther 304:524-30. 2003..05), in HepG2 cells treated with omeprazole. Finally, MRP3 was induced in HepG2 cells by beta-naphthoflavone. In summary, treatment with omeprazole and beta-naphthoflavone is a determinant of variable human hepatic MRP3 expression... - Paraoxonase (PON1 and PON3) Polymorphisms: Impact on Liver Expression and Atorvastatin-Lactone HydrolysisStephan Riedmaier
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, University of Tuebingen Stuttgart, Germany
Front Pharmacol 2:41. 2011..In conclusion, PON-locus polymorphisms affect PON1 expression whereas non-genetic factors have an effect on PON1 and PON3 expression. This may influence response to therapy or adverse events in statin treatment... - RNA-interference approach to study functions of NADPH : cytochrome P450 oxidoreductase in human hepatocytesDiana M Feidt
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, Auerbachstrasse 112, DE 70376 Stuttgart
Chem Biodivers 6:2084-91. 2009..This will allow systematic studies of various consequences of POR variability in human cells... - Profiling induction of cytochrome p450 enzyme activity by statins using a new liquid chromatography-tandem mass spectrometry cocktail assay in human hepatocytesDiana M Feidt
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, Stuttgart, Germany
Drug Metab Dispos 38:1589-97. 2010..Our cocktail assay should be helpful for economical use of human hepatocytes in the assessment of P450 induction by drugs and drug candidates... - Pathway-Targeted Pharmacogenomics of CYP1A2 in Human LiverKathrin Klein
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, University of Tuebingen Stuttgart, Germany
Front Pharmacol 1:129. 2010..In conclusion, we identified novel trans-associations between regulatory genes and hepatic CYP1A2 function and expression, but additional genetic factors must be assumed to explain the full extent of CYP1A2 heritability... - Sensitive method for the quantification of urinary pyrimidine metabolites in healthy adults by gas chromatography-tandem mass spectrometryUte Hofmann
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstrasse 112, D 70376 Stuttgart, Germany
J Chromatogr B Analyt Technol Biomed Life Sci 791:371-80. 2003..The method was used for investigating the stability of urine samples and the influence of urine collection at different times... - Expression polymorphism of the blood-brain barrier component P-glycoprotein (MDR1) in relation to Parkinson's diseaseTaku Furuno
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Auerbachstr 112, 70376 Stuttgart, Germany
Pharmacogenetics 12:529-34. 2002..In conclusion, MDR1 and other drug transporters represent plausible candidates as Parkinson's disease risk genes. Larger studies are required to confirm this role in the etiology of Parkinson's disease... - Novel CYP2B6 Enzyme Variants in a Rwandese Population: Functional Characterization and Assessment of In Silico Prediction ToolsRobert Radloff
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart, and University of Tuebingen, Tuebingen, Germany
Hum Mutat 34:725-34. 2013..Because low-activity alleles of CYP2B6 are associated with impaired EFV metabolism and adverse drug response, these results are of potential utility for personalized treatment strategies in HIV/AIDS therapy... - Pharmacogenomics of Cytochrome P450 3A4: Recent Progress Toward the "Missing Heritability" ProblemKathrin Klein
Dr Margarete Fischer Bosch Institute of Clinical Pharmacology, Stuttgart Stuttgart, Germany University of Tübingen Tübingen, Germany
Front Genet 4:12. 2013.... - Interindividual variability of canalicular ATP-binding-cassette (ABC)-transporter expression in human liverYvonne Meier
Division of Clinical Pharmacology and Toxicology, Department of Medicine, University Hospital, Zurich, Switzerland
Hepatology 44:62-74. 2006..Furthermore, data suggest a polymorphic transporter expression pattern, which might constitute a risk factor for the development of acquired forms of cholestatic liver diseases... - Detection of single nucleotide polymorphisms in CYP2B6 geneUlrich M Zanger
Dr. Margarete Fischer-Bosch Institute of Clinical Pharmacology, D-70 376 Stuttgart, Germany
