The human bile salt export pump: Characterization of substrate specificity and identification of inhibitors

Gastroenterology

Volumn 123, Issue 5, 2002, Pages 1649-1658

  Byrne, Jane A ^a   Strautnieks, Sandra S ^a   MieliVergani, Giorgina ^a   Higgins, Christopher F ^b   Linton, Kenneth J ^b   Thompson, Richard J ^a  

^a KING S COLLEGE HOSPITAL   (United Kingdom)

^b HAMMERSMITH HOSPITAL   (United Kingdom)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATASE; BILE SALT; CYCLOSPORIN A; GENE PRODUCT; GLIBENCLAMIDE; GLYCOCHENODEOXYCHOLIC ACID; GLYCOCHOLIC ACID; PROGESTERONE; PROTEIN ABCB11; RIFAMPICIN; TAMOXIFEN; TAUROCHENODEOXYCHOLIC ACID; TAUROCHOLIC ACID; UNCLASSIFIED DRUG;

ARTICLE; BACULOVIRUS; BILE FLOW; BILE SECRETION; CHOLESTASIS; CONTROLLED STUDY; ENZYME ACTIVITY; ENZYME ASSAY; ENZYME INHIBITION; FLOW RATE; GENE EXPRESSION; HEPATOBILIARY SYSTEM; HUMAN; HUMAN TISSUE; INSECT CELL; MICHAELIS CONSTANT; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; PROTEIN EXPRESSION; VELOCITY;

EID: 0036829089     PISSN: 00165085     EISSN: None     Source Type: Journal    
DOI: 10.1053/gast.2002.36591     Document Type: Article

References (41)

