Research Topics
| K W BockSummaryCountry: Germany Publications
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Publications
Human UDP-glucuronosyltransferases: feedback loops between substrates and ligands of their transcription factorsKarl Walter Bock
Department of Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Tubingen, Wilhelmstrasse 56, D 72074 Tubingen, Germany
Biochem Pharmacol 84:1000-6. 2012..Although many newly developed drugs are conjugated by promiscuous UGTs, the discussed regulatory circuits may provide hints to evolutionary important UGT substrates...- Ah receptor- and Nrf2-gene battery members: modulators of quinone-mediated oxidative and endoplasmic reticulum stressKarl Walter Bock
Deparment of Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Tubingen, Wilhelmstrasse 56, D 72074 Tubingen, Germany
Biochem Pharmacol 83:833-8. 2012..In conclusion, tight coupling of Ah receptor- and Nrf2-regulated enzymes may prevent quinone-mediated oxidative and ER stress... 
Ah receptor: dioxin-mediated toxic responses as hints to deregulated physiologic functionsKarl Walter Bock
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Tubingen, Germany
Biochem Pharmacol 72:393-404. 2006..Though important issues remain unresolved, the commentary is intended to stimulate efforts to understand dioxin-mediated toxic responses with emphasis on carcinogenesis in comparison with AhR-mediated physiologic functions...- Vertebrate UDP-glucuronosyltransferases: functional and evolutionary aspectsKarl Walter Bock
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Tubingen, Germany
Biochem Pharmacol 66:691-6. 2003..Related UDP-glucosyltransferases evolved in insects. Even in plants and bacteria UDP-glucosyltransferases have been characterized which may be functionally related... - Topological aspects of oligomeric UDP-glucuronosyltransferases in endoplasmic reticulum membranes: advances and open questionsKarl Walter Bock
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Germany
Biochem Pharmacol 77:1458-65. 2009.... - The mammalian aryl hydrocarbon (Ah) receptor: from mediator of dioxin toxicity toward physiological functions in skin and liverKarl Walter Bock
Department of Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Tubingen, Wilhelmstrasse 56, D 72074 Tubingen, Germany
Biol Chem 390:1225-35. 2009..The AhR is involved in extensive crosstalk with other transcription factors and multiple signaling pathways. Efforts elucidating the pathway toward identification of physiological functions of the AhR remain challenging and promising... - Contributions of the Ah receptor to bilirubin homeostasis and its antioxidative and atheroprotective functionsKarl Walter Bock
Department of Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Tubingen, Wilhelmstrasse 56, D 72074 Tubingen, Germany
Biol Chem 391:645-53. 2010.... - Tissue-specific regulation of canine intestinal and hepatic phenol and morphine UDP-glucuronosyltransferases by beta-naphthoflavone in comparison with humansKarl Walter Bock
Institute of Toxicology, University of Tubingen, Tubingen, Germany
Biochem Pharmacol 63:1683-90. 2002..The results suggest marked differences in tissue-specific regulation of canine vs. human hepatic and intestinal phenol or morphine UGTs... - Influence of t-butylhydroquinone and beta-naphthoflavone on formation and transport of 4-methylumbelliferone glucuronide in Caco-2/TC-7 cell monolayersBarbara S Bock-Hennig
Institute of Toxicology, University of Tubingen, Wilhelmstrasse 56, D 72074, Tubingen, Germany
Biochem Pharmacol 63:123-8. 2002..The results suggest that MUF-GA is mostly secreted basolaterally in Caco-2 cell monolayers. Treatment with TBHQ or BNF significantly enhanced MUF-GA formation in the intact cell... - Density-dependent growth of normal and nodular hepatocytesK W Bock
