메뉴 건너뛰기




Volumn 23, Issue 1-3, 1997, Pages 77-98

Applications of the Caco-2 model in the design and development of orally active drugs: Elucidation of biochemical and physical barriers posed by the intestinal epithelium

Author keywords

active transport; Caco 2 cells; CYP1A; CYP3A; cytochrome P 450; drug discovery and development; drug interactions; glutath ione S transferase; intestinal epithelium; MDR P glycoprotein; mucosal toxicity; oral absorption; paracellular; phase I enzymes; phase II enzymes; sulfotransferase; transcellular; UDP glucuronosyltransferase

Indexed keywords

CELLS; DRUG INTERACTIONS; DRUG THERAPY; ENZYMES; METABOLISM; PROTEINS; TOXICITY;

EID: 0031022120     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0169-409X(96)00427-9     Document Type: Review
Times cited : (166)

References (84)
  • 1
    • 84934020420 scopus 로고
    • Intestinal absorption of xenobiotics
    • T.Z. Csaky (Ed.). Springer-Verlag, New York
    • Csaky, T.Z. (1984) Intestinal absorption of xenobiotics. In: T.Z. Csaky (Ed.), Pharmacology of Intestinal Permeation II. Springer-Verlag, New York, pp. 1 -30.
    • (1984) Pharmacology of Intestinal Permeation II , pp. 1-30
    • Csaky, T.Z.1
  • 2
    • 0000727573 scopus 로고
    • Functional morphology of the mucosa of the small intestine
    • L.R. Johnson (Ed.). Raven Press, New York
    • Madara. J.L and Trier, J.S. (1987) Functional morphology of the mucosa of the small intestine. In: L.R. Johnson (Ed.), Physiology of the Gastrointestinal Tract. Second edition. Raven Press, New York, pp. 1209-1249.
    • (1987) Physiology of the Gastrointestinal Tract. Second Edition , pp. 1209-1249
    • Madara, J.L.1    Trier, J.S.2
  • 3
    • 0000845392 scopus 로고
    • Drug transport across gastrointestinal epithelia
    • L.R. Johnson (Ed.). Raven Press, New York
    • Jackson, M.J. (1987) Drug transport across gastrointestinal epithelia. In: L.R. Johnson (Ed.), Physiology of the Gastrointestinal Tract. Second edition. Raven Press, New York, pp. 1597-1621.
    • (1987) Physiology of the Gastrointestinal Tract. Second Edition , pp. 1597-1621
    • Jackson, M.J.1
  • 4
    • 0028859318 scopus 로고
    • In vitro systems for studying intestinal drug absorption
    • Hillgren, K.M., Kato, A. and Borchardt, R.T. (1995) In vitro systems for studying intestinal drug absorption. Med. Res. Rev. 15, 83-109.
    • (1995) Med. Res. Rev. , vol.15 , pp. 83-109
    • Hillgren, K.M.1    Kato, A.2    Borchardt, R.T.3
  • 6
    • 0343653596 scopus 로고
    • In vivo biliary excretion and the isolated perfused liver preparation
    • C.-P. Siegers and J.B. Watkins III (Eds.). Gustav Fischer Verlag, New York
    • Siegers, C.-P. (1991) In vivo biliary excretion and the isolated perfused liver preparation. In: C.-P. Siegers and J.B. Watkins III (Eds.), Biliary Excretion of Drugs and other Chemicals. Gustav Fischer Verlag, New York, pp. 25-32.
    • (1991) Biliary Excretion of Drugs and Other Chemicals , pp. 25-32
    • Siegers, C.-P.1
  • 9
    • 0024593744 scopus 로고
    • Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability
    • Hidalgo, J., Raub, T.J. and Borchardt, R.T. (1989) Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology 96, 736-749.
    • (1989) Gastroenterology , vol.96 , pp. 736-749
    • Hidalgo, J.1    Raub, T.J.2    Borchardt, R.T.3
  • 10
    • 0025311288 scopus 로고
    • Epithelial transport of drugs in cell culture. I: A model for studying the passive diffusion of drugs over intestinal absorptive (Caco-2) cells
    • Artursson, P. (1990) Epithelial transport of drugs in cell culture. I: a model for studying the passive diffusion of drugs over intestinal absorptive (Caco-2) cells. J. Pharm. Sci. 79, 476-482.
    • (1990) J. Pharm. Sci. , vol.79 , pp. 476-482
