Hepatobiliary elimination of cationic drugs: The role of P- glycoproteins and other ATP-dependent transporters

Advanced Drug Delivery Reviews

Volumn 25, Issue 2-3, 1997, Pages 159-200

  Meijer, D K F ^a   Smit, J W ^a,c   Muller M ^b  

^a UNIVERSITY OF GRONINGEN   (Netherlands)

^b UNIVERSITY MEDICAL CENTER GRONINGEN   (Netherlands)

^c Antonius Deusinglaan 1   (Netherlands)

Author keywords

[No Author keywords available]

Indexed keywords

DRUG PRODUCTS; IONIC DRUGS; PHARMACOKINETICS; PROTEINS;

GLYCOPROTEINS; LIVER;

DRUG THERAPY;

ACEBUTOLOL; ANTINEOPLASTIC AGENT; CARDIAC GLYCOSIDE; DIGOXIN; DIMETHYLTUBOCURARINE CHLORIDE; DOXORUBICIN; GLYCOPROTEIN P; HEXAFLURONIUM BROMIDE; PANCURONIUM; PIPECURONIUM; PRACTOLOL; ROCURONIUM; TUBOCURARINE CHLORIDE; VECURONIUM; VINBLASTINE;

ARTICLE; BILIARY EXCRETION; DRUG ELIMINATION; DRUG METABOLISM; DRUG PROTEIN BINDING; DRUG TRANSPORT; HEPATOBILIARY SYSTEM; HUMAN; NONHUMAN; PRIORITY JOURNAL; PROTEIN ANALYSIS;

EID: 0342872090     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0169-409X(97)00498-5     Document Type: Review

References (330)

