Overcoming drug resistance by regulating nuclear receptors

Advanced Drug Delivery Reviews

Volumn 62, Issue 13, 2010, Pages 1257-1264

  Chen, Taosheng ^a  

^a ST JUDE CHILDREN S RESEARCH HOSPITAL   (United States)

Author keywords

ABC transporters; CYP3A4; Drug resistance; Drug metabolizing enzymes; MDR1; PXR

Indexed keywords

ABC TRANSPORTER; CYP3A4; DRUG RESISTANCE; DRUG-METABOLIZING ENZYMES; MDR1; PXR;

CATALYSTS; ENZYMES; ONCOLOGY; TOXICITY; TRANSCRIPTION FACTORS;

DRUG THERAPY;

ABC TRANSPORTER; ANTIBIOTIC AGENT; ANTINEOPLASTIC AGENT; BIRICODAR; BREAST CANCER RESISTANCE PROTEIN; CALCIUM CHANNEL BLOCKING AGENT; CELL NUCLEUS RECEPTOR; CYCLOSPORIN A; CYTARABINE; CYTOTOXIC AGENT; DAUNORUBICIN; ELACRIDAR; ETOPOSIDE; IMMUNOSUPPRESSIVE AGENT; LANIQUIDAR; LIPOSOME; MULTIDRUG RESISTANCE PROTEIN; MULTIDRUG RESISTANCE PROTEIN 1; MULTIDRUG RESISTANCE PROTEIN 1 INHIBITOR; PACLITAXEL; PREGNANE X RECEPTOR; PROTEIN INHIBITOR; QUININE; SMALL INTERFERING RNA; TARIQUIDAR; UNCLASSIFIED DRUG; UNINDEXED DRUG; VALSPODAR; VERAPAMIL; VINBLASTINE; ZOSUQUIDAR;

ACUTE GRANULOCYTIC LEUKEMIA; BREAST CANCER; CANCER CHEMOTHERAPY; CANCER RESISTANCE; CHEMOSENSITIVITY; CLINICAL TRIAL; DRUG CLEARANCE; DRUG DELIVERY SYSTEM; DRUG EFFECT; DRUG ELIMINATION; DRUG METABOLISM; DRUG POTENTIATION; DRUG SAFETY; DRUG SYNTHESIS; DRUG TREATMENT FAILURE; HUMAN; IMMUNE DEFICIENCY; LUNG NON SMALL CELL CANCER; MALIGNANT NEOPLASTIC DISEASE; METASTASIS; MULTIDRUG RESISTANCE; PHENOTYPE; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN FUNCTION; RECURRENT CANCER; REGULATORY MECHANISM; REVIEW; UNSPECIFIED SIDE EFFECT;

ANTINEOPLASTIC AGENTS; DRUG RESISTANCE, MULTIPLE; DRUG RESISTANCE, NEOPLASM; HUMANS; MOLECULAR TARGETED THERAPY; NEOPLASMS; P-GLYCOPROTEINS; RECEPTORS, CYTOPLASMIC AND NUCLEAR; RECEPTORS, STEROID;

EID: 78649284256     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.addr.2010.07.008     Document Type: Review

References (114)