Methods Enzymol 357:45-53. 2002 - Sex-dependent genetic markers of CYP3A4 expression and activity in human liver microsomesMarkus Schirmer
Georg August University, Department of Clinical Pharmacology, Gottingen, Germany
Pharmacogenomics 8:443-53. 2007..To find genetic markers of the individual cytochrome P450 (CYP)3A expression... - Mutational analysis of the human dihydropyrimidine dehydrogenase gene by denaturing high-performance liquid chromatographyJoachim Fischer
Margarete Fischer-Bosch Institute of Clinical Pharmacology, D-70376 Stuttgart, Germany
Genet Test 7:97-105. 2003..Sequence analysis confirmed all base changes detected. This method will be useful in identifying patients at risk for toxicity prior to 5-FU treatment, as well as in the analysis of individual patients with thymine-uraciluria... - A naturally occurring mutation in the SLC21A6 gene causing impaired membrane localization of the hepatocyte uptake transporterChristoph Michalski
Division of Tumor Biochemistry, Deutsches Krebsforschungszentrum, D 69120 Heidelberg, Germany
J Biol Chem 277:43058-63. 2002..Importantly, most of the mutant protein SLC21A6-L193R was retained intracellularly, and this single amino acid exchange abolished transport function... - ABCB1 genotype of the donor but not of the recipient is a major risk factor for cyclosporine-related nephrotoxicity after renal transplantationIngeborg A Hauser
Department of Nephrology, Medical Clinic IV, University Hospital Johann Wolfgang Goethe University, Theodor Stern Kai 7, D 60596 Frankfurt am Main, Germany
J Am Soc Nephrol 16:1501-11. 2005..4; 95% confidence interval, 1.2 to 148; P = 0.034). A dominant role of the donor's ABCB1 genotype was identified for development of CsA nephrotoxicity. This suggests that P-glycoprotein is an important factor in CsA nephrotoxicity... - Thiopurine methyltransferase (TPMT) genotype and early treatment response to mercaptopurine in childhood acute lymphoblastic leukemiaMartin Stanulla
Department of Pediatric Hematology and Oncology, Hannover Medical School, Hannover, Germany
JAMA 293:1485-9. 2005..Thiopurine methyltransferase (TPMT) is involved in the metabolism of mercaptopurine and subject to genetic polymorphism, with heterozygous individuals having intermediate and homozygous mutant individuals having very low TPMT activity... - Contribution of CYP3A5 to the in vitro hepatic clearance of tacrolimusLandry K Kamdem
Department of Clinical Pharmacology and Clinical Chemistry, Georg-August University, Goettingen, Germany
Clin Chem 51:1374-81. 2005..The importance of CYP3A5 status for tacrolimus clearance is also dependent on the concomitant CYP3A4 activity... - Three haplotypes associated with CYP2A6 phenotypes in CaucasiansMichael Haberl
EPIDAUROS Biotechnologie AG, Bernried, Germany
Pharmacogenet Genomics 15:609-24. 2005..In summary A CYP2A6*1A-like allele, *9B and *12B are major genetic determinants of CYP2A6 phenotype variation in Caucasians... - Genetic signature consistent with selection against the CYP3A4*1B allele in non-African populationsMarkus Schirmer
Department of Pharmacology, Johannes Gutenberg University, Mainz, Germany
Pharmacogenet Genomics 16:59-71. 2006..The elimination of CYP3A4*1B involved different parts of the CYP3A locus in European Caucasians and Asians. Because CYP3A4 is involved in the vitamin D metabolism, rickets may have been the underlying selecting factor... - Limited contribution of CYP3A5 to the hepatic 6beta-hydroxylation of testosteroneLandry K Kamdem
Department of Clinical Pharmacology, , Robert-Koch Strasse 40, 37099, Germany
Naunyn Schmiedebergs Arch Pharmacol 370:71-7. 2004..However, the contribution of CYP3A5 to 6beta-hydroxylation of testosterone in Caucasian livers is limited, due to the much lower expression levels of CYP3A5... - Cytochrome P450 2B6 activity as measured by bupropion hydroxylation: effect of induction by rifampin and ethnicityKatarzyna K Loboz
Faculty of Pharmacy, University of Sydney, Sydney, Australia
Clin Pharmacol Ther 80:75-84. 2006.... - Multiple novel nonsynonymous CYP2B6 gene polymorphisms in Caucasians: demonstration of phenotypic null allelesThomas Lang
EPIDAUROS Biotechnologie AG, AM Neuland, Bernried, Germany