1. Kullak-Ublick GA, Beuers U, Paumgartner G. Hepatobiliary transport. J Hepatol 2000;32:3-18.
2. Hofmann AF. Bile acids. In: Arias IM, ed. The Liver: Biology and Pathobiology. 3rd Ed. New York: Raven, 1994:677-718.
3. Marschall H-U, Matern H, Sjövall J, Matern S. Conjugation of bile acids. In: Fromm H, Leuschner U, eds. Bile Acids-cholestasisgallstones. Dordrecht, the Netherlands: Kluwer, 1996:13-22.
4. Higgins CF. ABC transporters: From microorganisms to man. Annu Rev Cell Biol 1992;8:67-113.
5. Dean M, Hamon Y, Chimini G. The human ATP-binding cassette (ABC) transporter superfamily. J Lipid Res 2001;42:1007-1017.
6. Gerloff T, Stieger B, Hagenbuch B, Madon J, Landmann L, Roth J, Hofmann AF, Meier PJ. The sister of P-glycoprotein represents the canalicular bile salt export pump of mammalian liver. J Biol Chem 1998;273:10046-10050.
7. Green RM, Hoda F, Ward KL. Molecular cloning and characterization of the murine bile salt export pump. Gene 2000;241:117-123.
8. Noe J, Hagenbuch B, Meier PJ, St-Pierre MV. Characterization of the mouse bile salt export pump overexpressed in the baculovirus system. Hepatology 2001;33:1223-1231.
9. Cai SY, Wang L, Ballatori N, Boyer JL. Bile salt export pump is highly conserved during vertebrate evolution and its expression is inhibited by PFIC type II mutations. Am J Physiol Gastrointest Liver Physiol 2001;281:G316-322.
10. Strautnieks SS, Bull LN, Knisely AS, Kocoshis SA, Dahl N, Arnell H, Sokal E, Dahan K, Childs S, Ling V, Tanner MS, Kagalwalla AF, Nemeth A, Pawlowska J, Baker A, Mieli-Vergani G, Freimer NB, Gardiner RM, Thompson RJ. A gene encoding a liver-specific ABC transporter is mutated in progressive familial intrahepatic cholestasis. Nat Genet 1998;20:233-238.
11. Jansen PL, Strautnieks SS, Jacquemin E, Hadchouel M, Sokal EM, Hooiveld GJ, Koning JH, De Jager-Krikken A, Kuipers F, Stellaard F, Bijleveld CM, Gouw A, Van Goor H, Thompson RJ, Muller M. Hepatocanalicular bile salt export pump deficiency in patients with progressive familial intrahepatic cholestasis. Gastroenterology 1999;117:1370-1379.
12. Byrne J, Soler E, Strautnieks S, Thompson R. Genetic analysis of progressive familial intrahepatic cholestasis. In: van Berge Henegouwen GP, Keppler D, Leuschner U, Paumgartner G, Stiehl A, eds. Biology of Bile Acids in Health and Disease. Dordrecht, the Netherlands: Kluwer, 2001:288-300.
13. Chen HL, Chang PS, Hsu HC, Ni YH, Hsu HY, Lee JH, Jeng YM, Shau WY, Chang MH. FIC1 and BSEP defects in Taiwanese patients with chronic intrahepatic cholestasis with low gamma-glutamyltranspeptidase levels. J Pediatr 2002;140:119-124.
14. Bohan A, Boyer JL. Mechanisms of hepatic transport of drugs: Implications for cholestatic drug reactions. Semin Liver Dis 2002;22:123-136.
15. Bissell DM, Gores GJ, Laskin DL, Hoofnagle JH. Drug-induced liver injury: Mechanisms and test systems. Hepatology 2001;33:1009-1013.
16. Stieger B, Fattinger K, Madon J, Kullak-Ublick GA, Meier PJ. Drug-and estrogen-induced cholestasis through inhibition of the hepatocellular bile salt export pump (Bsep) of rat liver. Gastroenterology 2000;118:422-430.
17. Fattinger K, Funk C, Pantze M, Weber C, Reichen J, Stieger B, Meier PJ. The endothelin antagonist bosentan inhibits the canalicular bile salt export pump: A potential mechanism for hepatic adverse reactions. Clin Pharmacol Ther 2001;69:223-231.
18. Funk C, Pantze M, Jehle L, Ponelle C, Scheuermann G, Lazendic M, Gasser R. Troglitazone-induced intrahepatic cholestasis by an interference with the hepatobiliary export of bile acids in male and female rats. Correlation with the gender difference in troglitazone sulfate formation and the inhibition of the canalicular bile salt export pump (Bsep) by troglitazone and troglitazone sulfate. Toxicology 2001;167:83-98.
19. Lammert F, Marschall HU, Glantz A, Matern S. Intrahepatic cholestasis of pregnancy: Molecular pathogenesis, diagnosis and management. J Hepatol 2000;33:1012-1021.
20. de Vree JM, Jacquemin E, Sturm E, Cresteil D, Bosma PJ, Aten J, Deleuze JF, Desrochers M, Burdelski M, Bernard O, Oude Elferink RP, Hadchouel M. Mutations in the MDR3 gene cause progressive familial intrahepatic cholestasis. Proc Natl Acad Sci U S A 1998;95:282-287.