1. Nguyen M.H., Garcia R.T., Trinh H.N., Nguyen H.A., Nguyen K.K., Nguyen L.H., Levitt B. Prevalence of hepatitis B virus DNA polymerase mutations in treatment-naïve patients with chronic hepatitis B. Aliment. Pharmacol. Ther. 2009, 30:1150-1158.
2. Clarke R., Liu M.C., Bouker K.B., Gu Z., Lee R.Y., Zhu Y., Skaar T.C., Gomez B., O'Brien K., Wang Y., Hilakivi-Clarke L.A. Antiestrogen resistance in breast cancer and the role of estrogen receptor signaling. Oncogene 2003, 22:7316-7339.
3. Mellor H.R., Callaghan R. Resistance to chemotherapy in cancer: a complex and integrated cellular response. Pharmacology 2008, 81:275-300.
4. Szakács G., Paterson J.K., Ludwig J.A., Booth-Genthe C., Gottesman M.M. Targeting multidrug resistance in cancer. Nat. Rev. Drug Discov. 2006, 5:219-234.
5. Harasym T.O., Liboiron B.D., Mayer L.D. Drug ratio-dependent antagonism: a new category of multidrug resistance and strategies for its circumvention. Meth. Mol. Biol. 2010, 596:291-323.
6. Jemal A., Siegel R., Ward E., Hao Y., Xu J., Thun M.J. Cancer statistics, 2009. CA Cancer J. Clin. 2009, 59:225-249.
7. Lee C.H. Reversing agents for ATP-binding cassette drug transporters. Meth. Mol. Biol. 2010, 596:325-340.
8. Zhang B., Xie W., Krasowski M.D. PXR: a xenobiotic receptor of diverse function implicated in pharmacogenetics. Pharmacogenomics 2008, 9:1695-1709.
9. Pondugula S.R., Dong H., Chen T. Phosphorylation and protein-protein interactions in PXR-mediated CYP3A repression. Expert Opin. Drug Metab. Toxicol. 2009, 5:861-873.
10. Robertson G.R., Liddle C., Clarke S.J. Inflammation and altered drug clearance in cancer: transcriptional repression of a human CYP3A4 transgene in tumor-bearing mice. Clin. Pharmacol. Ther. 2008, 83:894-897.
11. Dano K. Active outward transport of daunomycin in resistant Ehrlich ascites tumor cells. Biochem. Biophys. Acta 1973, 323:466-483.
12. Tsuruo T., Iida H., Tsukagoshi S., Sakurai Y. Overcoming of vincrintine resistance in PP388 leukemia in vivo and in vitro through enhanced cytotoxicity of vincristine and vinblastine by verapamil. Cancer Res. 1981, 41:1967-1972.
13. Daenen S., van der Holt B., Verhoef G.E., Löwenberg B., Wijermans P.W., Huijgens P.C., van Marwijk Kooy R., Schouten H.C., Kramer M.H., Ferrant A., van den Berg E., Steijaert M.M., Verdonck L.F., Sonneveld P. Addition of cyclosporin A to the combination of mitoxantrone and etoposide to overcome resistance to chemotherapy in refractory or relapsing acute myeloid leukaemia: a randomised phase II trial from HOVON, the Dutch-Belgian Haemato-Oncology Working Group for adults. Leuk. Res. 2004, 28:1057-1067.
14. Wattel E., Solary E., Hecquet B., Caillot D., Ifrah N., Brion A., Milpied N., Janvier M., Guerci A., Rochant H., Cordonnier C., Dreyfus F., Veil A., Hoang-Ngoc L., Stoppa A.M., Gratecos N., Sadoun A., Tilly H., Brice P., Lioure B., Desablens B., Pignon B., Abgrall J.P., Leporrier M., Fenaux P., et al. Quinine improves results of intensive chemotherapy (IC) in myelodysplastic syndromes (MDS) expressing P-glycoprotein (PGP). Updated results of a randomized study. Groupe Français des Myélodysplasies (GFM) and Groupe GOELAMS. Adv. Exp. Med. Biol. 1999, 457:35-46.
15. Kolitz J.E., George S.L., Dodge R.K., Hurd D.D., Powell B.L., Allen S.L., Velez-Garcia E., Moore J.O., Shea T.C., Hoke E., Caligiuri M.A., Vardiman J.W., Bloomfield C.D., Larson R.A. Dose escalation studies of cytarabine, daunorubicin, and etoposide with and without multidrug resistance modulation with PSC-833 in untreated adults with acute myeloid leukemia younger than 60years: final induction results of Cancer and Leukemia Group B Study 9621. J. Clin. Oncol. 2004, 22:4290-4301.