Institute of Toxicology, University of Tubingen, Wilhelmstrasse 56, D 72074, Tubingen, Germany
Toxicology 144:51-6. 2000..The results suggest marked differences in growth behavior of nodular versus normal hepatocyte cultures probably due to paracrine stimulation by growth factors and altered cell-cell interaction... - Coordinate induction by antioxidants of UDP-glucuronosyltransferase UGT1A6 and the apical conjugate export pump MRP2 (multidrug resistance protein 2) in Caco-2 cellsK W Bock
Institute of Toxicology, University of Tubingen, Germany
Biochem Pharmacol 59:467-70. 2000..The results indicate that UGT1A6 and MRP2 are coordinately induced by antioxidants, facilitating chemoprotection against phenolic toxins and excretion of conjugates into the intestinal lumen... - Mono- and Diglucuronide formation from benzo[a]pyrene and chrysene diphenols by AHH-1 cell-expressed UDP-glucuronosyltransferase UGT1A7K W Bock
Institute of Toxicology, University of Tubingen, Germany
Biochem Pharmacol 57:653-6. 1999..1 microM) than UGT1A6 (10 microM). The results suggest that the two PAH-inducible UGTs may cooperate in conjugating PAH metabolites, but that UGT1A7 is more efficient... - Functions and transcriptional regulation of adult human hepatic UDP-glucuronosyl-transferases (UGTs): mechanisms responsible for interindividual variation of UGT levelsKarl Walter Bock
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Wilhelmstrasse 56, D 72074 Tubingen, Germany
Biochem Pharmacol 80:771-7. 2010..and the Ah receptor are discussed. Unraveling the mechanisms responsible for interindividual variation of UGT expression will be beneficial for drug therapy but still remains a major challenge... - From differential induction of UDP-glucuronosyltransferases in rat liver to characterization of responsible ligand-activated transcription factors, and their multilevel crosstalk in humansKarl Walter Bock
Department of Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, University of Tubingen, Wilhelmstrasse, Germany
Biochem Pharmacol 82:9-16. 2011..Nevertheless, as drug targets ligand-activated transcription factors provide promising therapeutic possibilities... - Ah receptor- and TCDD-mediated liver tumor promotion: clonal selection and expansion of cells evading growth arrest and apoptosisKarl Walter Bock
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Tubingen, Germany
Biochem Pharmacol 69:1403-8. 2005..Models are discussed which may facilitate verification of this hypothesis... - Functions and transcriptional regulation of PAH-inducible human UDP-glucuronosyltransferasesK W Bock
Institute of Toxicology, University of Tubingen, Germany
Drug Metab Rev 31:411-22. 1999..Studies with stably expressed isoforms suggest that UGT1A9 is responsible for the formation of benzo(a)pyrene-3.6-diphenol diglucuronide, the major biliary metabolite of benzo(a)pyrene... - Contribution of the Ah receptor to the phenolic antioxidant-mediated expression of human and rat UDP-glucuronosyltransferase UGT1A6 in Caco-2 and rat hepatoma 5L cellsPeter A Munzel
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Tübingen D 72074, Germany
Biochem Pharmacol 66:841-7. 2003..The results suggest a contribution of the AhR pathway and of proteins binding to the XRE flanking region to the induction of human UGT1A6 by both AhR agonists and phenolic antioxidants... - Radiation inactivation analysis of microsomal UDP-glucuronosyltransferases catalysing mono- and diglucuronide formation of 3,6-dihydroxybenzo(a)pyrene and 3,6-dihydroxychryseneH Gschaidmeier
Institute of Toxicology, University of Tubingen, Germany
Biochem Pharmacol 48:1545-9. 1994..In contrast, UGTs involved in diglucuronide formation of diphenols of polycyclic aromatic hydrocarbons may function as tetramers in microsomes in situ... 