1. Chaudhary, P.M., Mechetner, E.B. and Roninson, I.B. (1992) Expression and activity of the multidrug resistance P-glycoprotein in human peripheral blood lymphocytes. Blood 80, 2735-2739.
2. Nikaido, H. and Saier, M.H., Jr. (1992) Transport proteins in bacteria: common themes in their design. Science 258, 936-942.
3. Henderson, P.J.F. (1993) The 12-transmembrane helix transporters. Curr. Opin. Cell Biol. 5, 708-721.
4. Higgins, C.F. (1992) ABC Transporters - From Microorganisms to Man. Annu. Rev. Cell Biol. 8, 67-113.
5. Hyde, S.C., Emsley, P., Hartshorn, M.J., Mimmack, M.M., Gileadi, U., Pearce, S.R., Gallagher, M.P., Gill, D.R., Hubbard, R.E. and Higgins, C.F. (1990) Structural model of ATP-binding proteins associated with cystic fibrosis, multi-drug resistance and bacterial transport. Nature 346, 362-365.
6. Marger, M.D. and Saier, M.H. (1993) A major superfamily of transmembrane facilitators that catalyse uniport, symport and antiport. Trends Biochem. Sci. 18, 13-20.
7. Sadee, W., Drubbisch, V. and Amidon, G.-L. (1995) Biology of membrane transport proteins. Pharm. Res, 12, 1823-1837.
8. Gottesman, M.M. and Pastan, I. (1993) Biochemistry of multidrug resistance mediated by the multidrug transporter. Annu. Rev. Biochem. 62, 385-427.
9. Giros, B. and Caron, M.G. (1996) Molecular characterization of the dopamine transporter. Trends Pharmacol. Sci. 14, 43-49.
10. +: uptake and toxicity in non-neuronal COS cells expressing dopamine transporter cDNA. Ann. Neurobiol. 32, 109-111.
11. + toxicity encodes a vesicular amine transporter. Cell 70, 539-551.
12. Meijer, D.K.F. and Groothuis, G.M.M. (1991) Hepatic transport of drugs and proteins. In: N. McIntyre, J.P. Benhamou, J. Bircher, M. Rizzetto and J. Rodes (Eds.), Oxford Textbook of Clinical Hepatology, Volume 1, Oxford University Press, Oxford, New York, Tokyo, pp. 40-78.
13. Meijer, D.K.F. (1989) Transport and metabolism in the hepatobiliary system. In: S.G. Schultz, J.G. Forte and B.B. Rauner (Eds.), Handbook of Physiology, Section 6, Vol. III. Oxford University Press, New York, pp. 717-758.
14. Meijer, D.K.F., Mol, W.E.M., Müller, M. and Kurz, G. (1990) Carrier-mediated transport in the hepatic distribution and elimination of drugs, with special reference to the category of organic cations. J. Pharmacokinet. Biopharm. 18, 35-70.
15. Germann, U.A., Pastan, I. and Gottesman, M.M. (1993) P-glycoproteins: mediators of multidrug resistance. Semin. Cell Biol. 4, 63-76.
16. Doige, C.A. and Ames, G.F.L. (1993) ATP-dependent transport systems in bacteria and humans: Relevance to cystic fibrosis and multidrug resistance. Annu. Rev. Microbiol. 47, 291-319.
17. Steen, H. and Meijer, D.K.F. (1991) Organic cations. In: C.-P. Siegers and J.B. Watkins, III (Eds.), Biliary Excretion of Drugs and other Chemicals, Gustav Fischer Verlag, Stuttgart, pp. 239-272.
18. Neef, C., Oosting, R. and Meijer, D.K.F. (1984) Structure -pharmacokinetics relationship of quaternary ammonium compounds. Elimination and distribution characteristics. Naunyn-Schmiedeberg's Arch. Pharmacol. 328, 103-110.
19. Neef, C. and Meijer, D.K.F. (1984) Structure-pharmacokinetics relationship of quaternary ammonium compounds. Correlation of physicochemical and pharmacokinetic parameters. Naunyn-Schmiedeberg's Arch. Pharmacol. 328, 111-118.
20. Mol, W.E.M., Rombout, F., Paanakker, J.E., Oosting, R., Scaf, A.H.J. and Meijer, D.K.F. (1992) Pharmacokinetics of steroidal muscle relaxants in isolated perfused rat liver. Biochem. Pharmacol. 44, 1453-1459.
21. Hirom, P.C., Hughes, R.D. and Millburn, P. (1974) The physicochemical factor required for the biliary excretion of organic cations and anions. Biochem. Soc. Trans. 2, 327-330.
22. Hughes, R.D., Millburn, P. and Williams, R.T. (1973) Biliary excretion of some diquaternary ammonium cations in the rat, guinea pig and rabbit. Biochem. J. 136, 979-984.
23. Hughes, R.D., Millburn, P. and Williams, R.T. (1973) Molecular weight as a factor in the excretion of mono-quaternary ammonium cations in the bile of the rat, rabbit and guinea pig. Biochem. J. 136, 967-978.
24. Groothuis, G.M.M. and Meijer, D.K.F. (1992) Hepatocyte heterogeneity in bile formation and hepatobiliary transport of drugs. Enzyme 46, 94-138.
25. Meijer, D.K.F. and Nijssen, H.M.J. (1991) Transport of drugs, proteins and drug-protein conjugates. In: F. Ballet and R.G. Thurman (Eds.), Research in Perfused Liver: Clinical and Basic Applications. INSERM/John Libbey, London, pp. 165-208.
26. Meijer, D.K.F. and Ziegler, K. (1993) Mechanisms for the hepatic clearance of oligopeptides and proteins. Implications for rate of elimination, bioavailability and cell-specific drug delivery to the liver. In: K.L. Audus and T.J. Raub (Eds.), Biological Barriers to Protein Delivery. Plenum Press, New York and London, pp. 339-408.
27. Brass, E.P. (1992) Carnitine transport. In: R. Ferrari, S. DiMauro and G. Sherwood (Eds.), L-Carnitine and its Role in Medicine: From Function to Therapy. Academic Press-Harcourt Brace Jovanovich, London, pp. 21-36.
28. Liscovitch, M. and Lavie, Y. (1991) Sphingoid bases as endogenous cationic amphiphilic "drugs". Biochem. Pharmacol. 42, 2071-2075.
29. Byers, T.L., Bitonti, A.J. and McCann, P.P. (1990) Bis-(benzyl)polyamine analogues are substrates for a mammalian cell-transport system which is distinct from the polyamine-transport system. Biochem. J. 269, 35-40.
30. Khan, N.A., Quemener, V. and Moulinoux, J.P. (1991) Polyamine membrane transport regulation. Cell Biol. Int. Rep. 15, 9-24.
31. Toninello, A., Dalla Via, L., Siliprandi, D. and Garlid, K.D. (1992) Evidence that spermine, spermidine, and putrescine are transported etectrophoretically in mitochondria by a specific polyamine uniporter. J. Biol. Chem. 267, 18393-18397.
32. Wierda, J.M.K.H., Proost, J.H., Muir, A.W. and Marshall, R.J. (1993) Design of drugs for rapid onset. Anaesth. Pharmacol. Rev. 1, 57-68.
33. Pritchard, J.B. and Miller, D.S. (1993) Mechanisms mediating renal secretion of organic anions and cations. Physiol. Rev. 73, 765-796.
34. Ullrich, K.J., Rumrich, G., David, C. and Fritzsch, G. (1993) Bisubstrates: substances that interact with renal contraluminal organic anion and organic cation transport systems. I. Amines, piperidines, piperazines, azepines, pyridines, quinolines, imidazoles, thiazoles, guanidines and hydrazines. Pflug.-Arch. Eur. J. Physiol. 425, 280-299.
35. Ullrich, K.J. and Rumrich, G. (1993) Renal transport mechanisms for xenobiotics: chemicals and drugs. Clin. Invest. 71, 843-848.
36. Braakman, I. Hepatocyte heterogeneity in organic cation transport. Thesis, University of Groningen, 1988.
37. Van der Sluijs, P. and Meijer, D.K.F. (1985) Binding of drugs with a quaternary ammonium group to alpha-1 acid glycoprotein and asialo alpha-1 acid glycoprotein. J. Pharmacol. Exp. Ther. 234, 703-707.
38. Neef, C., Keulemans, K.T.P. and Meijer, D.K.F. (1984) Hepatic uptake and biliary excretion of organic cations. I. Characterization of three new model compounds. Biochem. Pharmacol. 33, 3977-3990.
39. Braakman, I., Verest, O., Pijning, T., Meijer, D.K.F. and Groothuis, G.M.M. (1990) Zonal distribution of the cation lucigenin in rat liver: influence of taurocholate. Mol. Pharmacol. 36, 532-536.
40. Braakman, I., Verest, O., Pijning, T., Meijer, D.K.F. and Groothuis, G.M.M. (1988) Zonal and intracellular distribution of the organic cation lucigenin: influence of taurocholate. Hepatology 8, 1386 (Abstract no. 670).
41. Feitsma, K.G., Drenth, B.F.H., De Zeeuw, R.A., Oosting, R. and Meijer, D.K.F. (1989) Unequal disposition of enantiomers of the organic cation oxyphenonium in the rat isolated perfused liver. J. Pharm. Pharmacol. 41, 27-31.
42. Lanting, A.B.L., Ensing, K., Drenth, B.F.H., Meijer, D.K.F. and De Zeeuw, R.A. (1997) Stereochemical factors in the hepatic transport and metabolism of the organic cations N-methyl dextrorphan and N-methyl levorphanol in the isolated perfused rat liver. Thesis, University of Groningen, The Netherlands.
43. Hedman, A. and Meijer, D.K.F., unpublished data.
44. Okudaira, K., Sawada, Y., Sugiyama, Y., Iga, T. and Hanano, M. (1988) Effects of basic drugs on the hepatic transport of cardiac glycosides in rats. Biochem. Pharmacol. 37, 2949-2955.
45. Okudaira, K., Yachi, K., Sawada, Y., Sugiyama, Y., Iga, T. and Hanano, M. (1992) Effect of basic drugs on the hepatic uptake of ouabain by sinusoidal plasma membrane vesicles isolated from rat liver. Biopharm. Drug Dispos. 13, 295-304.
46. Gründemann, D., Gorboulev, V., Gambaryan, S., Veyhl, M. and Koepsell, H. (1994) Drug excretion mediated by a new prototype of polyspecific transporter. Nature 372, 549-552.
47. Busch, A.E., Quester, S., Ulzheimer, J., Waldegger, S., Gorboulev, V., Lang, F. and Koepsell, H. (1996) Electrogenic properties and substrate specificity of the polyspecific rat cation transporter OCT1. J. Biol. Chem. 271, 32599-32604.
48. Hedman, A., Angelin, B., Arvidsson, A., Dahlqvist, R. and Nilsson, B. (1990) Interactions in the renal and biliary elimination of digoxin: Stereoselective difference between quinine and quinidine. Clin. Pharmacol. Ther. 47, 20-26.
49. Wandell, M., Powell, J.R., Hager, W.D., Fenster, P.E., Graves, P.E., Conrad, K.A. and Goldman, S. (1980) Effect of quinine on digoxin kinetics. Clin. Pharmacol. Ther. 28, 425-430.
50. Le Corre, P., Malledant, Y., Chevanne, F., Sado, P. and Le Verge, R. (1992) Stereoselective biliary elimination of disopyramide and mono-N-desisopropyldisopyramide in humans. Chirality 4, 80-83.
51. Agoston, S., Vermeer, G.A., Kersten, U.W. and Meijer, D.K.F. (1973) The fate of pancuronium bromide in man. Acta Anaesthesiol. Scand. 17, 267-275.