16. Baer M.R., George S.L., Dodge R.K., O'Loughlin K.L., Minderman H., Caligiuri M.A., Anastasi J., Powell B.L., Kolitz J.E., Schiffer C.A., Bloomfield C.D., Larson R.A. Phase 3 study of the multidrug resistance modulator PSC-833 in previously untreated patients 60years of age and older with acute myeloid leukemia: Cancer and Leukemia Group B Study 9720. Blood 2002, 100:1224-1232.
17. Goldman B. Multidrug resistance: can new drugs help chemotherapy score against cancer?. J. Natl. Cancer Inst. 2003, 95:255-257.
18. Fox E., Bates S.E. Tariquidar (XR9576): a P-glycoprotein drug efflux pump inhibitor. Expert Rev. Anticancer Ther. 2007, 7:447-459.
19. Ruff P., Vorobiof D.A., Jordaan J.P., Demetriou G.S., Moodley S.D., Nosworthy A.L., Werner I.D., Raats J., Burgess L.J. A randomized, placebo-controlled, double-blind phase 2 study of docetaxel compared to docetaxel plus zosuquidar (LY335979) in women with metastatic or locally recurrent breast cancer who have received one prior chemotherapy regimen. Cancer Chemother. Pharmacol. 2009, 64:763-768.
20. Cordon-Cardo C., O'Brien J.P., Boccia J., Casals D., Bertino J.R., Melamed M.R. Expression of the multidrug resistance gene product (P-glycoprotein) in human normal and tumor tissues. J. Histochem. Cytochem. 1990, 38:1277-1287.
21. Comerford K.M., Wallace T.J., Karhausen J., Louis N.A., Montalto M.C., Colgan S.P. Hypoxia-inducible factor-1-dependent regulation of the multidrug resistance (MDR1) gene. Cancer Res. 2002, 62:3387-3394.
22. Sampath J., Sun D., Kidd V.J., Grenet J., Gandhi A., Shapiro L.H., Wang Q., Zambetti G.P., Schuetz J.D. Mutant p53 cooperates with ETS and selectively up-regulates human MDR1 not MRP1. J. Biol. Chem. 2001, 276:39359-39367.
23. Huff L.M., Lee J.S., Robey R.W., Fojo T. Characterization of gene rearrangements leading to activation of MDR-1. J. Biol. Chem. 2006, 281:36501-36509.
24. El-Osta A., Kantharidis P., Zalcberg J.R., Wolffe A.P. Precipitous release of methyl-CpG binding protein 2 and histone deacetylase 1 from the methylated human multidrug resistance gene (MDR1) on activation. Mol. Cell. Biol. 2002, 22:1844-1857.
25. Tada Y., Wada M., Kuroiwa K., Kinugawa N., Harada T., Nagayama J., Nakagawa M., Naito S., Kuwano M. MDR1 gene overexpression and altered degree of methylation at the promoter region in bladder cancer during chemotherapeutic treatment. Clin. Cancer Res. 2000, 6:4618-4627.
26. Baker E.K., Johnstone R.W., Zalcberg J.R., El-Osta A. Epigenetic changes to the MDR1 locus in response to chemotherapeutic drugs. Oncogene 2005, 24:8061-8675.
27. Gómez-Martínez A., García-Morales P., Carrato A., Castro-Galache M.D., Soto J.L., Carrasco-García E., García-Bautista M., Guaraz P., Ferragut J.A., Saceda M. Post-transcriptional regulation of P-glycoprotein expression in cancer cell lines. Mol. Cancer Res. 2007, 5:641-653.
28. Zhu H., Wu H., Liu X., Evans B.R., Medina D.J., Liu C.G., Yang J.M. Role of MicroRNA miR-27a and miR-451 in the regulation of MDR1/P-glycoprotein expression in human cancer cells. Biochem. Pharmacol. 2008, 76:582-588.
29. Cerveny L., Svecova L., Anzenbacherova E., Vrzal R., Staud F., Dvorak Z., Ulrichova J., Anzenbacher P., Pavek P. Valproic acid induces CYP3A4 and MDR1 gene expression by activation of constitutive androstane receptor and pregnane X receptor pathways. Drug Metab. Dispos. 2007, 35:1032-1041.
30. Synold T.W., Dussault I., Forman B.M. The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux. Nat. Med. 2001, 7:584-590.
31. Geick A., Eichelbaum M., Burk O. Nuclear receptor response elements mediate induction of intestinal MDR1 by rifampin. J. Biol. Chem. 2001, 276:14581-14587.
32. Juliano R.L., Ling V. A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants. Biochim. Biophys. Acta 1976, 455:152-162.
