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Phosphorylation and protein–protein interactions in PXR-mediated CYP3A repression

, PhD, , PhD & , PhD
Pages 861-873 | Published online: 08 Jun 2009

Bibliography

  • Nebeker JR, Barach P, Samore MH. Clarifying adverse drug events: a clinician's guide to terminology, documentation, and reporting. Ann Intern Med 2004;140(10):795-801
  • Edwards IR, Aronson JK. Adverse drug reactions: definitions, diagnosis, and management. Lancet 2000;356(9237):1255-9
  • Leape LL, Brennan TA, Laird N, et al. The nature of adverse events in hospitalized patients. Results of the Harvard Medical Practice Study II. N Engl J Med 1991;324(6):377-84
  • Lazarou J, Pomeranz BH, Corey PN. Incidence of adverse drug reactions in hospitalized patients: a meta-analysis of prospective studies. JAMA 1998;279(15):1200-5
  • Johnson JA, Bootman JL. Drug-related morbidity and mortality. A cost-of-illness model. Arch Intern Med 1995;155(18):1949-56
  • Harmsen S, Meijerman I, Beijnen JH, Schellens JH. The role of nuclear receptors in pharmacokinetic drug-drug interactions in oncology. Cancer Treat Rev 2007;33(4):369-80
  • Zhou SF. Drugs behave as substrates, inhibitors and inducers of human cytochrome P450 3A4. Curr Drug Metab 2008;9(4):310-22
  • Guengerich FP. Cytochrome P-450 3A4: regulation and role in drug metabolism. Annu Rev Pharmacol Toxicol 1999;39:1-17
  • Lehmann JM, McKee DD, Watson MA, et al. The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. J Clin Invest 1998;102(5):1016-23
  • Kliewer SA, Moore JT, Wade L, et al. An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway. Cell 1998;92(1):73-82
  • Ding X, Staudinger JL. Induction of drug metabolism by forskolin: the role of the pregnane X receptor and the protein kinase a signal transduction pathway. J Pharmacol Exp Ther 2005;312(2):849-56
  • Ding X, Staudinger JL. Repression of PXR-mediated induction of hepatic CYP3A gene expression by protein kinase C. Biochem Pharmacol 2005;69(5):867-73
  • Johnson DR, Li CW, Chen LY, et al. Regulation and binding of pregnane X receptor by nuclear receptor corepressor silencing mediator of retinoid and thyroid hormone receptors (SMRT). Mol Pharmacol 2006;69(1):99-108
  • Li CW, Dinh GK, Chen JD. Preferential physical and functional interaction of pregnane X receptor with the SMRTalpha isoform. Mol Pharmacol 2009;75(2):363-73
  • Noble SM, Carnahan VE, Moore LB, et al. Human PXR forms a tryptophan zipper-mediated homodimer. Biochemistry 2006;45(28):8579-89
  • Pondugula SR, Brimer-cline C, Wu J, et al. A phosphomimetic mutation at threonine-57 abolishes transactivation activity and alters nuclear localization pattern of human pregnane X receptor. Drug Metab Dispos 2009;37(4):719-30
  • Kawana K, Ikuta T, Kobayashi Y, et al. Molecular mechanism of nuclear translocation of an orphan nuclear receptor, SXR. Mol Pharmacol 2003;63(3):524-31
  • Saradhi M, Krishna B, Mukhopadhyay G, Tyagi RK. Purification of full-length human pregnane and xenobiotic receptor: polyclonal antibody preparation for immunological characterization. Cell Res 2005;15(10):785-95
  • Echchgadda I, Song CS, Oh TS, et al. Gene regulation for the senescence marker protein DHEA-sulfotransferase by the xenobiotic-activated nuclear pregnane X receptor (PXR). Mech Ageing Dev 2004;125(10-11):733-45
  • Chen Y, Tang Y, Wang MT, et al. Human pregnane X receptor and resistance to chemotherapy in prostate cancer. Cancer Res 2007;67(21):10361-7
  • Masuyama H, Hiramatsu Y, Kodama J, Kudo T. Expression and potential roles of pregnane X receptor in endometrial cancer. J Clin Endocrinol Metab 2003;88(9):4446-54
  • Squires EJ, Sueyoshi T, Negishi M. Cytoplasmic localization of pregnane X receptor and ligand-dependent nuclear translocation in mouse liver. J Biol Chem 2004;279(47):49307-14