52. Meijer, D.K.F., Vermeer, G.A. and Kwant, G. (1971) The excretion of hexafluorenium in man and rat. Eur. J. Pharmacol. 14, 280-285.
53. Meijer, D.K.F., Weitering, J.G., Vermeer, G.A. and Scaf, A.H.J. (1979) Comparative pharmacokinetics of d-tubocurarine and metocurine in man. Anesthesiology 51, 402-407.
54. Nakamura, H., Sano, H., Yamazaki, M. and Sugiyama, Y. (1994) Carrier-mediated active transport of histamine H2-receptor antagonists, cimetidine and nizatidine, into isolated rat hepatocytes: contribution of type I system. J. Pharmacol. Exp. Ther. 269, 1220-1227.
55. 1-methylnicotinamide by organic cation-proton exchange in rat liver membrane vesicles. Am. J. Physiol. 259, G973-G982.
56. Moseley, R.H., Jarose, S.M. and Permoad, P. (1992) Organic cation transport by rat liver plasma membrane vesicles: Studies with tetraethylammonium. Am. J. Physiol. 263, G775-G785.
57. McKinney, T.D. and Hosford, M.A. (1992) Organic cation transport by rat hepatocyte basolateral membrane vesicles. Am. J. Physiol. 263, G939-G946.
58. Moseley, R.H., Vashi, P.G., Jarose, S.M., Dickinson, C.J. and Permoad, P.A. (1992) Thiamine transport by basolateral rat liver plasma membrane vesicles. Gastroenterology 103, 1056-1065.
59. Mol, W.E.M., Müller, M., Kurz, G. and Meijer, D.K.F. (1992) Investigations on the hepatic uptake systems for organic cations with a photoaffinity probe of procainamide ethobromide. Biochem. Pharmacol. 43, 2217-2226.
60. Mol, W.E.M. (1988) Transport mechanisms for cationic drugs in the hepato-biliary system. A pharmacokinetic and cell biological study. Thesis, University of Groningen, The Netherlands.
61. Braakman, I., Groothuis, G.M.M. and Meijer, D.K.F. (1987) Acinar redistribution and heterogeneity in transport of the organic cation rhodamine B in rat liver. Hepatology 7, 849-855.
62. Braakman, I., Groothuis, G.M.M. and Meijer, D.K.F. (1989) Zonal compartmentation of perfused rat liver: plasma reappearance of rhodamine B explained. J. Pharmacol. Exp. Ther. 249, 869-873.
63. Van der Sluijs, P., Spanjer, H.H. and Meijer, D.K.F. (1987) Hepatic disposition of cationic drugs bound to asialo-orosomucoid: lack of co-endocytosis and evidence for intrahepatic dissociation.J. Pharmacol. Exp. Ther. 240, 668-673.
64. Braakman, I., Pijning, T., Verest, O., Weert, B., Meijer, D.K.F. and Groothuis, G.M.M. (1989) Vesicular uptake system for the cation lucigenin in the rat hepatocyte.Mol. Pharmacol. 36, 537-542.
65. Tulkens, P.M. (1991) Intracellular distribution and activity of antibiotics. Eur. J. Clin. Microbiol. 10, 100-106.
66. Yoshioka, K. and Nishimura, H. (1988) Choline accumulation in isolated rat hepatocytes. Experientia 44, 889-892.
67. Yoshioka, K., Nishimura, H., Himukai, M. and Iwashima, A. (1985) The inhibitory effect of choline and other quaternary ammonium compounds on thiamine transport in isolated rat hepatocytes. Biochim. Biophys. Acta 815, 499-504.
68. Lumeng, L., Edmondson, J.W., Schenker, S. and Li, T.-K. (1979) Transport and metabolism of thiamine in isolated rat hepatocytes. J. Biol. Chem. 254, 7265-7268.
69. Chen, C.P. (1978) Active transport of thiamine by freshly isolated rat hepatocytes. J. Nutr. Sci. Vitaminol. 24, 351-362.
70. Yoshioka, K. (1984) Some properties of the thiamine uptake system in isolated rat hepatocytes. Biochim. Biophys. Acta 778, 201-209.
71. Yoshioka, K., Nishimura, H. and Hasegawa, T. (1985) Effect of a phenyl group in quaternary ammonium compounds on thiamine uptake in isolated rat hepatocytes. Biochim. Biophys. Acta 819, 263-266.
72. Yoshioka, K. and Nishimura, H. (1986) Effect of lipophilic cations on thiamine transport system in isolated rat hepatocytes. Experientia 42, 1022-1023.
73. Yoshioka, K., Nishimura, H. and Iwashima, A. (1983) Active transport of dimethalium in isolated rat hepatocytes. Biochim. Biophys. Acta 732, 308-311.
74. Indiveri, .C., Palmieri, L. and Palmieri, F. (1994) Kinetic characterization of the reconstituted ornithine carrier from rat liver mitochondria. Biochim. Biophys. Acta 1188, 293-301.
75. King, P.D. and Cai, Z.-S. (1993) Uptake of tributylmethylammonium into rat liver basolateral plasma membrane vesicles is mediated by proton exchange. Gastroenterology 104, A927
76. Van Dyke, R.W., Faber, E.D. and Meijer, D.K.F. (1992) Sequestration of organic cations by acidified hepatic endocytic vesicles and implications for biliary excretion. J. Pharmacol. Exp. Ther. 261, 1-11.
77. Steen, H. and Meijer, D.K.F. (1991) Mechanisms for uptake of the organic cation tri-n-butylmethylammonium in the hepatocyte. J. Pharmacol. Exp. Ther. 258, 537-543.
78. Streich, S., Bruss, M. and Bonisch, H. (1996) Expression of the extraneuronal monoamine transporter (uptake 2) in human glioma cells. Naunyn-Schmiedeberg's Arch. Pharmacol. 353, 328-333.
79. +), is a substrate for the canalicular organic cation:H+ exchanger. Digestive Disease Week, pp. A-28 (no 109). (Abstract)
80. Moseley, R.H., Smit, H., Van Solkema, B.G.H., Wang, W. and Meijer, D.K.F. (1996) Mechanisms for the hepatic uptake and biliary excretion of tributylmethylammonium: studies with rat liver plasma membrane vesicles. J. Pharmacol. Exp. Ther. 276, 561-567.
81. Steen, H., Oosting, R. and Meijer, D.K.F. (1991) Mechanisms for the uptake of cationic drugs by the liver: A study with tributylmethylammonium (TBuMA). J. Pharmacol. Exp. Ther. 258, 537-543.
82. Mol, W.E.M., Fokkema, G.N., Weert, B. and Meijer, D.K.F. (1988) Mechanisms for the hepatic uptake of organic cations. Studies with the muscle relaxant vecuronium in isolated rat hepatocytes. J. Pharmacol. Exp. Ther. 244, 268-275.
83. Müller, M. (1988) Membrantransport von organischen kationen in hepatocyten. Ein beitrag zur aufklärung von hepatischen transportvorgängen. Dissertation, Universität von Freiburg, 1988.
84. Bossuyt, X., Müller, M., Hagenbuch, B. and Meier, P.J. (1996) Polyspecific steroid and drug clearance by an organic anion transporter of mammalian liver. J. Pharmacol. Exp. Ther. 276, 891-896.
85. Steen, H., Merema, M. and Meijer, D.K.F. (1992) A multispecific uptake system for taurocholate, cardiac glycosides and cationic drugs in the liver. Biochem. Pharmacol. 44, 2323-2331.
86. Okudaira, K., Yamazaki, M., Sawada, Y., Sugiyama, Y., Iga, T. and Hanano, M. (1992) Correlation between the inhibitory effects of basic drugs on the uptake of cardiac glycosides and taurocholate by isolated rat hepatocytes. Pharm. Res. 9, 1152-1156.
87. Steen, H., Maring, J.G. and Meijer, D.K.F. (1993) Differential effects of metabolic inhibitors on cellular and mitochondrial uptake of organic cations in rat liver. Biochem. Pharmacol. 45, 809-818.
88. Mol, W.E.M. and Meijer, D.K.F. (1990) Hepatic transport mechanisms for bivalent organic cations. Subcellular distribution and hepato-biliary concentration gradients of some steroidal muscle relaxants. Biochem. Pharmacol. 39, 383-390.
89. Meijer, D.K.F. (1976) The mechanisms for hepatic uptake and biliary excretion of organic cations. In: M. Kramer and F. Lauterbach (Eds.), Intestinal Permeation. Excerptia Medica, Amsterdam, pp. 196-207.
90. Meijer, D.K.F., Wester, J. and Gunnik, M. (1972) Distribution of quaternary ammonium compounds between particulate and soluble constituents of rat liver in relation to their transport from plasma into bile. Naunyn-Schmiedeberg's Arch. Pharmacol. 273, 179-192.
91. Moseley, R.H. and Van Dyke, R.W. (1995) Organic cation transport by rat liver lysosomes. Am. J. Physiol. Gastrointest. Liver Physiol. 31, G480-G486.
92. Stern-Bach, Y., Keen, J.N., Bejerano, M., Steiner-Mordoch, S., Wallach, M., Findlay, J.B.C. and Schuldiner, S. (1992) Homology of a vesicular amine transporter to a gene conferring resistance to 1-methyl-4-phenylpyridinium, Proc. Natl. Acad. Sci. U.S.A. 89, 9730-9733.
93. Meijer, D.K.F., Weitering, J.G. and Vonk, R.J. (1976) Hepatic uptake and biliary excretion of d-tubocurarine and trimethylcurarine in the rat in vivo and in isolated perfused rat livers. J. Pharmacol. Exp. Ther. 198, 229-239.
94. Weitering, J.G., Lammers, W., Meijer, D.K.F. and Mulder, G.J. (1977) Localization of d-tubocurarine in rat liver lysosomes. Lysosomal uptake, biliary excretion and displacement by quinacrine in vivo. Naunyn-Schmiedeberg's Arch. Pharmacol. 299, 277-281.
95. Weitering, J.G., Mulder, G.J., Meijer, D.K.F., Lammers, W., Veenhuis, M. and Wendelaar Bonga, S.E. (1975) On the localization of d-tubocurarine in rat liver lysosomes in vivo by electron microscopy and subcellular fractionation. Naunyn-Schmiedeberg's Arch. Pharmacol. 289, 251-256.
96. MacIntyre, A.C. and Cutler, D.J. (1988) Role of lysosomes in hepatic accumulation of chloroquine. J. Pharm. Sci. 77, 196-199.
97. Ward, S.A. (1988) Mechanisms of chloroquine resistance in malarial chemotherapy. Trends Pharmacol. Sci. 9, 241-246.
98. Smit, H., Duin, E., Steen, H., Roggeveld, J., Oosting, R. and Meijer, D.K.F. (1995) Multiple carriers involved in the biliary excretion of cationic drugs, Hepatology 22, 309A (Abstract).
99. Steen, H., (1992) Mitochondrial uptake and accumulation of organic cationic drugs. Thesis, University of Groningen, The Netherlands.
100. Steen, H. (1992) Mechanisms for the hepatic disposition of cationic drugs. Molecular aspects of membrane transport in the hepatocyte, Thesis, University of Groningen.
101. Woolley, G.A., Kapral, M.K. and Deber, C.M. (1987) Potential-sensitive membrane association of a fluorescent dye. FEBS Lett. 224, 337-342.
102. Rottenberg, H. (1989) Proton electrochemical potential gradient in vesicles, organelles, and prokaryotic cells. Methods Enzymol. 172, 63-84.
103. Bunting, J.R., Phan, T.V., Kamali, E. and Dowben, R.M. (1989) Fluorescent cationic probes of mitochondria. Metrics and mechanism of interaction, Biophys. J. 56, 979-993.