33. Duncan A.M., Deeley R.G., Cole S.P., Bhardwaj G., Gerlach J.H., Mackie J.E., Grant C.E., Almquist K.C., Stewart A.J., Kurz E.U. Overexpression of a transporter gene in a multidrug-resistant human lung cancer cell line. Science 1992, 258:1650-1654.
34. Doyle L.A., Yang W., Abruzzo L.V., Krogmann T., Gao Y., Rishi A.K., Ross D.D. A multidrug resistance transporter from human MCF-7 breast cancer cells. Proc. Natl. Acad. Sci. U.S.A. 1998, 95:15665-15670.
35. Hsu S.I., Lothstein L., Horwitz S.B. Differential overexpression of three mdr gene family members in multidrug-resistant J774.2 mouse cells. Evidence that distinct P-glycoprotein precursors are encoded by unique mdr genes. J. Biol. Chem. 1989, 264:12053-12062.
36. Thiebaut F., Tsuruo T., Hamada H., Gottesman M.M., Pastan I., Willingham M.C. Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proc. Natl. Acad. Sci. U.S.A. 1987, 84:7735-7738.
37. Terao T., Hisanaga E., Sai Y., Tamai I., Tsuji A. Active secretion of drugs from the small intestinal epithelium in rats by P-glycoprotein functioning as an absorption barrier. J. Pharm. Pharmacol. 1996, 48:1083-1089.
38. Stephens R.H., O'Neill C.A., Bennett J., Humphrey M., Henry B., Rowland M., Warhurst G. Resolution of P-glycoprotein and non-P-glycoprotein effects on drug permeability using intestinal tissues from mdr1a (-/-) mice. Br. J. Pharmacol. 2002, 135:2038-2046.
39. Drescher S., Glaeser H., Mürdter T., Hitzl M., Eichelbaum M., Fromm M.F. P-glycoprotein-mediated intestinal and biliary digoxin transport in humans. Clin. Pharmacol. Ther. 2003, 73:223-231.
40. Annaert P.P., Turncliff R.Z., Booth C.L., Thakker D.R., Brouwer K.L. P-glycoprotein-mediated in vitro biliary excretion in sandwich-cultured rat hepatocytes. Drug Metab. Dispos. 2001, 29:1277-1283.
41. de Lannoy I.A., Mandin R.S., Silverman M. Renal secretion of vinblastine, vincristine and colchicine in vivo. Pharmacol. Exp. Ther. 1994, 268:388-395.
42. Cordon-Cardo C., O'Brien J.P., Casals D., Rittman-Grauer L., Biedler J.L., Melamed M.R., Bertino J.R. Multidrug-resistance gene (P-glycoprotein) is expressed by endothelial cells at blood-brain barrier sites. Proc. Natl. Acad. Sci. U.S.A. 1989, 86:695-698.
43. Tatsuta T., Naito M., Oh-hara T., Sugawara I., Tsuruo T. Functional involvement of P-glycoprotein in blood-brain barrier. J. Biol. Chem. 1992, 267:20383-20391.
44. Schinkel A.H., Smit J.J., van Tellingen O., Beijnen J.H., Wagenaar E., van Deemter L., Mol C.A., van der Valk M.A., Robanus-Maandag E.C., te Riele H.P., et al. Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs. Cell 1994, 77:491-502.
45. Tahara H., Kusuhara H., Fuse E., Sugiyama Y. P-glycoprotein plays a major role in the efflux of fexofenadine in the small intestine and blood-brain barrier, but only a limited role in its biliary excretion. Drug Metab. Dispos. 2005, 33:963-968.
46. Zhang Y., Benet L.Z. The gut as a barrier to drug absorption: combined role of cytochrome P450 3A and P-glycoprotein. Clin. Pharmacokinet. 2001, 40:159-168.
47. Chan L.M., Lowes S., Hirst B.H. The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability. Eur. J. Pharm. Sci. 2004, 21:25-51.
48. Dietrich C.G., Geier A., Oude Elferink R.P. ABC of oral bioavailability: transporters as gatekeepers in the gut. Gut 2003, 52:1788-1795.
49. Haimeur A., Conseil G., Deeley R.G., Cole S.P. The MRP-related and BCRP/ABCG2 multidrug resistance proteins: biology, substrate specificity and regulation. Curr. Drug Metab. 2004, 5:21-53.
50. Leslie E.M., Deeley R.G., Cole S.P. Multidrug resistance proteins: role of P-glycoprotein, MRP1, MRP2, and BCRP (ABCG2) in tissue defense. Toxicol. Appl. Pharmacol. 2005, 204:216-237.