  • Lichti-Kaiser K, Xu C, Staudinger JL. Cyclic AMP-dependent protein kinase signaling modulates pregnane X receptor activity in a species-specific manner. J Biol Chem 2009;284(11):6639-49
  • Moore LB, Maglich JM, McKee DD, et al. Pregnane X receptor (PXR), constitutive androstane receptor (CAR), and benzoate X receptor (BXR) define three pharmacologically distinct classes of nuclear receptors. Mol Endocrinol 2002;16(5):977-86
  • Kliewer SA, Goodwin B, Willson TM. The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism. Endocr Rev 2002;23(5):687-702
  • Xie W, Barwick JL, Downes M, et al. Humanized xenobiotic response in mice expressing nuclear receptor SXR. Nature 2000;406(6794):435-9
  • Ma X, Shah Y, Cheung C, et al. The PREgnane X receptor gene-humanized mouse: a model for investigating drug-drug interactions mediated by cytochromes P450 3A. Drug Metab Dispos 2007;35(2):194-200
  • Morgan ET. Regulation of cytochrome p450 by inflammatory mediators: why and how? Drug Metab Dispos 2001;29(3):207-12
  • Morgan ET, Goralski KB, Piquette-Miller M, et al. Regulation of drug-metabolizing enzymes and transporters in infection, inflammation, and cancer. Drug Metab Dispos 2008;36(2):205-16
  • Kacevska M, Robertson GR, Clarke SJ, Liddle C. Inflammation and CYP3A4-mediated drug metabolism in advanced cancer: impact and implications for chemotherapeutic drug dosing. Expert Opin Drug Metab Toxicol 2008;4(2):137-49
  • Robertson GR, Liddle C, Clarke SJ. Inflammation and altered drug clearance in cancer: transcriptional repression of a human CYP3A4 transgene in tumor-bearing mice. Clin Pharmacol Ther 2008;83(6):894-7
  • Renton KW. Alteration of drug biotransformation and elimination during infection and inflammation. Pharmacol Ther 2001;92(2-3):147-63
  • Renton KW. Cytochrome P450 regulation and drug biotransformation during inflammation and infection. Curr Drug Metab 2004;5(3):235-43
  • Grant MH, Duthie SJ, Gray AG, Burke MD. Mixed function oxidase and UDP-glucuronyltransferase activities in the human Hep G2 hepatoma cell line. Biochem Pharmacol 1988;37(21):4111-6
  • Donato MT, Bassi AM, Gomez-Lechon MJ, et al. Evaluation of the xenobiotic biotransformation capability of six rodent hepatoma cell lines in comparison with rat hepatocytes. In Vitro Cell Dev Biol Anim 1994;30A(9):574-80
  • Donato MT, Gomez-Lechon MJ, Jover R, et al. Human hepatocyte growth factor down-regulates the expression of cytochrome P450 isozymes in human hepatocytes in primary culture. J Pharmacol Exp Ther 1998;284(2):760-7
  • Thasler WE, Dayoub R, Muhlbauer M, et al. Repression of cytochrome P450 activity in human hepatocytes in vitro by a novel hepatotrophic factor, augmenter of liver regeneration. J Pharmacol Exp Ther 2006;316(2):822-9
  • Papeleu P, Vanhaecke T, Henkens T, et al. Isolation of rat hepatocytes. Methods Mol Biol 2006;320:229-37
  • Giachelli CM, Omiecinski CJ. Developmental regulation of cytochrome P-450 genes in the rat. Mol Pharmacol 1987;31(5):477-84
  • Blake MJ, Gaedigk A, Pearce RE, et al. Ontogeny of dextromethorphan O- and N-demethylation in the first year of life. Clin Pharmacol Ther 2007;81(4):510-6
  • Hakkola J, Pasanen M, Purkunen R, et al. Expression of xenobiotic-metabolizing cytochrome P450 forms in human adult and fetal liver. Biochem Pharmacol 1994;48(1):59-64
  • Hines RN. Ontogeny of human hepatic cytochromes P450. J Biochem Mol Toxicol 2007;21(4):169-75
  • Alcorn J, McNamara PJ. Using ontogeny information to build predictive models for drug elimination. Drug Discov Today 2008;13(11-12):507-12
  • Degawa M, Miura S, Yoshinari K, Hashimoto Y. Altered expression of hepatic CYP1A enzymes in rat hepatocarcinogenesis. Jpn J Cancer Res 1995;86(6):535-9