104. +. Biochem. Biophys. Res. Commun. 134, 743-748.
105. Ramsay, R.R. and Singer, T.P. (1986) Energy-dependent uptake of N-methyl-4-phenylpyridinium, the neurotoxic metabolite of 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine, by mitochondria. J. Biol. Chem. 261, 7585-7587.
106. Gluck, M.R., Youngster, S.K., Ramsay, R.R., Singer, T.P. and Nicklas, W.J. (1994) Studies on the characterization of the inhibitory mechanism of 4′-alkylated 1-methyl-4-phenylpyridinium and phenylpyridine analogues in mitochondria and electron transport particles. J. Neurochem. 63, 655-661.
107. Singh, G., Sharkey, S.M. and Moorehead, R. (1992) Mitochondrial DNA damage by anticancer agents. Pharmacol. Ther. 54, 217-230.
108. Diwan, J.J., Yune, H.H., Bawa, R., Haley, T. and Mannella, C.A. (1988) Enhanced uptake of spermidine and methylglyoxal-bis(guanylhydrazone) by rat liver mitochondria following outer membrane lysis. Biochem. Pharmacol. 37, 957-961.
109. Berman, J.J. (1988) Ethidium bromide resistance in a rat liver epithelial cell line: association with enhanced drug efflux. Cell Biol. Toxicol. 4, 325-332.
110. Porter, R.K., Scott, J.M. and Brand, M.D. (1992) Choline transport into rat liver mitochondria. Characterization and kinetics of a specific transporter. J. Biol. Chem. 267, 14637-14646.
111. Buscher, H.-P., Fricker, G., Gerok, W., Kramer, W., Kurz, G., Müller, M. and Schneider, S. (1986) Membrane transport of amphiphilic compounds by hepatocytes. In: H. Greten, E. Windler and U. Beisiegel (Eds.), Receptor-mediated Uptake in the Liver, Springer Verlag, Berlin, Heidelberg, pp. 189-199.
112. Koch, J.K. and Gallagher, C.H. (1960) The effect of neuromuscular blocking agents on mitochondria. I. Effects of d-tubocurarine and of complex ions on mitochondrial enzyme systems. Biochem. Pharmacol. 3, 231-243.
113. 3 exchange in canalicular rat liver plasma membrane vesicles. J. Clin. Invest. 75, 1256-1263.
114. Mannella, C.A. and Wang, Q. (1989) Permeability of the mitochondrial outer membrane to organic cations. Biochim. Biophys. Acta 981, 363-366.
115. Zimmermann, H.W. (1986) Physicochemical and cytochemical investigations on the binding of ethidium and acridine dyes to DNA and to organelles in living cells. Angew. Chem., Int. Ed. Engl. 25, 115-130.
116. Yeh, C.G., Hsi, B. and Faulk, W.P. (1981) Propidium iodide as a nuclear marker in immunofluorescence. II. Use with cellular identification and viability studies. J. Immunol. 43, 269-275.
117. Ronot, X., Benel, L., Adolphe, M. and Mounolou, J.C. (1986) Mitochondrial analysis in living cells: The use of rhodamine 123 and flow cytometry. Biol. Cell 57, 1-8.
118. Csermely, P., Schnaider, T. and Szántó, I. (1995) Signalling and transport through the nuclear membrane. Biochim. Biophys. Acta 1241, 425-452.
119. 4-acetylprocainamide ethobromide. Naunyn-Schmiedeberg's Arch. Pharmacol. 302, 1-9.
120. Ruifrok, P.G. (1982) Uptake of quaternary ammonium compounds into rat liver plasma membrane vesicles. Biochem. Pharmacol. 31, 1431-1435.
121. Neef, C., Keulemans, K.T.P. and Meijer, D.K.F. (1984) Hepatic uptake and biliary excretion of organic cations. II. The influence of ion pair formation. Biochem. Pharmacol. 33, 3991-4002.
122. Kamimoto, Y., Gatmaitan, Z., Hsu, J. and Arias, I.M. (1989) The function of Gp170, the multidrug resistance gene product, in rat liver canalicular membrane vesicles. J. Biol. Chem. 264, 11693-11698.
123. Ziegler, K., Kolac, C. and Ising, W. (1994) ATP-dependent transport of the linear renin-inhibiting peptide EMD 51921 by canalicular plasma membrane vesicles of rat liver: Evidence of drug-stimulatable ATP-hydrolysis. Biochim. Biophys. Acta 1196, 209-217.
124. Sinicrope, F.A., Dudeja, P.K., Bissonnette, B.M., Safa, A.R. and Brasitus, T.A. (1992) Modulation of P-glycoprotein-mediated drug transport by alterations in lipid fluidity of rat liver canalicular membrane vesicles. J. Biol. Chem. 267, 24995-25002.
125. Ballet, F., Vrignaud, P., Robert, J., Rey, C. and Poupon, R. (1987) Hepatic extraction, metabolism and biliary excretion of doxorubicin in the isolated perfused rat liver. Cancer Chemother. Pharmacol. 19, 240-245.
126. Smit, J.W., Steen, H. and Meijer, D.K.F. (1994) Modulators of protein kinase C as well as MDR reversal agents have a major influence on the biliary excretion of the cationic drugs tri-N-butylmethyl-ammonium (TBuMA) and doxorubicin. In: D. Keppler and K. Jungermann (Eds.), Transport in the Liver. Falk Symposium No. 74, Heidelberg, Abstract no. 27.
127. Speeg, K.V. and Maldonado, A.L. (1993) Effect of cyclosporine on colchicine partitioning in the rat liver. Cancer Chemother. Pharmacol. 32, 434-436.
128. Speeg, K.V., Maldonado, A.L., Liaci, J. and Muirhead, D. (1992) Effect of cyclosporine on colchicine secretion by a liver canalicular transporter studied in vivo. Hepatology 15, 899-903.
129. Thalhammer, T., Stapf, V., Gajdzik, L. and Graf, J. (1994) Bile canalicular cationic dye secretion as a model for P-glycoprotein mediated transport. Eur. J. Pharmacol. 270, 213-220.
130. Watanabe, T., Miyauchi, S., Sawada, Y., Iga, T., Hanano, M., Inaba, M. and Sugiyama, Y. (1992) Kinetic analysis of hepatobiliary transport of vincristine in perfused rat liver. Possible roles of P-glycoprotein in biliary excretion of vincristine. J. Hepatol. 16, 77-88.
131. Zamora, J.M., Pearce, H.L. and Beck, W.T. (1988) Physical-chemical properties shared by compounds that modulate multidrug resistance in human leukemic cells. Mol. Pharmacol. 33, 454-462.
132. Buschman, E., Arceci, R.J., Croop, J.M., Che, M.X., Arias, I.M., Housman, D.E. and Gros, P. (1992) mdr2 Encodes P-glycoprotein expressed in the bile canaucular membrane as determined by isoform-specific antibodies. J. Biol. Chem. 267, 18093-18099.
133. Thiebaut, F., Tsuruo, T., Hamada, H., Gottesman, M.M., Pastan, I. and Willingham, M.C. (1987) Cellular localization of the multidrug-resistance gene product P-glycoprotein in normal human tissues. Proc. Natl. Acad. Sci. U.S.A. 84, 7735-7738.
134. Bradley, G., Georges, E. and Ling, V. (1990) Sex dependent and independent expression of the P-glycoprotein isoforms in Chinese hamster. J. Cell. Physiol. 145, 398-408.
135. Fojo, A.T., Ueda, K., Slamon, D.J., Poplack, D.G., Gottesman, M.M. and Pastan, I. (1987) Expression of a multidrug-resistance gene in human tumors and tissues. Proc. Natl. Acad. Sci. U.S.A. 84, 265-269.
136. Smit, J.J.M., Schinkel, A.M., Oude Elferink, R.P.J., Groen, A.K., Wagenaar, E., Van Deemter, L., Mol, C.A.A.M., Ottenhoff, R., Van der Lugt, N.M.T., van Roon, M.A., Van der Valk, M.A., Offerhaus, G.J.A., Berns, A.J.M. and Borst, P. (1993) Homozygous disruption of the murine mdr2 P-glycoprotein gene leads to a complete absence of phospholipid from bile and to liver disease. Cell 75, 451-462.
137. Roninson, I.B. (1992) The role of the MDR1 (P-glycoprotein) gene in multidrug resistance in vitro and in vivo. Biochem. Pharmacol. 43, 95-102.
138. Schinkel, A.H. and Borst, P. (1991) Multidrug resistance mediated by P-glycoproteins. Semin. Cancer Biol. 2, 213-226.
139. Borst, P. (1991) Genetic mechanisms of drug resistance. A review. Acta Oncol. 30, 87-105.
140. Chen, C.J., Chin, J.E., Ueda, K., Clark, D.P., Pastan, I., Gottesman, M.M. and Robinson, I.B. (1986) Internal duplication and homology with bacterial transport proteins in the mdr1 (P-glycoprotein) gene from multidrug-resistant human cells. Cell 47, 381-389.
141. Kast, C., Canfield, V., Levenson, R. and Gros, P. (1995) Membrane topology of P-glycoprotein as determined by epitope insertion: transmembrane organization of the N-terminal domain of mdr3. Biochemistry 34, 4402-4411.
142. Loo, T.W. and Clarke, D.M. (1994) Mutations to amino acids located in predicted transmembrane segment 6 (TM6) modulate the activity and substrate specificity of human P-glycoyrotein. Biochemistry 33, 14049-14057.
143. Zhang, X.P., Collins, K.I. and Greenberger, L.M. (1995) Functional evidence that transmembrane 12 and the loop between transmembrane 11 and 12 form part of the drug-binding domain in P-glycoprotein encoded by MDR1. J. Biol. Chem. 270, 5441-5448.
144. Loo, T.W. and Clarke, D.M. (1995) Membrane topology of a cysteine-less mutant of human P-glycoprotein. J. Biol. Chem. 270, 843-848.
145. Zhang, J.-T., Lee, C.H., Duthie, M. and Ling, V. (1995) Topological determinants of internal transmembrane segments in P-glycoprotein sequences. J. Biol. Chem. 270, 1742-1746.
146. Beja, O. and Bibi, E. (1995) Multidrug resistance protein (Mdr)-alkaline phosphatase hybrids in Escherichia coli suggest a major revision in the topology of the C-terminal half of Mdr. J. Biol. Chem. 270, 12351-12354.
147. Zhang, J.-T. and Ling, V. (1995) Involvement of cytoplasmic factors regulating the membrane orientation of P-glycoprotein sequences. Biochemistry 9159-9165.
148. Poruchynsky, M.S. and Ling, V. (1994) Detection of oligomeric and monomeric forms of P-glycoprotein in multidrug resistant cells. [published erratum appears in Biochemistry (1994) 33, 9032], Biochemistry 33, 4163-4174.
149. Teeter, L.D., Estes, M., Chan, J.Y., Atassi, H., Sell, S., Becker, F.F. and Kuo, M.T. (1993) Activation of distinct multidrug-resistance (P-glycoprotein) genes during rat liver regeneration and hepatocarcinogenesis. Mol. Carcinog. 8, 67-73.
150. Schrenk, D., Gant, T.W., Preisegger, K.-H., Silverman, J.A., Marino, P.A. and Thorgeirsson, S.S. (1993) Induction of multidrug resistance gene expression during cholestasis in rats and nonhuman primates. Hepatology 17, 854-860.