51. Burk O., Arnold K.A., Geick A., Tegude H., Eichelbaum M. A role for constitutive androstane receptor in the regulation of human intestinal MDR1 expression. Biol. Chem. 2005, 386:503-513.
52. Ee P.L., Kamalakaran S., Tonetti D., He X., Ross D.D., Beck W.T. Identification of a novel estrogen response element in the breast cancer resistance protein (ABCG2) gene. Cancer Res. 2004, 64:1247-1251.
53. Szatmari I., Vámosi G., Brazda P., Balint B.L., Benko S., Széles L., Jeney V., Ozvegy-Laczka C., Szántó A., Barta E., Balla J., Sarkadi B., Nagy L. Peroxisome proliferator-activated receptor gamma-regulated ABCG2 expression confers cytoprotection to human dendritic cells. J. Biol. Chem. 2006, 281:23812-23823.
54. Huang R., Murry D.J., Kolwankar D., Hall S.D., Foster D.R. Vincristine transcriptional regulation of efflux drug transporters in carcinoma cell lines. Biochem. Pharmacol. 2006, 71:1695-1704.
55. Mani S., Huang H., Sundarababu S., Liu W., Kalpana G., Smith A.B., Horwitz S.B. Activation of the steroid and xenobiotic receptor (human pregnane X receptor) by nontaxane microtubule-stabilizing agents. Clin. Cancer Res. 2005, 11:6359-6369.
56. Nallani S.C., Goodwin B., Maglich J.M., Buckley D.J., Buckley A.R., Desai P.B. Induction of cytochrome P450 3A by paclitaxel in mice: pivotal role of the nuclear xenobiotic receptor, pregnane X receptor. Drug Metab. Dispos. 2003, 31:681-684.
57. Gustafson D.L., Long M.E., Bradshaw E.L., Merz A.L., Kerzic P.J. P450 induction alters paclitaxel pharmacokinetics and tissue distribution with multiple dosing. Cancer Chemother. Pharmacol. 2005, 56:248-254.
58. Staudinger J.L., Goodwin B., Jones S.A., Hawkins-Brown D., MacKenzie K.I., LaTour A., Liu Y., Klaassen C.D., Brown K.K., Reinhard J., Willson T.M., Koller B.H., Kliewer S.A. The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity. Proc. Natl. Acad. Sci. U.S.A. 2001, 98:3369-3374.
59. Lehmann J.M., McKee D.D., Watson M.A., Willson T.M., Moore J.T., Kliewer S.A. The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions. J. Clin. Invest. 1998, 102:1016-1023.
60. Bertilsson G., Heidrich J., Svensson K., Asman M., Jendeberg L., Sydow-Bäckman M., Ohlsson R., Postlind H., Blomquist P., Berkenstam A. Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction. Proc. Natl. Acad. Sci. U.S.A. 1998, 95:12208-12213.
61. Bauer B., Hartz A.M., Fricker G., Miller D.S. Pregnane X receptor up-regulation of P-glycoprotein expression and transport function at the blood-brain barrier. Mol. Pharmacol. 2004, 66:413-419.
62. Dotzlaw H., Leygue E., Watson P., Murphy L.C. The human orphan receptor PXR messenger RNA is expressed in both normal and neoplastic breast tissue. Clin. Cancer Res. 1999, 5:2103-2107.
63. Chen Y., Tang Y., Wang M.T., Zeng S., Nie D. Human pregnane X receptor and resistance to chemotherapy in prostate cancer. Cancer Res. 2007, 67:10361-10367.
64. Owen A., Chandler B., Back D.J., Khoo S.H. Expression of pregnane-X-receptor transcript in peripheral blood mononuclear cells and correlation with MDR1 mRNA. Antivir. Ther. 2004, 9:819-821.
65. Albermann N., Schmitz-Winnenthal F.H., Z'graggen K., Volk C., Hoffmann M.M., Haefeli W.E., Weiss J. Expression of the drug transporters MDR1/ABCB1, MRP1/ABCC1, MRP2/ABCC2, BCRP/ABCG2, and PXR in peripheral blood mononuclear cells and their relationship with the expression in intestine and liver. Biochem. Pharmacol. 2005, 70:949-958.
66. Lamba V., Yasuda K., Lamba J.K., Assem M., Davila J., Strom S., Schuetz E.G. PXR (NR1I2): splice variants in human tissues, including brain, and identification of neurosteroids and nicotine as PXR activators. Toxicol. Appl. Pharmacol. 2004, 199:251-265.