  • George J, Liddle C, Murray M, et al. Pre-translational regulation of cytochrome P450 genes is responsible for disease-specific changes of individual P450 enzymes among patients with cirrhosis. Biochem Pharmacol 1995;49(7):873-81
  • von der Deck, Hultin T. The enzymatic composition of rat liver microsomes during liver regeneration. Exp Cell Res 1960;19:591-604
  • Marie IJ, Dalet C, Blanchard JM, et al. Inhibition of cytochrome P-450p (P450IIIA1) gene expression during liver regeneration from two-thirds hepatectomy in the rat. Biochem Pharmacol 1988;37(18):3515-21
  • Habib SL, Srikanth NS, Scappaticci FA, et al. Altered expression of cytochrome P450 mRNA during chemical-induced hepatocarcinogenesis and following partial hepatectomy. Toxicol Appl Pharmacol 1994;124(1):139-48
  • Michalopoulos GK. Liver regeneration. J Cell Physiol 2007;213(2):286-300
  • Lin W, Wu J, Dong H, et al. Cyclin-dependent kinase 2 negatively regulates human pregnane X receptor-mediated CYP3A4 gene expression in HepG2 liver carcinoma cells. J Biol Chem 2008;283(45):30650-7
  • Kodama S, Koike C, Negishi M, Yamamoto Y. Nuclear receptors CAR and PXR cross talk with FOXO1 to regulate genes that encode drug-metabolizing and gluconeogenic enzymes. Mol Cell Biol 2004;24(18):7931-40
  • Aitken AE, Richardson TA, Morgan ET. Regulation of drug-metabolizing enzymes and transporters in inflammation. Annu Rev Pharmacol Toxicol 2006;46:123-49
  • Zhou C, Tabb MM, Nelson EL, et al. Mutual repression between steroid and xenobiotic receptor and NF-kappaB signaling pathways links xenobiotic metabolism and inflammation. J Clin Invest 2006;116(8):2280-9
  • Chen JQ, Strom A, Gustafsson JA, Morgan ET. Suppression of the constitutive expression of cytochrome P-450 2C11 by cytokines and interferons in primary cultures of rat hepatocytes: comparison with induction of acute-phase genes and demonstration that CYP2C11 promoter sequences are involved in the suppressive response to interleukins 1 and 6. Mol Pharmacol 1995;47(5):940-7
  • Jover R, Bort R, Gomez-Lechon MJ, Castell JV. Down-regulation of human CYP3A4 by the inflammatory signal interleukin-6: molecular mechanism and transcription factors involved. FASEB J 2002;16(13):1799-801
  • Ferrari L, Peng N, Halpert JR, Morgan ET. Role of nitric oxide in down-regulation of CYP2B1 protein, but not RNA, in primary cultures of rat hepatocytes. Mol Pharmacol 2001;60(1):209-16
  • Charles KA, Rivory LP, Brown SL, et al. Transcriptional repression of hepatic cytochrome P450 3A4 gene in the presence of cancer. Clin Cancer Res 2006;12(24):7492-7
  • Renton KW, Nicholson TE. Hepatic and central nervous system cytochrome P450 are down-regulated during lipopolysaccharide-evoked localized inflammation in brain. J Pharmacol Exp Ther 2000;294(2):524-30
  • Abdulla D, Goralski KB, Renton KW. The regulation of cytochrome P450 2E1 during LPS-induced inflammation in the rat. Toxicol Appl Pharmacol 2006;216(1):1-10
  • Cohen P. The regulation of protein function by multisite phosphorylation–a 25 year update. Trends Biochem Sci 2000;25(12):596-601
  • Cohen P. The role of protein phosphorylation in human health and disease. The sir hans krebs medal lecture. Eur J Biochem 2001;268(19):5001-10
  • Pawson T, Nash P. Protein-protein interactions define specificity in signal transduction. Genes Dev 2000;14(9):1027-47
  • Orti E, Bodwell JE, Munck A. Phosphorylation of steroid hormone receptors. Endocr Rev 1992;13(1):105-28
  • Shao D, Lazar MA. Modulating nuclear receptor function: may the phos be with you. J Clin Invest 1999;103(12):1617-8
  • Ismaili N, Garabedian MJ. Modulation of glucocorticoid receptor function via phosphorylation. Ann NY Acad Sci 2004;1024:86-101
  • Weigel NL, Moore NL. Steroid receptor phosphorylation: a key modulator of multiple receptor functions. Mol Endocrinol 2007;21(10):2311-9
  • Blumberg B, Sabbagh W Jr, Juguilon H, et al. SXR, a novel steroid and xenobiotic-sensing nuclear receptor. Genes Dev 1998;12(20):3195-205