151. Nakatsukasa, H., Silverman, J.A., Gant, T.W., Evarts, R.P. and Thorgeirsson, S.S. (1993) Expression of multidrug resistance genes in rat liver during regeneration and after carbon tetrachloride intoxication. Hepatology 18, 1202-1207.
152. Kuo, M.T. (1993) Expression of multidrug-resistance (P-glycoprotein) genes in liver cancers: A molecular example of the convergence theory of hepatocarcinogenesis? Mol. Carcinog. 7, 73-75.
153. Chenivesse, X., Franco, D. and Bréchot, C. (1993) MDR1 (multidrug resistance) gene expression in human primary liver cancer and cirrhosis. J. Hepatol. 18, 168-172.
154. Tang-Wai, D.F., Kajiji, S., Dicapua, F., de Graaf, D., Roninson, I.B. and Gros, P. (1995) Human (MDR1) and mouse (mdr1, mdr3) P-glycoproteins can be distinguished by their respective drug resistance profiles and sensitivity to modulators. Biochemistry 34, 32-39.
155. Berr, F., Meier, P.J. and Stieger, B. (1993) Evidence for the presence of a phosphatidylcholine translocator in isolated rat liver canalicular plasma membrane vesicles. J. Biol. Chem. 268, 3976-3979.
156. Ruetz, S. and Gros, P. (1994) Phosphatidylcholine translocase: A physiological role for the mdr2 gene. Cell 77, 1071-1081.
157. Oude Elferink, R.P.J. and Groen, A.K. (1995) The role of mdr2 P-glycoprotein in biliary lipid secretion. Cross-talk between cancer research and biliary physiology. J. Hepatol. 23, 617-625.
158. Deleuze, J.F., Jacquemin, E., Dubuisson, C., Cresteil, D., Dumont, M., Erlinger, S., Bernard, O. and Hadchouel, M. (1996) Defect of multidrug-resistance 3 gene expression in a subtype of progressive familial intrahepatic cholestasis. Hepatology 23, 904-908.
159. Ruetz, S. and Gros, P. (1995) Enhancement of Mdr2-mediated phosphatidylcholine translocation by the bile salt taurocholate - Implications for hepatic bile formation. J. Biol. Chem. 270, 25388-25395.
160. Beukeveld, G.J.J., In't Veld, G., Havinga, R., Groen, A.K., Wolthers, B.G. and Kuipers, F. (1996) Relationship between biliary lipid and protoporphyrin secretion; potential role of mdr 2 P-glycoprotein in hepatobiliary organic anion transport. J. Hepatol. 24, 343-352.
161. Chianale, J., Vollrath, V., Wielandt, A.M., Amigo, L., Rigotto, A., Nervi, F., Gonzalez, S., Andrade, L., Pizarro, M. and Accatino, L. (1996) Fibrates induce mdr2 gene expression and biliary phospholipid secretion in the mouse. Biochem. J. 314, 781-786.
162. Gupta, S. and Gollapudi, S. (1993) P-Glycoprotein (MDR 1 gene product) in cells of the immune system: Its possible physiologic role and alteration in aging and human immunodeficiency virus-1 (HIV-1) infection. J. Clin. Immunol. 13, 289-301.
163. Metherall, J.E., Li, H. and Waugh, K. (1996) Role of multidrug resistance P-glycoprotein in cholesterol biosynthesis. J. Biol. Chem. 271, 2634-2640.
164. Pinedo, H.M. and Giaccone, G. (1995) P-glycoprotein - a marker of cancer-cell behavior (editorial; comment). N. Engl. J. Med. 333, 1417-1419.
165. Endicott, J.A. and Ling, V. (1989) The biochemistry of P-glycoprotein-mediated multidrug resistance. Annu. Rev. Biochem. 58, 137-171.
166. Ambudkar, S.V., Lelong, I.H., Zhang, J.P., Cardarelli, C.O., Gottesman, M.M. and Pastan, I. (1992) Partial purification and reconstitution of the human multidrug-resistance pump: Characterization of the drug-stimulatable ATP hydrolysis. Proc. Natl. Acad. Sci. U.S.A. 89, 8472-8476.
167. Sharom, F.J., Yu, X.H. and Doige, C.A. (1993) Functional reconstitution of drug transport and ATPase activity in proteoliposomes containing partially purified P-glycoprotein. J. Biol. Chem. 268, 24197-24202.
168. Garrigos, M., Belehradek, J., Jr., Mir, L.M. and Orlowski, S. (1993) Absence of cooperativity for MgATP and verapamil effects on the ATPase activity of P-glycoprotein containing membrane vesicles. Biochem. Biophys. Res. Commun. 196, 1034-1041.
169. Scarborough, G.A. (1995) Drug-stimulated ATPase activity of the human P-glycoprotein. J. Bioenerg. Biomembr. 27, 37-41.
170. 3H]vinblastine from Chinese hamster ovary cells transfected with a full-length complementary DNA clone for the mdr1 gene. Cancer Res. 49, 3867-3871.
171. Gros, P., Croop, J. and Housman, D. (1986) Mammalian multidrug resistance gene: Complete cDNA sequence indicates strong homology to bacterial transport proteins. Cell 47, 371-380.
172. Ueda, K., Cardarelli, C.O., Gottesman, M.M. and Pastan, I. (1987) Expression of a full-length cDNA for the human "MDR1" gene confers resistance to colchicine, doxorubicin, and vinblastine. Proc. Natl. Acad. Sci. U.S.A. 84, 3004-3008.
173. Boer, R., Dichtl, M., Borchers, C., Ulrich, W.R., Marecek, J.F., Prestwich, G.D., Glossmann, H. and Striessnig, J. (1996) Reversible binding of a chemosensitizer binding domain of p-glycoprotein with a novel 1,4-dihydropyridine drug transport inhibitor. Biochemistry 35, 1387-1396.
174. Boer, R., Ulrich, W.R., Haas, S., Borchers, C., Gekeler, V., Boss, H., Przybylski, M. and Schodl, A. (1996) Interaction of cytostatics and chemosensitizers with the dexniguldipine binding site on P-glycoprotein. Eur. J. Pharmacol. 295, 253-260.
175. Nare, B., Prichard, R.K. and Georges, E. (1994) Characterization of rhodamine 123 binding to P-glycbprotein in human multidrug-resistant cells. Mol. Pharmacol. 45, 1145-1152.
176. Borchers, C., Ulrich, W.R., Klemm, K., Ise, W., Gekeler, V., Haas, S., Schodl, A., Conrad, J., Przybylski, M. and Boer, R. (1995) B9209-005, an azido derivative of the chemosensitizer dexniguldipine-HCl, photolabels P-glycoprotein. Mol. Pharmacol. 48, 21-29.
177. Orr, G.A., Han, E.K., Browne, P.C., Nieves, E., O'Connor, B.M., Yang, C.P. and Horwitz, S.B. (1993) Identification of the major phosphorylation domain of murine mdr1b P-glycoprotein. Analysis of the protein kinase A and protein kinase C phosphorylation sites. J. Biol. Chem. 268, 25054-25062.
178. Müller, M., Bakos, E., Welker, E., Varadi, A., Germann, U.A., Gottesman, M.M., Morse, B.S., Roninson, I.B. and Sarkadi, B. (1996) Altered drug-stimulated ATPase activity in mutants of the human multidrug resistance protein. J. Biol. Chem. 271, 1877-1883.
179. Loo, T.W. and Clarke, D.M. (1995) Covalent modification of human P-glycoprotein mutants containing a single cysteine in either nucleotide-binding fold abolishes drug-stimulated ATPase activity. J. Biol. Chem. 270, 22957-22961.
180. Urbatsch, I.L., Sankaran, B., Weber, J. and Senior, A.E. (1995) P-glycoprotein is stably inhibited by vanadate-induced trapping of nucleotide at a single catalytic site. J. Biol. Chem. 270, 19383-19390.
181. Senior, A.E., Alshawi, M.K. and Urbatsch, I.L. (1995) The catalytic cycle of P-glycoprotein. FEBS Lett. 377, 285-289.
182. Gill, D.R., Hyde, S.C., Higgins, C.F., Valverde, M.A., Mintenig, G.M. and Sepúlveda, F.V. (1992) Separation of drug transport and chloride channel functions of the human multidrug resistance P-glycoprotein. Cell 71, 23-32.
183. Abraham, E.H., Prat, A.G., Gerweck, L., Seneveratne, T., Arceci, R.J., Kramer, R., Guidotti, G. and Cantiello, H.F. (1993) The multidrug resistance (mdr1) gene product functions as an ATP channel. Proc. Natl. Acad. Sci. U.S.A. 90, 312-316.
184. Al-Awqati, Q. (1995) Regulation of ion channels by ABC transporters that secrete ATP. Science 269, 805-806.
185. i homeostasis in multidrug-resistant (MDR) cells: Further characterization of a series of MDR cell lines expressing different levels of P-glycoprotein. Biochemistry 32, 11042-11056.
186. Boscoboinik, D., Gupta, R.S. and Epand, R.M. (1990) Investigation of the relationship between altered intracellular pH and multidrug resistance in mammalian cells. Br. J. Cancer 61, 568-572.
187. Keizer, H.G. and Joenje, H. (1989) Increased cytosolic pH in multidrug-resistant human lung tumor cells: effect of verapamil. J. Natl. Cancer Inst. 83, 706-709.
188. Thiebaut, F., Currier, S.J., Whitaker, J., Haugland, R.P., Gottesman, M.M., Pastan, I. and Willingham, M.C. (1990) Activity of the multidrug transporter results in alkalinization of the cytosol: measurement of cytosolic pH by microinjection of a pH-sensitive dye. J. Histochem. Cytochem. 38, 685-690.
189. Speeg, K.V., Jr., DeLeon, C. and McGuire, W.L. (1992) Uptake of the noncytotoxic transport probe procainamide in the Chinese hamster ovary model of multidrug resistance. Cancer Res. 52, 3539-3546.
190. Skovsgaard, T. (1989) Drug transport in multidrug-resistant tumor cells. A revision of the pump-hypothesis. In: H. Tapiero, J. Robert and T.J. Lampidis (Eds.), Anticancer Drugs. Colloque INSERM/John Libbey Eurotext, London, pp. 233-244.
191. De Greef, C., van der Heyden, S., Viana, F., Eggermont, J., De Bruijn, E.A., Raeymaekers, L., Droogmans, G. and Nilius, B. (1995) Lack of correlation between mdr-1 expression and volume-activation of chloride-currents in rat colon cancer cells. Pflug.-Arch. Eur. J. Physiol. 430, 296-298.
192. De Greef, C., Sehrer, J., Viana, F., Van Acker, K., Eggermont, J., Mertens, L., Raeymaekers, L., Droogmans, G. and Nilius, B. (1995) Volume-activated chloride currents are not correlated with P-glycoprotein expression. Biochem. J. 307, 713-718.
193. Roepe, P.D. (1995) The role of the MDR protein in altered drug translocation across tumor cell membranes. Biochim. Biophys. Acta 1241, 385-405.
194. Ghishan, F.K., Arab, N., Bulus, N., Said, H., Pietsch, J. and Abumrad, N. (1990) Glutamine transport by human intestinal basolateral membrane vesicle. Am. J. Clin. Nutr. 51, 612-616.
195. Altenberg, G.A., Young, G., Horton, J.K., Glass, D., Belli, J.A. and Reuss, L. (1993) Changes in intra- or extracellular pH do not mediate P-glycoprotein-dependent multidrug resistance. Proc. Natl. Acad. Sci. U.S.A. 90, 9735-9738.
196. Shapiro, A.B. and Ling, V. (1995) Reconstitution of drug transport by purified P-glycoprotein. J. Biol. Chem. 16167-16175.