67. Masuyama H., Hiramatsu Y., Mizutani Y., Inoshita H., Kudo T. The expression of pregnane X receptor and its target gene, cytochrome P450 3A1, in perinatal mouse. Mol. Cell. Endocrinol. 2001, 172:47-56.
68. Dubrac S., Elentner A., Ebner S., Horejs-Hoeck J., Schmuth M. Modulation of T lymphocyte function by the pregnane X receptor. J. Immunol. 2010, 184:2949-2957.
69. Miki Y., Suzuki T., Kitada K., Yabuki N., Shibuya R., Moriya T., Ishida T., Ohuchi N., Blumberg B., Sasano H. Expression of the steroid and xenobiotic receptor and its possible target gene, organic anion transporting polypeptide-A, in human breast carcinoma. Cancer Res. 2006, 66:535-542.
70. Zhou J., Liu M., Zhai Y., Xie W. The antiapoptotic role of pregnane X receptor in human colon cancer cells. Mol. Endocrinol. 2008, 22:868-880.
71. Mensah-Osman E.J., Thomas D.G., Tabb M.M., Larios J.M., Hughes D.P., Giordano T.J., Lizyness M.L., Rae J.M., Blumberg B., Hollenberg P.F., Baker L.H. Expression levels and activation of a PXR variant are directly related to drug resistance in osteosarcoma cell lines. Cancer 2007, 109:957-965.
72. Gupta D., Venkatesh M., Wang H., Kim S., Sinz M., Goldberg G.L., Whitney K., Longley C., Mani S. Expanding the roles for pregnane X receptor in cancer: proliferation and drug resistance in ovarian cancer. Clin. Cancer Res. 2008, 14:5332-5340.
73. Masuyama H., Hiramatsu Y., Kodama J., Kudo T. Expression and potential roles of pregnane X receptor in endometrial cancer. J. Clin. Endocrinol. Metab. 2003, 88:4446-4454.
74. Masuyama H., Nakatsukasa H., Takamoto N., Hiramatsu Y. Down-regulation of pregnane X receptor contributes to cell growth inhibition and apoptosis by anticancer agents in endometrial cancer cells. Mol. Pharmacol. 2007, 72:1045-1053.
75. Sonoda J., Pei L., Evans R.M. Nuclear receptors: decoding metabolic disease. FEBS Lett. 2008, 582:2-9.
76. Chen T. Nuclear receptor drug discovery. Curr. Opin. Chem. Biol. 2008, 12:418-426.
77. Kliewer S.A., Moore J.T., Wade L., Staudinger J.L., Watson M.A., Jones S.A., McKee D.D., Oliver B.B., Willson T.M., Zetterström R.H., Perlmann T., Lehmann J.M. An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway. Cell 1998, 92:73-82.
78. Blumberg B., Sabbagh W., Juguilon H., Bolado J., van Meter C.M., Ong E.S., Evans R.M. SXR, a novel steroid and xenobiotic-sensing nuclear receptor. Genes Dev. 1998, 12:3195-3205.
79. Squires E.J., Sueyoshi T., Negishi M. Cytoplasmic localization of pregnane X receptor and ligand-dependent nuclear translocation in mouse liver. J. Biol. Chem. 2004, 279:49307-49314.
80. Saradhi M., Sengupta A., Mukhopadhyay G., Tyagi R.K. Pregnane and Xenobiotic Receptor (PXR/SXR) resides predominantly in the nuclear compartment of the interphase cell and associates with the condensed chromosomes during mitosis. Biochim. Biophys. Acta 2005, 1746:85-94.
81. Johnson D.R., Li C.W., Chen L.Y., Ghosh J.C., Chen J.D. Regulation and Binding of Pregnane X Receptor by Nuclear Receptor Corepressor Silencing Mediator of Retinoid and Thyroid Hormone Receptors (SMRT). Mol. Pharmacol. 2006, 69:99-108.
82. Pondugula S.R., Brimer-Cline C., Wu J., Schuetz E.G., Tyagi R.K., Chen T. A phosphomimetic mutation at threonine-57 abolishes transactivation activity and alters nuclear localization pattern of human pregnane x receptor. Drug Metab. Dispos. 2009, 37:719-730.
83. Gong H., Sinz M.W., Feng Y., Chen T., Venkataramanan R., Xie W. Animal models of xenobiotic receptors in drug metabolism and diseases. Meth. Enzymol. 2005, 400:598-618.
84. Goodwin B., Hodgson E., Liddle C. The orphan human pregnane X receptor mediates the transcriptional activation of CYP3A4 by rifampicin through a distal enhancer module. Mol. Pharmacol. 1999, 56:1329-1339.
