Species-specific activation of nuclear receptors correlates with the response of liver drug metabolizing enzymes to EMD 392949 in vitro

Toxicology Letters

Volumn 193, Issue 1, 2010, Pages 120-123

  Mueller, Stefan O ^a,b   Fery, Yvonne ^c   Tuschl, Gregor ^a   Schrenk, Dieter ^c  

^a Merck Serono GmbH   (Germany)

^b KARLSRUHE INSTITUTE OF TECHNOLOGY   (Germany)

^c University of Koblenz Landau   (Germany)

Author keywords

AhR; Cytochrome P450; Nuclear receptor; PPAR; PXR

Indexed keywords

4 O TOLYLSULFANYL 2 (4 TRIFLUORMETHYL PHENOXY)BUTYRIC ACID; ARYLHYDROCARBON RECEPTOR; CELL NUCLEUS RECEPTOR; CYTOCHROME P450; CYTOCHROME P450 1A; CYTOCHROME P450 3A; DRUG METABOLIZING ENZYME; EMD 392949; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR AGONIST; PREGNANE X RECEPTOR; RIFAMPICIN; TRANSCRIPTION FACTOR; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CELL STRAIN HEPG2; CONTROLLED STUDY; ENZYME ACTIVATION; ENZYME REGULATION; GENE ACTIVATION; HUMAN; HUMAN CELL; HUMAN VERSUS ANIMAL COMPARISON; IN VITRO STUDY; LIVER METABOLISM; NONHUMAN; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; REPORTER GENE; SPECIES DIFFERENCE;

ANIMALS; BUTYRIC ACIDS; CELLS, CULTURED; CYTOCHROME P-450 CYP1A1; DNA PRIMERS; HUMANS; LIVER; LUCIFERASES; MICE; PHARMACEUTICAL PREPARATIONS; RATS; RECEPTORS, ARYL HYDROCARBON; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, STEROID; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; RNA, MESSENGER; SPECIES SPECIFICITY; TRANSFECTION;

RATTUS;

EID: 75749083948     PISSN: 03784274     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.toxlet.2009.12.014     Document Type: Article

References (13)

1. Ammerschlaeger M., Beigel J., Klein K.-U., and Mueller S.O. Characterization of the species-specificity of peroxisome proliferators in rat and human hepatocytes. Toxicol. Sci. 78 (2004) 229-240
2. Baumgart A., Schmidt M., Schmitz H.-J., and Schrenk D. Natural furocoumarins as inducers and inhibitors of cytochrome P450 1A1 in rat hepatocytes. Biochem. Pharmacol. 69 (2005) 657-667
3. Fery Y., et al. Technical pentabromodiphenyl ether and hexabromocyclododecane as activators of the pregnane-X-receptor (PXR). Toxicology 264 1-2 (2009) 45-51
4. Handschin C., and Meyer U.A. Induction of drug metabolism: the role of nuclear receptors. Pharmacol. Rev. 55 (2003) 649-673
5. Honkakoski P., and Negishi M. Regulation of cytochrome P450 (CYP) genes by nuclear receptors. Biochem. J. 347 (2000) 321-337
6. Mukherjee R., Jow L., Noonan D., and McDonnell D.P. Human and rat peroxisome proliferator activated receptors (PPARs) demonstrate similar tissue distribution but different responsiveness to PPAR activators. J. Steroid Biochem. Mol. Biol. 51 (1994) 157-166
7. Richert L., Tuschl G., Abadie C., Blanchard N., Pekthong D., Mantion G., Weber J.C., and Mueller S.O. Use of mRNA expression to detect the induction of drug metabolising enzymes in rat and human hepatocytes. Toxicol. Appl. Pharmacol. 235 (2009) 86-96
8. Richert L., Tuschl G., Viollon-Abadie C., Blanchard N., Bonet A., Heyd B., Halkic N., Wimmer E., Dolgos H., and Mueller S.O. Species differences in the response of liver drug-metabolizing enzymes to (S)-4-O-tolylsulfanyl-2-(4-trifluormethyl-phenoxy)-butyric acid (EMD 392949) in vivo and in vitro. Drug Metab. Dispos. 36 (2008) 702-714
9. Safe S. Molecular biology of the Ah receptor and its role in carcinogenesis. Toxicol. Lett. 120 (2001) 1-7
10. Sueyoshi T., Kawamoto T., Zelko I., Honkakoski P., and Negishi M. The repressed nuclear receptor CAR responds to phenobarbital in activating the human CYP2B6 gene. J. Biol. Chem. 274 (1999) 6043-6046
11. Sueyoshi T., and Negishi M. Phenobarbital response elements of cytochrome P450 genes and nuclear receptors. Annu. Rev. Pharmacol. Toxicol. 41 (2001) 123-143
12. Sugatani J., Nishitani S., Yamakawa K., Yoshinari K., Sueyoshi T., Negishi M., and Miwa M. Transcriptional regulation of human UGT1A1 gene expression: activated glucocorticoid receptor enhances constitutive androstane receptor/pregnane X receptor-mediated UDP-glucuronosyltransferase 1A1 regulation with glucocorticoid receptor-interacting protein 1. Mol. Pharmacol. 67 (2005) 845-855
13. Tuschl G., and Mueller S.O. Effects of cell culture conditions on primary rat hepatocytes-cell morphology and differential gene expression. Toxicology 218 (2006) 205-215