197. Wei, L.Y., Stutts, M.J., Hoffman, M.M. and Roepe, P.D. (1995) Overexpression of the cystic fibrosis transmembrane conductance regulator in NIH 3T3 cells lowers membrane potential and intracellular pH and confers a multidrug resistance phenotype. Biophys. J. 69, 883-895.
198. Higgins, C.F. and Gottesman, M.M. (1992) Is the multidrug transporter a flippase? Trends Biochem. Sci. 17, 18-21.
199. Shalinsky, D.R., Jekunen, A.P., Alcaraz, J.E., Christen, R.D., Kim, S., Khatibi, S. and Howell, S.B. (1993) Regulation of initial vinblastine influx by P-glycoprotein. Br. J. Cancer 67, 30-36.
200. Arias, I.M. (1993) Is the multidrug resistance an ATP channel? Hepatology 18, 216-217.
201. Sippel, C.J., Suchy, F.J., Ananthanarayanan, M. and Perlmutter, D.H. (1993) The rat liver ecto-ATPase is also a canalicular bile acid transport protein. J. Biol. Chem. 268, 2083-2091.
202. Klopman, G., Srivastava, S., Kolossvary, I., Epand, R.F., Ahmed, N. and Epand, R.M. (1992) Structure-activity study and design of multidrug-resistant reversal compounds by a computer automated structure evaluation methodology. Cancer Res. 52, 4121-4129.
203. Selassie, C.D., Hansch, C. and Khwaja, T.A. (1990) Structure-activity relationships of antineoplastic agents in multidrug resistance. J. Med. Chem. 33, 1914-1919.
204. Callaghan, R. and Higgins, C.F. (1995) Interaction of tamoxifen with the multidrug resistance P-glycoprotein. Br. J. Cancer 71, 294-299.
205. de Graaf, D., Sharma, R.C., Mechetner, E.B., Schimke, R.T. and Roninson, I.B. (1996) P-glycoprotein confers methotrexate resistance in 3T6 cells with deficient carrier-mediated methotrexate uptake. Proc. Natl. Acad. Sci. U.S.A. 93, 1238-1242.
206. Zhang, L., Sachs, C.W., Fu, H.W., Fine, R.L. and Casey, P.J. (1995) Characterization of prenylcysteines that interact with P-glycoprotein and inhibit drug transport in tumor cells. J. Biol. Chem. 270, 22859-22865.
207. Goda, K., Krasznai, Z., Gaspar, R., Lankelma, J., Westerhoff, H.V., Damjanovich, S. and Szabo, G. (1996) Reversal of multidrug resistance by valinomycin is overcome by CCCP. Biochem. Biophys. Res. Commun. 219, 306-310.
208. Pereira, E., Teodori, E., Dei, S., Gualtieri, F. and Garnier-Suillerot, A. (1995) Reversal of multidrug resistance by verapamil analogues, Biochem. Pharmacol. 50, 451-457.
209. Borgnia, M.J., Eytan, G.D. and Assaraf, Y.G. (1996) Competition of hydrophobic peptides, cytotoxic drugs, and chemosensitizers on a common P-glycoprotein pharmacophore as revealed by its ATPase activity. J. Biol. Chem. 271, 3163-3171.
210. Sarkadi, B., Müller, M., Homolya, L., Hollo, Z., Seprodi, J., Germann, U.A., Gottesman, M.M., Price, E.M. and Boucher, R.C. (1994) Interaction of bioactive hydrophobic peptides with the human multidrug transporter. FASEB J. 8, 766-770.
211. Piwnica-Worms, D., Rao, W., Kronauge, J.F. and Croop, J.M. (1995) Characterization of multidrug resistance P-glycoprotein transport function with an organotechnetium cation. Biochemistry 34, 12210-12220.
212. Raymond, M., Gros, P., Whiteway, M. and Thomas, D.Y. (1992) Functional complementation of yeast ste6 by a mammalian multidrug resistance gene. Science 256, 232-239.
213. Pearce, H.L., Safa, A.R., Bach, N.J., Winter, M.A., Cirtain, M.C. and Beck, W.T. (1989) Essential features of the P-glycoprotein pharmacophore as defined by a series of reserpine analogs that modulate multidrug resistance. Proc. Natl. Acad. Sci. U.S.A. 86, 5128-5132.
214. Ford, J.M., Bruggemann, E.P., Pastan, I., Gottesman, M.M. and Hait, W.N. (1990) Cellular and biochemical characterization of thioxanthenes for reversal of multidrug resistance in human and murine cell lines. Cancer Res. 50, 1748-1756.
215. Nogae, I., Kohno, K., Kikuchi, J., Kuwano, M., Akiyama, S.I., Kiue, A., Suzuki, K.I., Yoshida, Y., Cornwell, M.M., Pastan, I. and Gottesman, M.M. (1989) Analysis of structural features of dihydropyridine analogs needed to reverse multidrug resistance and to inhibit photoaffinity labeling of P-glycoprotein. Biochem. Pharmacol. 38, 519-527.
216. Hofsli, E. and Nissen-Meyer, J. (1990) Reversal of multidrug resistance by lipophilic drugs. Cancer Res. 50, 3997-4002.
217. Dellinger, M., Pressman, B.C., Calderon-Higginson, C., Savaraj, N., Tapiero, H., Kolonias, D. and Lampidis, T.J. (1992) Structural requirements of simple organic cations for recognition by multidrug-resistant cells. Cancer Res. 52, 6385-6389.
218. Ramu, A. and Ramu, N. (1992) Reversal of multidrug resistance by phenothiazines and structurally related compounds. Cancer Chemother. Pharmacol. 30, 165-173.
219. Piwnica-Worms, D., Chiu, M.L., Budding, M., Kronauge, J.F., Kramer, R.A. and Croop, J.M. (1993) Functional imaging of multidrug-resistant P-glycoprotein with an organotechnetium complex. Cancer Res. 53, 977-984.
220. Tang-Wai, D.F., Brossi, A., Arnold, L.D. and Gros, P. (1993) The nitrogen of the acetamido group of colchicine modulates P-glycoprotein-mediated multidrug resistance. Biochemistry 32, 6470-6476.
221. Priebe, W., Van, N.T., Burke, T.G. and Perez-Soler, R. (1993) Removal of the basic center from doxorubicin partially overcomes multidrug resistance and decreases cardiotoxicity. Anti-Cancer Drugs 4, 37-48.
222. Schinkel, A.H., Wagenaar, E., Van Deemter, L., Mol, C.A.A.M. and Borst, P. (1995) Absence of the mdr1a P-glycoprotein in mice affects tissue distribution and pharmacokinetics of dexamethasone, digoxin, and cyclosporin A. J. Clin. Invest. 96, 1698-1705.
223. Schinkel, A.H., Smit, J.J.M., Vantellingen, O., Beijnen, J.H., Wagenaar, E., Vandeemter, L., Mol, C.A.A.M., Vandervalk, M.A., Robanusmaandag, E.C., Teriele, H.P.J., Berns, A.J.M. and Borst, P. (1994) Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs. Cell 77, 491-502.
224. Eytan, G.D., Regev, R., Oren, G. and Assaraf, Y.G. (1996) The role of passive transbilayer drug movement in multidrug resistance and its modulation. J. Biol. Chem. 271, 12897-12902.
225. Gruber, A., Peterson, C. and Reizenstein, P. (1988) D-verapamil and L-verapamil are equally effective in increasing vincristine accumulation in leukemic cells in vitro. Int. J. Cancer 41, 224-226.
226. Höllt, V., Kouba, M., Dietel, M. and Vogt, G. (1992) Stereoisomers of calcium antagonists which differ markedly in their potencies as calcium blockers are equally effective in modulating drug transport by P-glycoprotein. Biochem. Pharmacol. 43, 2601-2608.
227. Eliason, J.F., Ramuz, H. and Kaufmann, F. (1990) Human multi-drug-resistant cancer cells exhibit a high degree of selectivity for stereoisomers of verapamil and quinidine. Int. J. Cancer 46, 113-117.
228. Sehested, M., Skovsgaard, T., Van Deurs, B. and Winther-Nielsen, H. (1987) Increased plasma membrane traffic in daunorubicin-resistant P388 leukaemia cells. Effect of daunorubicin and verapamil. Br. J. Cancer 56, 747-751.
229. Bruggemann, E.P., Currier, S.J., Gottesman, M.M. and Pastan, I. (1992) Characterization of the azidopine and vinblastine binding site of P-glycoprotein. J. Biol. Chem. 267, 21020-21026.
230. Tamai, I. and Safa, A.R. (1991) Azidopine noncompetively interacts with vinblastine and cyclosporin A binding to P-glycoprotein in multidrug resistant cells. J. Biol. Chem. 266, 16796-16800.
231. Loo, T.W. and Clarke, D.M. (1993) Functional consequences of phenylalanine mutations in the predicted transmembrane domain of P-glycoprotein. J. Biol. Chem. 268, 19965-19972.
232. Ferry, D.R., Russell, M.A. and Cullen, M.H. (1992) P-glycoprotein possesses a 1,4-dihydropyridine-selective drug acceptor site which is allosterically coupled to a vinca-alkaloid-selective binding site. Biochem. Biophys. Res. Commun. 188, 440-445.
233. Chen, H.-X., Bamberger, U., Heckel, A., Guo, X. and Cheng, Y.-C. (1993) BIBW 22, a dipyridamole analogue, acts as a bifunctional modulator on tumor cells by influencing both P-glycoprotein and nucleoside transport, Cancer Res. 53, 1974-1977.
234. Gruber, A., Briese, B., Areström, I., Vitols, S., Björkholm, M. and Peterson, C. (1993) Effect of verapamil on daunorubicin accumulation in human leukemic cells with different levels of MDR1 gene expression. Leuk. Res. 17, 353-358.
235. Zaman, G.J.R., Versantvoort, C.H.M., Smit, J.J.M., Eijdems, E.W.H.M., de Haas, M., Smith, A.J., Broxterman, H.J., Mulder, N.H., De Vries, E.G.E., Baas, F. and Borst, P. (1993) Analysis of the expression of MRP, the gene for a new putative transmembrane drug transporter, in human multidrug resistant lung cancer cell lines. Cancer Res. 53, 1747-1750.
236. Grant, C.E., Valdimarsson, G., Hipfner, D.R., Almquist, K.C., Cole, S.P.C. and Deeley, R.G. (1994) Overexpression of multidrug resistance-associated protein (MRP) increases resistance to natural product drugs. Cancer Res. 54, 357-361.
237. Mülder, H.S., van Grondelle, R., Westerhoff, H.V. and Lankelma, J. (1993) A plasma membrane 'vacuum cleaner' for daunorubicin in non-P-glycoprotein multidrug-resistant SW-1573 human non-small cell lung carcinoma cells. A study using fluorescence resonance energy transfer. Eur. J. Biochem. 218, 871-882.
238. Krishnamachary, N. and Center, M.S. (1993) The MRP gene associated with a non-P-glycoprotein multidrug resistance encodes a 190-kDa membrane bound glycoprotein. Cancer Res. 53, 3658-3661.
239. Versantvoort, C.H.M., Schuurhuis, G.J., Pinedo, H.M., Eekman, C.A., Kuiper, C.M., Lankelma, J. and Broxterman, H.J. (1993) Genistein modulates the decreased drug accumulation in non-P-glycoprotein mediated multidrug resistant tumour cells. Br. J. Cancer 68, 939-946.
240. Cole, S.P.C., Bhardwaj, G., Gerlach, J.H., Mackie, J.E., Grant, C.E., Almquist, K.C., Stewart, A.J., Kurz, E.U., Duncan, A.M.V. and Deeley, R.G. (1992) Overexpression of a transporter gene in a multidrug resistant human lung cancer cell line. Science 258, 1650-1654.