85. Timsit Y.E., Negishi M. CAR and PXR: the xenobiotic-sensing receptors. Steroids 2007, 72:231-246.
86. Hu X., Lazar M.A. The CoRNR motif controls the recruitment of corepressors by nuclear hormone receptors. Nature 1999, 402:93-96.
87. Lin W., Wu J., Dong H., Bouck D., Zeng F.Y., Chen T. Cyclin-dependent kinase 2 negatively regulates human pregnane X receptor-mediated CYP3A4 gene expression in HepG2 liver carcinoma cells. J. Biol. Chem. 2008, 283:30650-30657.
88. Watkins R.E., Wisely G.B., Moore L.B., Collins J.L., Lambert M.H., Williams S.P., Willson T.M., Kliewer S.A., Redinbo M.R. The human nuclear xenobiotic receptor PXR: structural determinants of directed promiscuity. Science 2001, 292:2329-2333.
89. Watkins R.E., Noble S.M., Redinbo M.R. Structural insights into the promiscuity and function of the human pregnane X receptor. Curr. Opin. Drug Discov. Dev. 2002, 5:150-158.
90. Sinz M., Kim S., Zhu Z., Chen T., Anthony M., Dickinson K., Rodrigues A.D. Evaluation of 170 xenobiotics as transactivators of human pregnane X receptor (hPXR) and correlation to known CYP3A4 drug interactions. Curr. Drug Metab. 2006, 7:375-388.
91. Sonoda J., Chong L.W., Downes M., Barish G.D., Coulter S., Liddle C., Lee C.H., Evans R.M. Pregnane X receptor prevents hepatorenal toxicity from cholesterol metabolites. Proc. Natl. Acad. Sci. U.S.A. 2005, 102:2198-2203.
92. Dussault I., Lin M., Hollister K., Wang E.H., Synold T.W., Forman B.M. Peptide mimetic HIV protease inhibitors are ligands for the orphan receptor SXR. J. Biol. Chem. 2001, 276:33309-33312.
93. Dürr D., Stieger B., Kullak-Ublick G.A., Rentsch K.M., Steinert H.C., Meier P.J., Fattinger K. St John's Wort induces intestinal P-glycoprotein/MDR1 and intestinal and hepatic CYP3A4. Clin. Pharmacol. Ther. 2000, 68:598-604.
94. Greiner B., Eichelbaum M., Fritz P., Kreichgauer H.P., von Richter O., Zundler J., Kroemer H.K. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin. J. Clin. Invest. 1999, 104:147-153.
95. Jigorel E., Le Vee M., Boursier-Neyret C., Parmentier Y., Fardel O. Differential regulation of sinusoidal and canalicular hepatic drug transporter expression by xenobiotics activating drug-sensing receptors in primary human hepatocytes. Drug Metab. Dispos. 2006, 34:1756-1763.
96. Oscarson M., Burk O., Winter S., Schwab M., Wolbold R., Dippon J., Eichelbaum M., Meyer U.A. Effects of rifampicin on global gene expression in human small intestine. Pharmacogenet. Genomics 2007, 17:907-918.
97. Richert L., Liguori M.J., Abadie C., Heyd B., Mantion G., Halkic N., Waring J.F. Gene expression in human hepatocytes in suspension after isolation is similar to the liver of origin, is not affected by hepatocyte cold storage and cryopreservation, but is strongly changed after hepatocyte plating. Drug Metab. Dispos. 2006, 34:870-879.
98. Westphal K., Weinbrenner A., Zschiesche M., Franke G., Knoke M., Oertel R., Fritz P., von Richter O., Warzok R., Hachenberg T., Kauffmann H.M., Schrenk D., Terhaag B., Kroemer H.K., Siegmund W. Induction of P-glycoprotein by rifampin increases intestinal secretion of talinolol in human beings: a new type of drug/drug interaction. Clin. Pharmacol. Ther. 2000, 68:345-355.
99. Giessmann T., May K., Modess C., Wegner D., Hecker U., Zschiesche M., Dazert P., Grube M., Schroeder E., Warzok R., Cascorbi I., Kroemer H.K., Siegmund W. Carbamazepine regulates intestinal P-glycoprotein and multidrug resistance protein MRP2 and influences disposition of talinolol in humans. Clin. Pharmacol. Ther. 2004, 76:192-200.
100. Johne A., Brockmöller J., Bauer S., Maurer A., Langheinrich M., Roots I. Pharmacokinetic interaction of digoxin with an herbal extract from St John's wort (Hypericum perforatum). Clin. Pharmacol. Ther. 1999, 66:338-345.
