The pregnane X receptor down-regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for ("squelching") SRC-1 coactivator

British Journal of Pharmacology

Volumn 173, Issue 10, 2016, Pages 1703-1715

  Hyrsova, Lucie ^a   Smutny, Tomas ^a   Carazo, Alejandro ^a   Moravcik, Stefan ^a   Mandikova, Jana ^a   Trejtnar, Frantisek ^a   Gerbal Chaloin, Sabine ^b,c   Pavek, Petr ^a  

^a Charles University in Prague Faculty of Pharmacy   (Czech Republic)

^b INSERM   (France)

^c UNIV MONTPELLIER   (France)

Author keywords

[No Author keywords available]

Indexed keywords

HEPATOCYTE NUCLEAR FACTOR 4ALPHA; HYPERFORIN; MESSENGER RNA; ORGANIC CATION TRANSPORTER 1; PEROXISOME PROLIFERATOR ACTIVATED RECEPTOR GAMMA COACTIVATOR 1ALPHA; PREGNANE X RECEPTOR; RIFAMPICIN; STEROID RECEPTOR COACTIVATOR 1; UPSTREAM STIMULATORY FACTOR 1; NCOA1 PROTEIN, HUMAN; OCTAMER TRANSCRIPTION FACTOR 1; PHLOROGLUCINOL; POU2F1 PROTEIN, HUMAN; STEROID RECEPTOR; TERPENE;

ADULT; AGED; ARTICLE; CELL DIFFERENTIATION; CELL TRANSPORT; CONTROLLED STUDY; DOWN REGULATION; FEMALE; HUMAN; HUMAN CELL; LIVER CELL; MUTATION; PRIORITY JOURNAL; PROMOTER REGION; PROTEIN ANALYSIS; PROTEIN EXPRESSION; PROTEIN FUNCTION; ANALOGS AND DERIVATIVES; DOSE RESPONSE; GENETICS; HEP-G2 CELL LINE; METABOLISM; STRUCTURE ACTIVITY RELATION; TUMOR CELL CULTURE;

DOSE-RESPONSE RELATIONSHIP, DRUG; DOWN-REGULATION; HEP G2 CELLS; HEPATOCYTES; HUMANS; NUCLEAR RECEPTOR COACTIVATOR 1; OCTAMER TRANSCRIPTION FACTOR-1; PHLOROGLUCINOL; RECEPTORS, STEROID; RIFAMPIN; STRUCTURE-ACTIVITY RELATIONSHIP; TERPENES; TUMOR CELLS, CULTURED;

EID: 84962631812     PISSN: 00071188     EISSN: 14765381     Source Type: Journal    
DOI: 10.1111/bph.13472     Document Type: Article

References (38)