241. Bakos, E., Hegedus, T., Hollos, Z., Welker, E., Tusnady, G.E., Zaman, G.J.R., Flens, M.J., Varadi, A. and Sarkadi, B. (1996) Membrane topology and glycosylation of the human multidrug resistance-associated protein. J. Biol. Chem. 271, 12322-12326.
242. Flens, M.J., Zaman, G.J.R., Van der Valk, P., Izquierdo, M.A., Schroeijers, A.B., Scheffer, G.L., van der Groep, P., de Haas, M., Meijer, C.J.L.M. and Scheper, R.J. (1996) Tissue distribution of the multidrug resistance protein. Am. J. Pathol. 148, 1237-1247.
243. Evers, R., Zaman, G.J.R., Van Deemter, L., Jansen, H., Calafat, J., Oomen, L.C.J.M., Oude Elferink, R.P.J., Borst, P. and Schinkel, A.H. (1996) Basolateral localization and export activity of the human multidrug resistance-associated protein (MRP) in polarized pig kidney cells. J. Clin. Invest. 97, 1211-1218.
244. Mayer, R., Kartenbeck, J., Büchler, M., Jedlitschky, G., Leier, I. and Keppler, D. (1995) Expression of the MRP gene-encoded conjugate export pump in liver and its selective absence from the canalicular membrane in transport-deficient mutant hepatocytes. J. Cell Biol. 131, 137-150.
245. Gekeler, V., Boer, R., Ise, W., Sanders, K.H., Schächtele, C. and Beck, J. (1995) The specific bisindolylmaleimide PKC-inhibitor GF 109203X efficiently modulates MRP-associated multiple drug resistance, Biochem. Biophys. Res. Commun. 206, 119-126.
246. Ma, L., Krishnamachary, N. and Center, M.S. (1995) Phosphorylation of the multidrug resistance associated protein gene encoded protein 190. Biochemistry 34, 3338-3343.
247. Müller, M., Meijer, C., Zaman, G.J.R., Borst, P. Scheper, R.J., Mulder, N.H., De Vries, E.G.E. and Jansen, P.L.M. (1994) Overexpression of the gene encoding the multidrug resistance-associated protein results in increased ATP-dependent glutathione S-conjugate transport. Proc. Natl. Acad. Sci. U.S.A. 91, 13033-13037.
248. Leier, I., Jedlitschky, G., Buchholz, U., Cole, S.P.C., Deeley, R.G. and Keppler, D. (1994) The MRP gene encodes an ATP-dependent export pump for leukotriene C-4, and structurally related conjugates. J. Biol. Chem. 269, 27807-27810.
249. Saxena, M. and Henderson, G.B. (1995) ATP-dependent efflux of 2,4-dinitrophenyl-S-glutathione: Properties of two distinct transport systems in inside-out vesicles from L1210 cells and a variant subline with altered efflux of methotrexate and cholate. J. Biol. Chem. 5312-5319.
250. Leier, I., Jedlitschky, G., Buchholz, U., Center, M., Cole, S.P.C., Deeley, R.G. and Keppler, D. (1996) ATP-dependent glutathione disulphide transport mediated by the MRP gene-encoded conjugate export pump. Biochem. J. 314, 433-437.
251. Jedlitschky, G., Leier, I., Buchholz, U., Barnouin, K., Kurz, G. and Keppler, D. (1996) Transport of glutathione, glucuronate, and sulfate conjugates by the MRP gene-encoded conjugate export pump. Cancer Res. 56, 988-994.
252. Zaman, G.J.R., Lankelma, J., van Tellingen, O., Beijnen, J.H., Dekker, H., Paulusma, C., Oude Elferink, R.P.J., Baas, F. and Borst, P. (1995) Role of glutathione in the export of compounds from cells by the multidrug-resistance-associated protein. Proc. Natl. Acad. Sci. U.S.A. 92, 7690-7694.
253. Loe, D.W., Almquist, K.C., Cole, S.P.C. and Deeley, R.G. (1996) ATP-dependent 17beta-estradiol 17-(beta-D-glucuronide) transport by multidrug resistance protein (MRP). J. Biol. Chem. 271, 9683-9689.
254. Feller, N., Broxterman, H.J., Wahrer, D.C.R. and Pinedo, H.M. (1995) ATP-dependent efflux of calcein by the multidrug resistance protein (MRP): No inhibition by intracellular glutathione depletion. FEBS Lett. 385-388.
255. Shen, H., Paul, S., Breuninger, L.M., Ciaccio, P.J., Laing, N.M., Helt, M., Tew, K.D. and Kruh, G.D. (1996) Cellular and in vitro transport of glutathione conjugates by MRP. Biochemistry 35, 5719-5725.
256. Loe, D.W., Almquist, K.C., Deeley, R.G. and Cole, S.P.C. (1996) Multidrug resistance protein (MRP)-mediated transport of leukotriene C4 and chemotherapeutic agents in membrane vesicles. J. Biol. Chem. 271, 9675-9682.
257. Paulusma, C.C., Bosma, P.J., Zaman, G.J.R., Bakker, C.T.M., Otter, M., Scheffer, G.L., Scheper, R.J., Borst, P. and Oude Elferink, R.P.J. (1996) Congenital jaundice in rats with a mutation in a multidrug resistance-associated protein gene. Science 271, 1126-1128.
258. Büchler, M., König, J., Brom, M., Kartenbeck, J., Spring, H., Horie, T. and Keppler, D. (1996) cDNA cloning of the hepatocyte canalicular isoform of the multidrug resistance protein, cMrp, reveals a novel conjugate export pump deficient in hyperbilirubinemic mutant rats. J. Biol. Chem. 271, 15091-15098.
259. Childs, S., Yen, R.L., Georges, E. and Ling, V. (1995) Identification of a sister gene to P-glycoprotein. Cancer Res. 55, 2029-2034.
260. Teeter, L.D., Hsu, H.-C., Curley, S.A., Tong, M.J. and Kuo, M.T. (1993) Expression of multidrug resistance (P-glycoprotein) MDR1 and MDR2 genes in human hepatocellular carcinomas and liver metastases of colonic tumors. Int. J. Oncol. 2, 73-80.
261. Kuo, M.T., Zhao, J.Y., Teeter, L.D., Ikeguchi, M. and Chisari, F.V. (1992) Activation of multidrug resistance (P-glycoprotein) mdr3/mdr1a gene during the development of hepatocellular carcinoma in hepatitis B virus transgenic mice. Cell Growth Differ. 3, 531-540.
262. Nakatsukasa, H., Evarts, R.P., Burt, R.K., Nagy, P. and Thorgeirsson, S.S. (1992) Cellular pattern of multidrug-resistance gene expression during chemical hepatocarcinogenesis in the rat. Mol. Carcinog. 6, 190-198.
263. Bradley, G., Sharma, R., Rajalakshmi, S. and Ling, V. (1992) P-glycoprotein expression during tumor progression in the rat liver. Cancer Res. 52, 5154-5161.
264. Fardel, O., Lecureur, V., Corlu, A. and Guillouzo, A. (1996) P-glycoprotein induction in rat liver epithelial cells in response to acute 3-methylcholanthrene treatment. Biochem. Pharmacol. 51, 1427-1436.
265. Watanabe, T., Suzuki, H., Sawada, Y., Naito, M., Tsuruo, T., Inaba, M., Hanano, M. and Sugiyama, Y. (1995) Induction of hepatic P-glycoprotein enhances biliary excretion of vincristine in rats. J. Hepatol. 23, 440-448.
266. Herzog, C.E., Tsokos, M., Bates, S.E. and Fojo, A.T. (1993) Increased mdr-1/P-glycoprotein expression after treatment of human colon carcinoma cells with P-glycoprotein antagonists. J. Biol. Chem. 268, 2946-2952.
267. Schuetz, E.G., Beck, W.T. and Schuetz, J.D. (1996) Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately up-regulate these proteins in human colon carcinoma cells. Mol. Pharmacol. 49, 311-318.
268. Schuetz, E.G., Schinkel, A.H., Relling, M.Y. and Schuetz, J.D. (1996) P-glycoprotein: a major determinant of rifampicin-inducible expression of cytochrome P4503a in mice and humans. Proc. Natl. Acad. Sci. U.S.A. 93, 4001-4005.
269. Fardel, O., Ratanasavanh, D., Loyer, P., Ketterer, B. and Guillouzo, A. (1992) Overexpression of the multidrug resistance gene product in adult rat hepatocytes during primary culture. Eur. J. Biochem. 205, 847-852.
270. Fardel, O., Morel, F. and Guillouzo, A. (1993) P-glycoprotein expression in human, mouse, hamster and rat hepatocytes in primary culture. Carcinogenesis 14, 781-783.
271. Lee, C.H., Bradley, G., Zhang, J.-T. and Ling, V. (1993) Differential expression of P-glycoprotein genes in primary rat hepatocyte culture. J. Cell. Physiol. 157, 392-402.
272. Acuña, C., Vollrath, V., Wielandt, A., Andrade, L., Duarte, I. and Chianale, J. (1994) Effect of colchicine and heat shock on multidrug resistance gene and P-glycoprotein expression in rat liver. J. Hepatol. 21, 754-763.
273. Dunn, S., Hughes, C.S., LeBlanc, G.A. and Cullen, J.M. (1996) Overexpression of a P-glycoprotein in hepatocellular carcinomas from Woodchuck hepatitis virus-infected Woodchucks (Marmota monax). Hepatology 23, 662-668.
274. Lee, C.H., Bradley, G. and Ling, V. (1995) Overexpression of the class II P-glycoprotein gene in primary rat hepatocyte culture: Evidence for increased mRNA stability. Cell Growth Differ. 6, 347-354.
275. Schott, B., Bennit, S., Pourquier, P., Ries, C., Londos-Gagliardi, D. and Robert, J. (1993) Differential over-expression of mdr1 genes in multidrug-resistant rat glioblastoma cell lines selected with doxorubicin or vincristine. Int. J. Cancer 55, 115-121.
276. Silverman, J.A. and Hill, B.A. (1995) Characterization of the basal and carcinogen regulatory elements of the rat mdr1b promotor. Mol. Carcinog. 13, 50-59. (Abstract)
277. Bhat, U.G., Winter, M.A., Pearce, H.L. and Beck, W.T. (1995) A structure-function relationship among reserpine and yohimbine analogues in their ability to increase expression of mdr1 and P-glycoprotein in a human colon carcinoma cell line. Mol. Pharmacol. 48, 682-689.
278. Taub, R. (1995) Expression and function of growth-induced genes during liver regeneration. In: R.L. Jirtle (ed.) Liver Regeneration and Carcinogenesis. Academic Press, London, pp. 71-97.
279. Hait, W.N. and Aftab, D.T. (1992) Rational design and pre-clinical pharmacology of drugs for reversing multidrug resistance. Biochem. Pharmacol. 43, 103-107.
280. Fine, R.L., Chambers, T.C. and Sachs, C.W. (1996) P-glycoprotein, multidrug resistance and protein kinase C. Stem Cells 14, 47-55.
281. Chambers, T.C., Chalikonda, I. and Eilon, G. (1990) Correlation of protein kinase C translocation, P-glycoprotein phosphorylation and reduced drug accumulation in multi-drug resistant human KB cells. Biochem. Biophys. Res. Commun. 169, 253-259.
282. Chambers, T.C., McAvoy, E.M., Jacobs, J.W. and Eilon, G. (1990) Protein kinase C phosphorylates P-glycoprotein in multidrug resistant human KB carcinoma cells. J. Biol. Chem. 265, 7679-7686.