  • Rochette-Egly C. Nuclear receptors: integration of multiple signalling pathways through phosphorylation. Cell Signal 2003;15(4):355-66
  • Sun K, Montana V, Chellappa K, et al. Phosphorylation of a conserved serine in the deoxyribonucleic acid binding domain of nuclear receptors alters intracellular localization. Mol Endocrinol 2007;21(6):1297-311
  • Gu X, Ke S, Liu D, et al. Role of NF-kappaB in regulation of PXR-mediated gene expression: a mechanism for the suppression of cytochrome P-450 3A4 by proinflammatory agents. J Biol Chem 2006;281(26):17882-9
  • Xie W, Tian Y. Xenobiotic receptor meets NF-kappaB, a collision in the small bowel. Cell Metab 2006;4(3):177-8
  • Roth A, Looser R, Kaufmann M, Meyer UA. Sterol regulatory element binding protein 1 interacts with pregnane X receptor and constitutive androstane receptor and represses their target genes. Pharmacogenet Genomics 2008;18(4):325-37
  • Ourlin JC, Lasserre F, Pineau T, et al. The small heterodimer partner interacts with the pregnane X receptor and represses its transcriptional activity. Mol Endocrinol 2003;17(9):1693-703
  • Pascussi JM, Gerbal-Chaloin S, Duret C, et al. The tangle of nuclear receptors that controls xenobiotic metabolism and transport: crosstalk and consequences. Annu Rev Pharmacol Toxicol 2008;48:1-32
  • Lim YP, Huang JD. Interplay of pregnane X receptor with other nuclear receptors on gene regulation. Drug Metab Pharmacokinet 2008;23(1):14-21
  • Handschin C, Podvinec M, Amherd R, et al. Cholesterol and bile acids regulate xenosensor signaling in drug-mediated induction of cytochromes P450. J Biol Chem 2002;277(33):29561-7
  • Xie Y, Ke S, Ouyang N, et al. Epigenetic regulation of transcriptional activity of pregnane X receptor by protein arginine methyltransferase 1. J Biol Chem 2009;284(14):9199-205
  • Greuet J, Pichard L, Ourlin JC, et al. Effect of cell density and epidermal growth factor on the inducible expression of CYP3A and CYP1A genes in human hepatocytes in primary culture. Hepatology 1997;25(5):1166-75
  • Michalopoulos GK, DeFrances MC. Liver regeneration. Science 1997;276(5309):60-6
  • Fausto N, Campbell JS, Riehle KJ. Liver regeneration. Hepatology 2006;43(2 Suppl 1):S45-53
  • Fausto N, Laird AD, Webber EM. Liver regeneration. 2. Role of growth factors and cytokines in hepatic regeneration. FASEB J 1995;9(15):1527-36
  • Galun E, Axelrod JH. The role of cytokines in liver failure and regeneration: potential new molecular therapies. Biochim Biophys Acta 2002;1592(3):345-58
  • Jackson LN, Larson SD, Silva SR, et al. PI3K/Akt activation is critical for early hepatic regeneration after partial hepatectomy. Am J Physiol Gastrointest Liver Physiol 2008;294(6):G1401-10
  • Sahin F, Kannangai R, Adegbola O, et al. mTOR and P70 S6 kinase expression in primary liver neoplasms. Clin Cancer Res 2004;10(24):8421-5
  • Ostrowski J, Woszczynski M, Kowalczyk P, et al. Increased activity of MAP, p70S6 and p90rs kinases is associated with AP-1 activation in spontaneous liver tumours, but not in adjacent tissue in mice. Br J Cancer 2000;82(5):1041-50
  • Dai G, He L, Bu P, Wan YJ. Pregnane X receptor is essential for normal progression of liver regeneration. Hepatology 2008;47(4):1277-87
  • Van Der Heide LP, Hoekman MF, Smidt MP. The ins and outs of FoxO shuttling: mechanisms of FoxO translocation and transcriptional regulation. Biochem J 2004;380(Pt 2):297-309
  • Tang ED, Nunez G, Barr FG, Guan KL. Negative regulation of the forkhead transcription factor FKHR by Akt. J Biol Chem 1999;274(24):16741-6
  • Horton JD, Goldstein JL, Brown MS. SREBPs: activators of the complete program of cholesterol and fatty acid synthesis in the liver. J Clin Invest 2002;109(9):1125-31