101. Hamman M.A., Bruce M.A., Haehner-Daniels B.D., Hall S.D. The effect of rifampin administration on the disposition of fexofenadine. Clin. Pharmacol. Ther. 2001, 69:114-121.
102. Wang T., Ma X., Krausz K.W., Idle J.R., Gonzalez F.J. Role of pregnane X receptor in control of all-trans retinoic acid (ATRA) metabolism and its potential contribution to ATRA resistance. J. Pharmacol. Exp. Ther. 2008, 324:674-684.
103. Desai P.B., Nallani S.C., Sane R.S., Moore L.B., Goodwin B.J., Buckley D.J., Buckley A.R. Induction of cytochrome P450 3A4 in primary human hepatocytes and activation of the human pregnane X receptor by tamoxifen and 4-hydroxytamoxifen. Drug Metab. Dispos. 2002, 30:608-612.
104. Zimmermann K., Wittman M.D., Saulnier M.G., Velaparthi U., Sang X., Frennesson D.B., Struzynski C., Seitz S.P., He L., Carboni J.M., Li A., Greer A.F., Gottardis M., Attar R.M., Yang Z., Balimane P., Discenza L.N., Lee F.Y., Sinz M., Kim S., Vyas D. SAR of PXR transactivation in benzimidazole-based IGF-1R kinase inhibitors. Bioorg. Med. Chem. Lett. 2010, 20:1744-1748.
105. Huang H., Wang H., Sinz M., Zoeckler M., Staudinger J., Redinbo M.R., Teotico D.G., Locker J., Kalpana G.V., Mani S. Inhibition of drug metabolism by blocking the activation of nuclear receptors by ketoconazole. Oncogene 2007, 26:258-268.
106. Healan-Greenberg C., Waring J.F., Kempf D.J., Blomme E.A., Tirona R.G., Kim R.B. A human immunodeficiency virus protease inhibitor is a novel functional inhibitor of human pregnane X receptor. Drug Metab. Dispos. 2008, 36:500-507.
107. Zhou C., Poulton E.J., Grün F., Bammler T.K., Blumberg B., Thummel K.E., Eaton D.L. The dietary isothiocyanate sulforaphane is an antagonist of the human steroid and xenobiotic nuclear receptor. Mol. Pharmacol. 2007, 71:220-229.
108. Wang H., Li H., Moore L.B., Johnson M.D., Maglich J.M., Goodwin B., Ittoop O.R., Wisely B., Creech K., Parks D.J., Collins J.L., Willson T.M., Kalpana G.V., Venkatesh M., Xie W., Cho S.Y., Roboz J., Redinbo M., Moore J.T., Mani S. The phytoestrogen coumestrol is a naturally occurring antagonist of the human pregnane X receptor. Mol. Endocrinol. 2008, 22:838-857.
109. Y. Chen, Y. Tang, G.T. Robbins, D. Nie, Camptothecin attenuates cytochrome P450 3A4 induction by blocking the activation of human pregnane X receptor, J. Pharmacol. Exp. Ther. doi:10.1124/jpet.110.168294.
110. Raynal C., Pascussi J.M., Leguelinel G., Breuker C., Kantar J., Lallemant B., Poujol S., Bonnans C., Joubert D., Hollande F., Lumbroso S., Brouillet J.P., Evrard A. Pregnane X Receptor (PXR) expression in colorectal cancer cells restricts irinotecan chemosensitivity through enhanced SN-38 glucuronidation. Mol. Cancer 2010, 9:46.
111. Ekins S., Chang C., Mani S., Krasowski M.D., Reschly E.J., Iyer M., Kholodovych V., Ai N., Welsh W.J., Sinz M., Swaan P.W., Patel R., Bachmann K. K, Human pregnane X receptor antagonists and agonists define molecular requirements for different binding sites. Mol. Pharmacol. 2007, 72:592-603.
112. Ekins S., Kholodovych V., Ai N., Sinz M., Gal J., Gera L., Welsh W.J., Bachmann K., Mani S. Computational discovery of novel low micromolar human pregnane X receptor antagonists. Mol. Pharmacol. 2008, 74:662-672.
113. Xue Y., Chao E., Zuercher W.J., Willson T.M., Collins J.L., Redinbo M.R. Crystal structure of the PXR-T1317 complex provides a scaffoldto examine the potential for receptor antagonism. Bioorg. Med. Chem. 2007, 15:2156-2166.
114. Thakur J.K., Arthanari H., Yang F., Pan S.J., Fan X., Breger J., Frueh D.P., Gulshan K., Li D.K., Mylonakis E., Struhl K., Moye-Rowley W.S., Cormack B.P., Wagner G., Näär A.M. A nuclear receptor-like pathway regulating multidrug resistance in fungi. Nature 2008, 452:604-609.