1. Alexander SP, Kelly E, Marrion N, Peters JA, Benson HE, Faccenda E, et al., (2015a). The Concise Guide to PHARMACOLOGY 2015/16: Transporters. Br J Pharmacol 172: 6110-6202.
2. Alexander SP, Cidlowski JA, Kelly E, Marrion N, Peters JA, Benson HE, et al., (2015b). The Concise Guide to PHARMACOLOGY 2015/16: Nuclear hormone receptors. Br J Pharmacol 172: 5956-5978.
3. Austin G, Holcroft A, Rinne N, Wang L, Clark RE, (2015). Evidence that the pregnane X and retinoid receptors PXR, RAR and RXR may regulate transcription of the transporter hOCT1 in chronic myeloid leukaemia cells. Eur J Haematol 94: 74-78.
4. Badolo L, Bundgaard C, Garmer M, Jensen B, (2013). The role of hepatic transport and metabolism in the interactions between pravastatin or repaglinide and two rOatp inhibitors in rats. Eur J Pharm Sci 49: 767-772.
5. Becker ML, Visser LE, van Schaik RH, Hofman A, Uitterlinden AG, Stricker BH, (2009). Genetic variation in the organic cation transporter 1 is associated with metformin response in patients with diabetes mellitus. Pharmacogenomics J 9: 242-247.
6. Boxberger KH, Hagenbuch B, Lampe JN, (2014). Common drugs inhibit human organic cation transporter 1 (OCT1)-mediated neurotransmitter uptake. Drug Metab Dispos 42: 990-995.
7. Cahill MA, Ernst WH, Janknecht R, Nordheim A, (1994). Regulatory squelching. FEBS Lett 344: 105-108.
8. Curtis MJ, Bond RA, Spina D, Ahluwalia A, Alexander SP, Giembycz MA, et al., (2015). Experimental design and analysis and their reporting: new guidance for publication in BJP. Br J Pharmacol 172: 3461-3471.
9. Doricakova A, Novotna A, Vrzal R, Pavek P, Dvorak Z, (2013). The role of residues T248, Y249 and T422 in the function of human pregnane X receptor. Arch Toxicol 87: 291-301.
10. Gripon P, Rumin S, Urban S, Le Seyec J, Glaise D, Cannie I, et al., (2002). Infection of a human hepatoma cell line by hepatitis B virus. Proc Natl Acad Sci U S A 99: 15655-15660.
11. Hilgendorf C, Ahlin G, Seithel A, Artursson P, Ungell AL, Karlsson J, (2007). Expression of thirty-six drug transporter genes in human intestine, liver, kidney, and organotypic cell lines. Drug Metab Dispos 35: 1333-1340.
12. Huang S, Li X, Yusufzai TM, Qiu Y, Felsenfeld G, (2007). USF1 recruits histone modification complexes and is critical for maintenance of a chromatin barrier. Mol Cell Biol 27: 7991-8002.
13. Chen Y, Tang Y, Guo C, Wang J, Boral D, Nie D, (2012). Nuclear receptors in the multidrug resistance through the regulation of drug-metabolizing enzymes and drug transporters. Biochem Pharmacol 83: 1112-1126.
14. Cho SK, Yoon JS, Lee MG, Lee DH, Lim LA, Park K, et al., (2011). Rifampin enhances the glucose-lowering effect of metformin and increases OCT1 mRNA levels in healthy participants. Clin Pharmacol Ther 89: 416-421.
15. Jigorel E, Le Vee M, Boursier-Neyret C, Parmentier Y, Fardel O, (2006). Differential regulation of sinusoidal and canalicular hepatic drug transporter expression by xenobiotics activating drug-sensing receptors in primary human hepatocytes. Drug Metab Dispos 34: 1756-1763.
16. Jonker JW, Schinkel AH, (2004). Pharmacological and physiological functions of the polyspecific organic cation transporters: OCT1, 2, and 3 (SLC22A1-3). J Pharmacol Exp Ther 308: 2-9.
17. Jonker JW, Wagenaar E, Van Eijl S, Schinkel AH, (2003). Deficiency in the organic cation transporters 1 and 2 (Oct1/Oct2 [Slc22a1/Slc22a2]) in mice abolishes renal secretion of organic cations. Mol Cell Biol 23: 7902-7908.
18. Kajiwara M, Terada T, Asaka J, Aoki M, Katsura T, Ikai I, et al., (2008). Regulation of basal core promoter activity of human organic cation transporter 1 (OCT1/SLC22A1). Am J Physiol Gastrointest Liver Physiol 295: G1211-G1216.
19. Kamiyama Y, Matsubara T, Yoshinari K, Nagata K, Kamimura H, Yamazoe Y, (2007). Role of human hepatocyte nuclear factor 4alpha in the expression of drug-metabolizing enzymes and transporters in human hepatocytes assessed by use of small interfering RNA. Drug Metab Pharmacokinet 22: 287-298.
20. Kliewer SA, Goodwin B, Willson TM, (2002). The nuclear pregnane X receptor: a key regulator of xenobiotic metabolism. Endocr Rev 23: 687-702.