  • Muntane-Relat J, Ourlin JC, Domergue J, Maurel P. Differential effects of cytokines on the inducible expression of CYP1A1, CYP1A2, and CYP3A4 in human hepatocytes in primary culture. Hepatology 1995;22(4 Pt 1):1143-53
  • Teng S, Piquette-Miller M. The involvement of the pregnane X receptor in hepatic gene regulation during inflammation in mice. J Pharmacol Exp Ther 2005;312(2):841-8
  • Pascussi JM, Gerbal-Chaloin S, Pichard-Garcia L, et al. Interleukin-6 negatively regulates the expression of pregnane X receptor and constitutively activated receptor in primary human hepatocytes. Biochem Biophys Res Commun 2000;274(3):707-13
  • Beigneux AP, Moser AH, Shigenaga JK, et al. Reduction in cytochrome P-450 enzyme expression is associated with repression of CAR (constitutive androstane receptor) and PXR (pregnane X receptor) in mouse liver during the acute phase response. Biochem Biophys Res Commun 2002;293(1):145-9
  • Xu DX, Wei W, Sun MF, et al. Kupffer cells and reactive oxygen species partially mediate lipopolysaccharide-induced downregulation of nuclear receptor pregnane x receptor and its target gene CYP3a in mouse liver. Free Radic Biol Med 2004;37(1):10-22
  • Fang C, Yoon S, Tindberg N, et al. Hepatic expression of multiple acute phase proteins and down-regulation of nuclear receptors after acute endotoxin exposure. Biochem Pharmacol 2004;67(7):1389-97
  • Kalitsky-Szirtes J, Shayeganpour A, Brocks DR, Piquette-Miller M. Suppression of drug-metabolizing enzymes and efflux transporters in the intestine of endotoxin-treated rats. Drug Metab Dispos 2004;32(1):20-7
  • Langmann T, Moehle C, Mauerer R, et al. Loss of detoxification in inflammatory bowel disease: dysregulation of pregnane X receptor target genes. Gastroenterology 2004;127(1):26-40
  • Iizasa H, Genda N, Kitano T, et al. Altered expression and function of P-glycoprotein in dextran sodium sulfate-induced colitis in mice. J Pharm Sci 2003;92(3):569-76
  • Abate A, Schroder H. Protease inhibitors protect macrophages from lipopolysaccharide-induced cytotoxicity: possible role for NF-kappaB. Life Sci 1998;62(12):1081-8
  • Lotem J, Sachs L. Differential suppression by protease inhibitors and cytokines of apoptosis induced by wild-type p53 and cytotoxic agents. Proc Natl Acad Sci USA 1996;93(22):12507-12
  • Taub R. Liver regeneration: from myth to mechanism. Nat Rev Mol Cell Biol 2004;5(10):836-47
  • Bankey P, Carlson A, Ortiz M, et al. Tumor necrosis factor production by Kupffer cells requires protein kinase C activation. J Surg Res 1990;49(3):256-61
  • Sayeed MM. Alterations in calcium signaling and cellular responses in septic injury. New Horiz 1996;4(1):72-86
  • bdel-Razzak Z, Loyer P, Fautrel A, et al. Cytokines down-regulate expression of major cytochrome P-450 enzymes in adult human hepatocytes in primary culture. Mol Pharmacol 1993;44(4):707-15
  • Thummel KE, Schenkman JB. Effects of testosterone and growth hormone treatment on hepatic microsomal P450 expression in the diabetic rat. Mol Pharmacol 1990;37(1):119-29
  • Yamazoe Y, Murayama N, Shimada M, et al. Cytochrome P450 in livers of diabetic rats: regulation by growth hormone and insulin. Arch Biochem Biophys 1989;268(2):567-75
  • Sotaniemi EA, Pelkonen O, Arranto AJ, et al. Diabetes and elimination of antipyrine in man: an analysis of 298 patients classified by type of diabetes, age, sex, duration of disease and liver involvement. Pharmacol Toxicol 2002;90(3):155-60
  • Sidhu JS, Omiecinski CJ. Insulin-mediated modulation of cytochrome P450 gene induction profiles in primary rat hepatocyte cultures. J Biochem Mol Toxicol 1999;13(1):1-9
  • Yoshida Y, Kimura N, Oda H, Kakinuma A. Insulin suppresses the induction of CYP2B1 and CYP2B2 gene expression by phenobarbital in adult rat cultured hepatocytes. Biochem Biophys Res Commun 1996;229(1):182-8

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