283. Ford, J.M. and Hait, W.N. (1990) Pharmacology of drugs that alter multidrug resistance in cancer. Pharmacol. Rev. 42, 155-199.
284. Fine, R.L., Patel, J., Hamilton, T.C., Cowan, K., Curt, G.A., Friedman, M.A. and Chabner, B.A. (1986) Activation of protein kinase C (PKC) increases vincristine (VC) efflux and resistance in drug sensitive MCF-7 cells. Proc. Am. Assoc. Cancer Res. 27, 271.
285. Hamada, H., Hagiwara, K., Jakajima, T. and Tsuruo, T. (1987) Phosphorylation of the 170,000 to 180,000 glycoprotein specific to multi-drug resistant tumor cells: effects of verapamil, trifluoperazine and phorbol esters. Cancer Res. 47, 2860-2865.
286. Mellado, W. and Horwitz, S.B. (1987) Phosphorylation of the multi-drug resistance associated glycoprotein. Biochemistry 26, 6900-6904.
287. Center, M.S. (1983) Evidence that adriamycin resistance in Chinese hamster lung cells is regulated by phosphorylation of a plasma membrane glycoprotein. Biochem. Biophys. Res. Commun. 115, 159-166.
288. Mickley, L.A., Bates, S.E., Richert, N.D., Currier, S., Tanaka, S., Foss, F., Rosen, N. and Fojo, A.T. (1989) Modulation of the expression of a multidrug resistance gene (mdr-1/P-glycoprotein) by differentiating agents. J. Biol. Chem. 264, 18031-18040.
289. Goodfellow, H.R., Sardini, A., Ruetz, S., Callaghan, R., Gros, P., McNaughton, P.A. and Higgins, C.F. (1996) Protein kinase C-mediated phosphorylation does not regulate drug transport by the human multidrug resistance P-glycoprotein. J. Biol. Chem. 271, 13668-13674.
290. Bates, S.E., Currier, S.J., Alvarez, M. and Fojo, A.T. (1992) Modulation of P-glycoprotein phosphorylation and drug transport by sodium butyrate. Biochemistry 31, 6366-6372.
291. Nishizuka, Y. (1988) The molecular heterogeneity of protein kinase C and its implications for cellular regulation. Nature 334, 661-665.
292. Ward, N.E. and O'Brian, C.A. (1993) Inhibition of protein kinase C by N-myristoylated peptide substrate analogs. Biochemistry 32, 11903-11909.
293. Germann, U.A., Chambers, T.C., Ambudkar, S.V., Pastan, I. and Gottesman, M.M. (1995) Effects of phosphorylation of P-glycoprotein on multidrug resistance. J. Bioenerg. Biomembr. 27, 53-61.
294. Gupta, K.P., Ward, N.E., Gravitt, K.R., Bergman, P.J. and O'Brian, C.A. (1996) Partial reversal of multidrug resistance in human breast cancer cells by an N-myristoylated protein kinase C-α pseudosubstrate peptide. J. Biol. Chem. 271, 2102-2111.
295. Germann, U.A., Chambers, T.C., Ambudkar, S.V., Licht, T., Cardarelli, C.O., Pastan, I. and Gottesman, M.M. (1996) Characterization of phosphorylation-defective mutants of human P-glycoprotein expressed in mammalian cells. J. Biol. Chem. 1708-1716.
296. Bates, S.E., Lee, J.S., Dickstein, B., Spolyar, M. and Fojo, A.T. (1993) Differential modulation of P-glycoprotein transport by protein kinase inhibition. Biochemistry 32, 9156-9164.
297. Smith, C.D. and Zilfou, J.T. (1995) Circumvention of P-glycoprotein-mediated multiple drug resistance by phosphorylation modulators is independent of protein kinases. J. Biol. Chem. 270, 28145-28152.
298. Yu, G., Ahmad, S., Aquino, A., Fairchild, C.R., Trepel, J.B., Ohno, S., Suzuki, K., Tsuruo, T., Cowan, K.H. and Glazer, R.I. (1991) Transfection with protein kinase Cα confers increased multi-drug resistance to MCF-7 cells expressing P-glycoprotein. Cancer Commun. 3, 181-189.
299. ++ -dependent protein kinase. Biochem. Biophys. Res. Commun. 135, 397-402.
300. Hidaka, H. and Kobayashi, R. (1992) Pharmacology of protein kinase inhibitors. Annu. Rev. Pharmacol. Toxicol. 32, 377-397.
301. Sato, W., Yusa, K., Naito, M. and Tsuruo, T. (1990) Staurosporine, a potent inhibitor of C-kinase, enhances drug accumulation in multidrug-resistant cells. Biochem. Biophys. Res. Commun. 173, 1252-1257.
302. Wakusawa, S., Inoko, K., Miyamoto, K., Kajita, S., Hasegawa, T., Harimaya, K. and Koyama, M. (1993) Staurosporine derivatives reverse multidrug resistance without correlation with their protein kinase inhibitory activities. J. Antibiot. 46, 353-355.
303. Kobayashi, E., Nakano, H., Morimoto, M. and Tamaoki, T. (1989) Calphostin C (UCN-1028C), a novel microbial compound, is a highly potent and specific inhibitor of protein kinase C. Biochem. Biophys. Res. Commun. 159, 548-553.
304. Brunton, V.G. and Workman, P. (1993) Cell-signalling targets for antitumour drug development. Cancer Chemother. Pharmacol. 32, 1-19.
305. Grunicke, H. and Hofmann, J. (1992) Cytotoxic and cytostatic effects of antitumor agents induced at the plasma membrane level. Pharmacol. Ther. 55, 1-30.
306. Bieri, F. (1993) Peroxisome proliferators and cellular signaling pathways. A Review. Biol. Cell 77, 43-46.
307. Tang, E.K.Y. and Houslay, M.D. (1992) Glucagon, vasopressin and angiotensin all elicit a rapid, transient increase in hepatocyte protein kinase C activity. Biochem. J. 283, 341-346.
308. Oishi, K., Zheng, B. and Kuo, J.F. (1990) Inhibition of Na,K-ATPase and sodium pump by protein kinase C regulators sphingosine, lysophosphatidylcholine, and oleic acid. J. Biol. Chem. 265, 70-75.
309. Mori, T., Takai, Y., Minakuchi, R., Yu, B. and Nishizuka, Y. (1980) Inhibitory action of chlorpromazine, dibucaine, and other phospholipid-interacting drugs on calcium-activated, phospholipid-dependent protein kinase. J. Biol, Chem. 255, 8378-8380.
310. Chaudhary, P.M. and Roninson, I.B. (1993) Induction of multidrug resistance in human cells by transient exposure to different chemotherapeutic drugs. J. Natl. Cancer Inst. 85, 632-639.
311. Chaudhary, P.M. and Roninson, I.B. (1992) Activation of MDR1 (P-glycoprotein) gene expression in human cells by protein kinase C agonists. Oncol. Res. 4, 281-290.
312. Roelofsen, H., Ottenhof, R., Oude Elferink, R.P.J. and Jansen, P.L.M. (1991) Hepatocanalicular organic-anion transport is regulated by protein kinase C. Biochem. J. 278, 637-641.
313. Steen, H., Smit, H., Nijholt, A., Merema, M. and Meijer, D.K.F. (1993) Modulators of the protein kinase C system influence biliary excretion of cationic drugs. Hepatology 18, 1208-1215.
314. Müller, M., Mayer, R., Hero, U. and Keppler, D. (1994) ATP-dependent transport of amphiphilic cations across the hepatocyte canalicular membrane mediated by mdr1 P-glycoprotein. FEBS Lett. 343, 168-172.
315. Müller, M., Roelofsen, H. and Jansen, P.L. (1996) Secretion of organic anions by hepatocytes: involvement of homologues of the multidrug resistance protein. Semin. Liver. Dis. 16, 211-220.
316. Sparreboom, A., van Asperen, J., Mayer, U., Schinkel, A.H., Smit, J.W., Meijer, D.K.F., Borst, P., Nooijen, W.J., Beijnen, J.H. and van Tellingen, O. (1996) Limited oral bio-availability and active epithelial excretion of paclitaxe(taxol*) caused by P-glycoprotein in the intestine. Proc. Natl. Acad. Sci. U.S.A., 94, 2031-2035.
317. Gosland, M., Tsuboi, C., Hoffman, T., Goodin, S. and Vore, M. (1993) 17β-Estradiol glucuronide: An inducer of cholestasis and a physiological substrate for the multidrug resistance transporter. Cancer Res. 53, 5382-5385.
318. Vore, M. (1993) Canalicular transport: Discovery of ATP-dependent mechanisms. Toxicol. Appl. Pharmacol. 118, 2-7.
319. Wolf, D.C. and Horwitz, S.B. (1992) P-glycoprotein transports corticosterone and is photoaffinity-labeled by the steroid. Int. J. Cancer 52, 141-146.
320. Van Kalken, C.K., Broxterman, H.J., Pinedo, H.M., Feller, N., Dekker, H., Lankelma, J. and Giaccone, G. (1993) Cortisol is transported by the multidrug resistance gene product P-glycoprotein. Br. J. Cancer 67, 284-289.
321. De Lannoy, I.A.M. and Silverman, M. (1992) The MDR1 gene product, P-glycoprotein, mediates the transport of the cardiac glycoside, digoxin. Biochem. Biophys. Res. Commun. 189, 551-557.
322. Hori, R., Okamura, N., Aiba, T. and Tanigawara, Y. (1993) Role of P-glycoprotein in renal tubular secretion of digoxin in the isolated perfused rat kidney. J. Pharmacol. Exp. Ther. 266, 1620-1625.
323. Okamura, N., Hirai, M., Tanigawara, Y., Tanaka, K., Yasuhara, M., Ueda, K., Komano, T. and Hori, R. (1993) Digoxin-cyclosporin A interaction: Modulation of the multidrug transporter P-glycoprotein in the kidney. J. Pharmacol. Exp. Ther. 266, 1614-1619.
324. Ito, S., Koren, G., Harper, P.A. and Silverman, M. (1993) Energy-dependent transport of digoxin across renal tubular cell monolayers (LLC-PK1). Can. J. Physiol. Pharmacol. 71, 40-47.
325. Becker, K.F., Allmeier, H. and Höllt, V. (1992) New mechanisms of hormone secretion: MDR-like gene products as extrusion pumps for hormones? Horm. Metab. Res. 24, 210-213.
326. Olinga, P., Merema, M.T., Sandker, G.W., Slooff, M.J.H., Meijer, D.K.F. and Groothuis, G.M.M. (1995) Use of human liver slices and hepatocytes in transport and metabolism studies. In: A.M. Goldberg and L.F.M. van Zutphen (Eds.), The World Congress on Alternatives and Animal Use in the Life Sciences: Education, Research, Testing. Mary Ann Liebert, New York, pp. 197-203.
327. Sandker, G.W. (1993) Isolated human hepatocytes: a research tool for
328. Mayer, U., Wagenaar, E., Beijnen, J.H., Smit, J.W., Meijer, D.K.F., van Asperen, J., Borst, P. and Schinkel, A.H. (1996) Substantial excretion of digoxin via the intestinal mucosa and prevention of long-term digoxin accumulation in the brain by the mdr1a P-glycoprotein. Br. J. Pharmacol. 119, 1038-1044.
329. Smit, J.W., Schinkel A.H., Borst, P. and Meyer, D.K.F. (1996) Involvement of P-glycoprotein in the biliary and intestinal excretion of amphiphitic drugs: mdr gene knockout studies. Hepatology 24, 351 (Abstract).
330. Greenberger, L.M., Cohen, D. and Horwitz, S.B. (1994) In vitro models of multiple drug resistance. Cancer Treat. Res. 73, 69-106.