21. Dixon PH, Weerasekera N, Linton KJ, Donaldson O, Chambers J, Egginton E, Weaver J, Nelson-Piercy C, Swiet M, Warnes G, Elias E, Higgins CF, Johnston DG, McCarthy MI, Williamson C. Heterozygous MDR3 missense mutation associated with intrahepatic cholestasis of pregnancy: Evidence for a defect in protein trafficking. Hum Mol Genet 2000;9:1209-1217.
22. Jacquemin E, De Vree JM, Cresteil D, Sokal EM, Sturm E, Dumont M, Scheffer GL, Paul M, Burdelski M, Bosma PJ, Bernard O, Hadchouel M, Elferink RP. The wide spectrum of multidrug resistance 3 deficiency: From neonatal cholestasis to cirrhosis of adulthood. Gastroenterology 2001;120:1448-1458.
23. Rosmorduc O, Hermelin B, Poupon R. MDR3 gene defect in adults with symptomatic intrahepatic and gallbladder cholesterol cholelithiasis. Gastroenterology 2001;120:1459-1467.
24. Meier PJ, Stieger B. Bile salt transporters. Annu Rev Physiol 2002;64:635-661.
25. Muller M, Ishikawa T, Berger U, Klunemann C, Lucka L, Schreyer A, Kannicht C, Reutter W, Kurz G, Keppler D. ATP-dependent transport of taurocholate across the hepatocyte canalicular membrane mediated by a 110-kDa glycoprotein binding ATP and bile salt. J Biol Chem 1991;266:18920-18926.
26. Nishida T, Gatmaitan Z, Che M, Arias IM. Rat liver canalicular membrane vesicles contain an ATP-dependent bile acid transport system. Proc Natl Acad Sci U S A 1991;88:6590-6594.
27. Stieger B, O'Neill B, Meier PJ. ATP-dependent bile-salt transport in canalicular rat liver plasma-membrane vesicles. Biochem J 1992;284:67-74.
28. Wolters H KF, Slooff MJ, Vonk RJ. Adenosine triphosphate-dependent taurocholate transport in human liver plasma membranes. J Clin Invest 1992;90:2321-2326.
29. Elferink R, Groen AK. Genetic defects in hepatobiliary transport. Biochim Biophys Acta 2002;1586:129-145.
30. Appel RD, Bairoch A, Hochstrasser DF. A new generation of information retrieval tool for biologists: The example of ExPASy WWW server. Trends Biochem Sci 1994;19:2581-260. SWISSPROT available from: http://www.expasy.ch/sprot/sprottop.html.
31. Sarkadi B, Price EM, Boucher RC, Germann UA, Scarborough GA. Expression of the human multidrug resistance cDNA in insect cells generates a high activity drug-stimulated membrane ATPase. J Biol Chem 1992;267:4854-4858.
32. Wang R, Salem M, Yousef IM, Tuchweber B, Lam P, Childs SJ, Helgason CD, Ackerley C, Phillips MJ, Ling V. Targeted inactivation of sister of P-glycoprotein gene (spgp) in mice results in nonprogressive but persistent intrahepatic cholestasis. Proc Natl Acad Sci U S A 2001;98:2011-2016.
33. Hofmann A. Bile secretion in mice and men. Hepatology 2001;34:848-849.
34. Eppens EF, van Mil SW, de Vree JM, Mok KS, Juijn JA, Oude Elferink RP, Berger R, Houwen RH, Klomp LW. FIC1, the protein affected in two forms of hereditary cholestasis, is localized in the cholangiocyte and the canalicular membrane of the hepatocyte. J Hepatol 2001;35:436-443.
35. Bull LN, van Eijk J, Pawlikowska L, DeYoung JA, Juijn JA, Liao M, Klomp LW, Lomri N, Berger R, Scharschmidt BF, Knisely AS, Houwen RH, Freimer NB. A gene encoding a P-type ATPase mutated in two forms of hereditary cholestasis. Nat Genet 1998;18:219-224.
36. Ujhazy P, Ortiz D, Misra S, Li S, Moseley J, Jones H, Arias IM. Familial intrahepatic cholestasis 1: Studies of localization and function. Hepatology 2001;34:768-775.
37. Stieger B. FIC1: Another bile salt carrier within the enterohepatic circulation? J Hepatol 2001;35:522-524.
38. Vavricka SR, Van Montfoort J, Ha HR, Meier PJ, Fattinger K. Interactions of rifamycin SV and rifampicin with organic anion uptake systems of human liver. Hepatology 2002;36:164-172.
39. Kadmon MKC, Bohme M, Ishikawa T, Gorgas K, Otto G, Herfarth C, Keppler D. Inhibition by cyclosporin A of adenosine triphosphate-dependent transport from the hepatocyte into bile. Gastroenterology 1993;104:1507-1514.
40. Meng U, Reyes H, Palma J, Hernandez I, Ribalta J, Sjovall J. Profiles of bile acids and progesterone metabolites in the urine and serum of women with intrahepatic cholestasis of pregnancy. J Hepatol 1997;27:346-357.
41. Riippa P, Kauppila A, Sundstrom H, Vihko R. Hepatic impairment during simultaneous administration of medroxyprogesterone acetate and tamoxifen in the treatment of endometrial and ovarian carcinoma. Anticancer Res 1984;4:109-112.