    • Artursson, P.1
  • 11
    • 0025189818 scopus 로고
    • Transport and permeability properties of human Caco-2 cells: An in vitro model of the intestinal epithelial cell barrier
    • Wilson, G., Hassan, I., Dix, C., Williamson, I., Shah, R., Mackay, M. and Artursson, P. (1990) Transport and permeability properties of human Caco-2 cells: an in vitro model of the intestinal epithelial cell barrier. J. Control. Release 11, 25-40.
    • (1990) J. Control. Release , vol.11 , pp. 25-40
    • Wilson, G.1    Hassan, I.2    Dix, C.3    Williamson, I.4    Shah, R.5    Mackay, M.6    Artursson, P.7
  • 12
    • 0025132942 scopus 로고
    • Caco-2 cell monolayers as a model for drug transport across the intestinal mucosa
    • Hilgers, A., Conradi, R. and Burton, P. (1990) Caco-2 cell monolayers as a model for drug transport across the intestinal mucosa. Pharm. Res. 7, 902-910.
    • (1990) Pharm. Res. , vol.7 , pp. 902-910
    • Hilgers, A.1    Conradi, R.2    Burton, P.3
  • 13
    • 0026321138 scopus 로고
    • Cell culture as models for drug absorption across the intestinal mucosa
    • Artursson. P. (1991) Cell culture as models for drug absorption across the intestinal mucosa. Crit. Rev. Ther. Drug Carrier Syst. 8, 305-330.
    • (1991) Crit. Rev. Ther. Drug Carrier Syst. , vol.8 , pp. 305-330
    • Artursson, P.1
  • 14
    • 0025732815 scopus 로고
    • A model of human small intestinal absorptive cells. 1. Transport barrier
    • Cogburn, J., Donovan, M. and Schasteen, C. (1991) A model of human small intestinal absorptive cells. 1. Transport barrier. Pharm. Res. 8, 210-216.
    • (1991) Pharm. Res. , vol.8 , pp. 210-216
    • Cogburn, J.1    Donovan, M.2    Schasteen, C.3
  • 16
    • 0026040218 scopus 로고
    • Active transport of amino acids by gamma-glutamyl transpeptidase through Caco-2 cell monolayers
    • Smith, T., Gibson, C., Howlin, B. and Pratt, J. (1991) Active transport of amino acids by gamma-glutamyl transpeptidase through Caco-2 cell monolayers. Biochem. Biophys. Res. Commun. 178, 1028-1035.
    • (1991) Biochem. Biophys. Res. Commun. , vol.178 , pp. 1028-1035
    • Smith, T.1    Gibson, C.2    Howlin, B.3    Pratt, J.4
  • 17
    • 0025904505 scopus 로고
    • Expression of dipeptidyl aminopeptidase IV during enterocytic differentiation of human colon cancer (Caco-2) cells
    • Yoshioka, M., Erickson, P., Matsumoto, H., Gum, E. and Kim, Y. (1991) Expression of dipeptidyl aminopeptidase IV during enterocytic differentiation of human colon cancer (Caco-2) cells. Int. J. Cancer 47, 916-921.
    • (1991) Int. J. Cancer , vol.47 , pp. 916-921
    • Yoshioka, M.1    Erickson, P.2    Matsumoto, H.3    Gum, E.4    Kim, Y.5
  • 18
    • 0025668535 scopus 로고
    • Mechanism of L-α-methyldopa transport through a monolayer of polarized human intestinal epithelial cells (Caco-2)
    • Hu, M. and Borchardt, R. (1990) Mechanism of L-α-methyldopa transport through a monolayer of polarized human intestinal epithelial cells (Caco-2). Pharm. Res. 7, 1313-1319.
    • (1990) Pharm. Res. , vol.7 , pp. 1313-1319
    • Hu, M.1    Borchardt, R.2
  • 19
    • 0025046860 scopus 로고
    • Uptake of the cephalosporin, Cephalexin by a dipeptide transport carrier in the human intestinal cell line, Caco-2
    • Dantzig, A. and Bergin, L. (1990) Uptake of the cephalosporin, Cephalexin by a dipeptide transport carrier in the human intestinal cell line, Caco-2. Biochim. Biophys. Acta 1027, 211-217.
    • (1990) Biochim. Biophys. Acta , vol.1027 , pp. 211-217
    • Dantzig, A.1    Bergin, L.2
  • 20
    • 0027279803 scopus 로고
    • Regulation of cytochrome P450 in cultured human colonic cells
    • Rosenberg, D.W. and Leff, T. (1993) Regulation of cytochrome P450 in cultured human colonic cells. Arch. Biochem. Biophys. 300, 186-192.