J Pharmacol Exp Ther 311:34-43. 2004..6% in a Caucasian study population. These data provide further insight into the genetic variability of CYP2B6 and demonstrate the existence of phenotypic null alleles in this gene... - Association of genetic polymorphism in ABCC2 with hepatic multidrug resistance-associated protein 2 expression and pravastatin pharmacokineticsMikko Niemi
Department of Clinical Pharmacology, University of Helsinki and Helsinki University Central Hospital, Helsinki, Finland
Pharmacogenet Genomics 16:801-8. 2006..Our aim was to investigate possible effects of sequence variations in ABCC2, encoding the multidrug resistance-associated protein 2 (MRP2), on the pharmacokinetics of the MRP2 substrate pravastatin... - Genetic polymorphisms in the multidrug resistance-associated protein 3 (ABCC3, MRP3) gene and relationship to its mRNA and protein expression in human liverThomas Lang
Epidauros Biotechnology, Pharmacogenetics Laboratory, Am Neuland 1, 82347 Bernried, Germany
Pharmacogenetics 14:155-64. 2004..To determine the genetic variability of multidrug resistance protein 3 (MRP3)... - Transcriptional profiling of genes induced in the livers of patients treated with carbamazepineMikael Oscarson
Division of Pharmacology/Neurobiology, Biozentrum, University of Basel, Basel, Switzerland
Clin Pharmacol Ther 80:440-456. 2006..CONCLUSIONS: CBZ is a potent inducer of a broad spectrum of drug-metabolizing enzymes and drug transporters in the human liver, and these effects are mediated at least in part by activation of PXR... - Functional study of the 830C>G polymorphism of the human carboxylesterase 2 geneRicardo Bellott
Laboratoire de Pharmacologie des Agents Anticancéreux, Institut Bergonie, Universite Victor Segalen Bordeaux 2, France
Cancer Chemother Pharmacol 61:481-8. 2008.... - Impact of CYP2B6 polymorphism on hepatic efavirenz metabolism in vitroZeruesenay Desta
Division of Clinical Pharmacology, Department of Medicine, Indiana University School of Medicine, 1001 West 10th Street, WD Myers Bldg, W7123, Indianapolis, IN 46202, USA
Pharmacogenomics 8:547-58. 2007..To determine the influence of cytochrome P450 2B6 (CYP2B6) genotype on the rate of oxidative efavirenz metabolism in human liver microsomes... - Non-synonymous polymorphisms in the human SLCO1B1 gene: an in vitro analysis of SNP c.1929A>CAnnick 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..1929A>C had no effect on the hepatic OATP1B1 protein expression and on the transport properties. Therefore, it is unlikely that c.1929A>C contributes to interindividual variability in drug disposition... - Bupropion and 4-OH-bupropion pharmacokinetics in relation to genetic polymorphisms in CYP2B6Julia Kirchheiner
Institute of Clinical Pharmacology, University Medical Center Charite, Humboldt University, Berlin, Germany
Pharmacogenetics 13:619-26. 2003..The role of this allele should also be studied in other CYP2B6 substrates, including cyclophosphamide, halothane, mianserin, promethazine and propofol... - V79 Chinese hamster cells genetically engineered for polymorphic cytochrome P450 2D6 and their predictive value for humansNiels Krebsfaenger
GenPharmTox BioTech AG, D-Planegg/Martinsried
ALTEX 20:143-54. 2003..Based on these results, CYP-mediated metabolism of tamoxifen was investigated... - GSTP1 and MDR1 genotypes and central nervous system relapse in childhood acute lymphoblastic leukemiaMartin Stanulla
Department of Pediatric Hematology and Oncology, Hannover Medical School, Hannover, Germany
Int J Hematol 81:39-44. 2005..These results suggested a modulating role for host genetic variation in the development of CNS relapse in childhood ALL treated according to Berlin-Frankfurt-Münster protocols... - 6-mercaptopurine and 9-(2-phosphonyl-methoxyethyl) adenine (PMEA) transport altered by two missense mutations in the drug transporter gene ABCC4Daniel Janke
Institute of Pharmacology, University of Mainz, Mainz, Germany
Hum Mutat 29:659-69. 2008..Our study shows that Xenopus oocytes are well suited to characterize MRP4 and its protein variants. Carriers of the rare MRP4 variants Y556C and V776I may have altered disposition of MRP4 substrates...