21. Koepsell H, Lips K, Volk C, (2007). Polyspecific organic cation transporters: structure, function, physiological roles, and biopharmaceutical implications. Pharm Res 24: 1227-1251.
22. Le Vee M, Jigorel E, Glaise D, Gripon P, Guguen-Guillouzo C, Fardel O, (2006). Functional expression of sinusoidal and canalicular hepatic drug transporters in the differentiated human hepatoma HepaRG cell line. Eur J Pharm Sci 28: 109-117.
23. Mandikova J, Volkova M, Pavek P, Cesnek M, Janeba Z, Kubicek V, et al., (2013). Interactions with selected drug renal transporters and transporter-mediated cytotoxicity in antiviral agents from the group of acyclic nucleoside phosphonates. Toxicology 311: 135-146.
24. Miao J, Fang S, Bae Y, Kemper JK, (2006). Functional inhibitory cross-talk between constitutive androstane receptor and hepatic nuclear factor-4 in hepatic lipid/glucose metabolism is mediated by competition for binding to the DR1 motif and to the common coactivators, GRIP-1 and PGC-1alpha. J Biol Chem 281: 14537-14546.
25. Min G, Kim H, Bae Y, Petz L, Kemper JK, (2002). Inhibitory cross-talk between estrogen receptor (ER) and constitutively activated androstane receptor (CAR). CAR inhibits ER-mediated signaling pathway by squelching p160 coactivators. J Biol Chem 277: 34626-34633.
26. Nies AT, Koepsell H, Winter S, Burk O, Klein K, Kerb R, et al., (2009). Expression of organic cation transporters OCT1 (SLC22A1) and OCT3 (SLC22A3) is affected by genetic factors and cholestasis in human liver. Hepatology 50: 1227-1240.
27. Pawson AJ, Sharman JL, Benson HE, Faccenda E, Alexander SP, Buneman OP, et al., (2014). The IUPHAR/BPS Guide to PHARMACOLOGY: an expert-driven knowledgebase of drug targets and their ligands. Nucleic Acids Res 42: D1098-D1106.
28. Rulcova A, Krausova L, Smutny T, Vrzal R, Dvorak Z, Jover R, et al., (2013). Glucocorticoid receptor regulates organic cation transporter 1 (OCT1, SLC22A1) expression via HNF4alpha upregulation in primary human hepatocytes. Pharmacol Rep 65: 1322-1335.
29. Saborowski M, Kullak-Ublick GA, Eloranta JJ, (2006). The human organic cation transporter-1 gene is transactivated by hepatocyte nuclear factor-4alpha. J Pharmacol Exp Ther 317: 778-785.
30. Saini SP, Mu Y, Gong H, Toma D, Uppal H, Ren S, et al., (2005). Dual role of orphan nuclear receptor pregnane X receptor in bilirubin detoxification in mice. Hepatology 41: 497-505.
31. Shu Y, Sheardown SA, Brown C, Owen RP, Zhang S, Castro RA, et al., (2007). Effect of genetic variation in the organic cation transporter 1 (OCT1) on metformin action. J Clin Invest 117: 1422-1431.
32. Smutny T, Bitman M, Urban M, Dubecka M, Vrzal R, Dvorak Z, et al., (2014). U0126, a mitogen-activated protein kinase kinase 1 and 2 (MEK1 and 2) inhibitor, selectively up-regulates main isoforms of CYP3A subfamily via a pregnane X receptor (PXR) in HepG2 cells. Arch Toxicol 88: 2243-2259.
33. Wada T, Kang HS, Jetten AM, Xie W, (2008). The emerging role of nuclear receptor RORalpha and its crosstalk with LXR in xeno- and endobiotic gene regulation. Exp Biol Med 233: 1191-1201.
34. Wang DS, Jonker JW, Kato Y, Kusuhara H, Schinkel AH, Sugiyama Y, (2002). Involvement of organic cation transporter 1 in hepatic and intestinal distribution of metformin. J Pharmacol Exp Ther 302: 510-515.
35. Wang DS, Kusuhara H, Kato Y, Jonker JW, Schinkel AH, Sugiyama Y, (2003). Involvement of organic cation transporter 1 in the lactic acidosis caused by metformin. Mol Pharmacol 63: 844-848.
36. Wang JC, Stafford JM, Granner DK, (1998). SRC-1 and GRIP1 coactivate transcription with hepatocyte nuclear factor 4. J Biol Chem 273: 30847-30850.
37. Watt AJ, Garrison WD, Duncan SA, (2003). HNF4: a central regulator of hepatocyte differentiation and function. Hepatology 37: 1249-1253.
38. Zhai Y, Wada T, Zhang B, Khadem S, Ren S, Kuruba R, et al., (2010). A functional cross-talk between liver X receptor-alpha and constitutive androstane receptor links lipogenesis and xenobiotic responses. Mol Pharmacol 78: 666-674.