Phase II metabolism of benzeneD Schrenk
Institute of Toxicology, University of Tubingen, Germany
Environ Health Perspect 104:1183-8. 1996..The higher susceptibility of mice toward benzene may be related to the high rate of formation of the myelotoxic metabolite HQ and the semistable phase II metabolites HQ sulfate and THB sulfate...- Aryl hydrocarbon receptor-inducible or constitutive expression of human UDP glucuronosyltransferase UGT1A6P A Münzel
Institute of Toxicology, University of Tubingen, Germany
Arch Biochem Biophys 350:72-8. 1998..Furthermore, primer extension studies suggest cell-specific use of multiple TATA boxes. Hence, regulation of human UGT1A6 appears to be cell-specific including both constitutive and aryl hydrocarbon receptor-controlled expression... - 2,3,7,8-tetrachlorodibenzo-p-dioxin-dependent release from contact inhibition in WB-F344 cells: involvement of cyclin AC Dietrich
Institute of Toxicology, Johannes Gutenberg University, Obere Zahlbacherstrasse 67, 55131 Mainz, Germany
Toxicol Appl Pharmacol 183:117-26. 2002..These data indicate cyclin A-dependent loss of G1 arrest after TCDD treatment mainly downstream of the retinoblastoma protein... - Serotonin glucuronidation by Ah receptor- and oxidative stress-inducible human UDP-glucuronosyltransferase (UGT) 1A6 in Caco-2 cellsChristoph Kohle
Institute of Pharmacology and Toxicology, Department of Toxicology, University of Tubingen, Germany
Biochem Pharmacol 69:1397-402. 2005..The results suggest that--in addition to its detoxification function--intestinal UGT1A6 contributes to intestinal homeostasis of 5-HT from dietary sources and from release by enterochromaffin cells... - Coordinate regulation of human drug-metabolizing enzymes, and conjugate transporters by the Ah receptor, pregnane X receptor and constitutive androstane receptorChristoph Kohle
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Tubingen, Germany
Biochem Pharmacol 77:689-99. 2009..Biotransformation appears to be tightly controlled to achieve efficient homeostasis of endobiotics and detoxification of dietary phytochemicals, but nuclear receptor agonists may also lead to potentially harmful drug interactions... - TCDD-dependent downregulation of gamma-catenin in rat liver epithelial cells (WB-F344)Cornelia Dietrich
Institute of Toxicology, Johannes Gutenberg University, Obere Zahlbacherstrasse 67, 55131 Mainz, Germany
Int J Cancer 103:435-9. 2003..Because gamma-catenin is considered to be a tumor suppressor, our findings might give more insight into the tumor promoting actions of TCDD... - A distribution study of CYP1A2 phenotypes among smokers and non-smokers in a cohort of healthy Caucasian volunteersD Schrenk
Institute of Toxicology, University of Tubingen, Germany
Eur J Clin Pharmacol 53:361-7. 1998.... - Coordinate regulation of drug metabolism by xenobiotic nuclear receptors: UGTs acting together with CYPs and glucuronide transportersKarl Walter Bock
Institute of Pharmacology and Toxicology, , , Germany
Drug Metab Rev 36:595-615. 2004..In addition, regulation by nuclear receptors was probably shaped by the need for homeostatic control of endobiotic signals in the evolution of multicellular organisms... - Frequent co-occurrence of the TATA box mutation associated with Gilbert's syndrome (UGT1A1*28) with other polymorphisms of the UDP-glucuronosyltransferase-1 locus (UGT1A6*2 and UGT1A7*3) in Caucasians and EgyptiansChristoph Kohle
Institute of Pharmacology and Toxicology, University of Tubingen, Tubingen, Germany
Biochem Pharmacol 65:1521-7. 2003..Frequent haplotypes containing several UGT1 allelic variants should be taken into account in studies on the association between diseases, abnormal drug reactions, and UGT1 family polymorphisms... - Activation of coupled Ah receptor and Nrf2 gene batteries by dietary phytochemicals in relation to chemopreventionChristoph Kohle
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Germany
Biochem Pharmacol 72:795-805. 2006.... - Promotion of hepatocarcinogenesis in humans and animal modelsChristoph Kohle
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Tubingen, Germany
Arch Toxicol 82:623-31. 2008..Further studies on the different modes of action may help to avoid overestimation of the risk of liver tumor promotion... - UDP-glucuronosyltransferase 1A6: structural, functional, and regulatory aspectsKarl Walter Bock
Institut of Pharmacology and Toxicology, Department of Toxicology, University of Tubingen, Germany
Methods Enzymol 400:57-75. 2005..However, marked differences have been noted in the expression of rat and human UGT1A6. Regulatory factors have been studied in detail in the human Caco-2 colon adenocarcinoma cell model... - Coordinate regulation of Phase I and II xenobiotic metabolisms by the Ah receptor and Nrf2Christoph Kohle
Department of Toxicology, Institute of Pharmacology and Toxicology, University of Tubingen, Germany
Biochem Pharmacol 73:1853-62. 2007..Better recognition of coordinate Phase I and II metabolisms may improve risk assessment of reactive toxic intermediates in the extrapolation to low level endo- and xenobiotic exposure... - Nomenclature update for the mammalian UDP glycosyltransferase (UGT) gene superfamilyPeter I Mackenzie
Department of Clinical Pharmacology, Flinders University School of Medicine, Flinders Medical Center, Bedford Park, Australia
Pharmacogenet Genomics 15:677-85. 2005..Most UGT1 and UGT8 enzymes have been characterized in detail; however, the catalytic functions of the UGT3A enzymes and several UGT2 enzymes remain to be characterized...