    • (1993) Arch. Biochem. Biophys. , vol.300 , pp. 186-192
    • Rosenberg, D.W.1    Leff, T.2
  • 21
    • 0026981085 scopus 로고
    • Regulation of cytochrome P4501A1 gene expression in a human intestinal cell line, Caco-2
    • Boulenc, X., Bourrie, M., Fabre, I., Roque, C., Joyeux, H., Berger, Y. and Fabre, G. (1992) Regulation of cytochrome P4501A1 gene expression in a human intestinal cell line, Caco-2. J. Pharm. Exp. Ther. 263, 1471-1472.
    • (1992) J. Pharm. Exp. Ther. , vol.263 , pp. 1471-1472
    • Boulenc, X.1    Bourrie, M.2    Fabre, I.3    Roque, C.4    Joyeux, H.5    Berger, Y.6    Fabre, G.7
  • 22
    • 0027427271 scopus 로고
    • Phase I and II biotransformations in living Caco-2 cells cultivated under serum-free conditions
    • Sergent-Engelen, T., Delistrie,V. and Schneider, Y.-J. (1993) Phase I and II biotransformations in living Caco-2 cells cultivated under serum-free conditions. Biochem. Pharm. 46, 1393-1401.
    • (1993) Biochem. Pharm. , vol.46 , pp. 1393-1401
    • Sergent-Engelen, T.1    Delistrie, V.2    Schneider, Y.-J.3
  • 23
    • 0024789567 scopus 로고
    • Time-dependent activity and expression of glutathione S-transferases in the human colon adenocarcinoma cell line Caco-2
    • Peters, W.H.N. and Roelofs, H.M.J. (1989) Time-dependent activity and expression of glutathione S-transferases in the human colon adenocarcinoma cell line Caco-2. Biochem. J. 264, 613-616
    • (1989) Biochem. J. , vol.264 , pp. 613-616
    • Peters, W.H.N.1    Roelofs, H.M.J.2
  • 24
    • 0025781413 scopus 로고
    • Substrate specificity and some properties of phenol sulfotransferase from human intestinal Caco-2 cells
    • Baranczyk-Kuzma, A., Garren, J.A., Hidalgo, I.J. and Borchardt, R. (1991) Substrate specificity and some properties of phenol sulfotransferase from human intestinal Caco-2 cells. Life Sci. 49, 1197-1206.
    • (1991) Life Sci. , vol.49 , pp. 1197-1206
    • Baranczyk-Kuzma, A.1    Garren, J.A.2    Hidalgo, I.J.3    Borchardt, R.4
  • 25
    • 0026050976 scopus 로고
    • Evidence for glucuronide conjugation of p-nitrophenol in the Caco-2 cell model
    • Bjorge, S., Hamelehle, K.L., Homan, R., Rose, S.E., Turluck, D.A. and Wright, D.S. ( 1991 ) Evidence for glucuronide conjugation of p-nitrophenol in the Caco-2 cell model. Pharm. Res. 8, 1441-1443.
    • (1991) Pharm. Res. , vol.8 , pp. 1441-1443
    • Bjorge, S.1    Hamelehle, K.L.2    Homan, R.3    Rose, S.E.4    Turluck, D.A.5    Wright, D.S.6
  • 26
    • 0028984234 scopus 로고
    • Glucuronidation in the Caco-2 human intestinal cell line: Induction of UDP-glucuronosyltransferase 1*6
    • Abid, A., Bouchon, I., Siest, G. and Sabolovic, N. (1995) Glucuronidation in the Caco-2 human intestinal cell line: induction of UDP-glucuronosyltransferase 1*6. Biochem. Pharmacol. 50, 557-561.
    • (1995) Biochem. Pharmacol. , vol.50 , pp. 557-561
    • Abid, A.1    Bouchon, I.2    Siest, G.3    Sabolovic, N.4
  • 29
    • 0026644535 scopus 로고
    • Drug metabolism by cytochromes P450 in the liver and small bowel
    • Watkins, P. (1992) Drug metabolism by cytochromes P450 in the liver and small bowel. Gastrointest. Pharmacol. 21, 511-526.
    • (1992) Gastrointest. Pharmacol. , vol.21 , pp. 511-526
    • Watkins, P.1
  • 31
    • 0026464616 scopus 로고
    • Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes
    • Kolars, J.C., Schmiedlin-Ren, P., Schuetz, D.J., Fang, C. and Watkins, P.B. (1992) Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes. J. Clin. Invest. 90, 1871-1878.
    • (1992) J. Clin. Invest. , vol.90 , pp. 1871-1878
    • Kolars, J.C.1    Schmiedlin-Ren, P.2    Schuetz, D.J.3    Fang, C.4    Watkins, P.B.5
  • 32
    • 0024604149 scopus 로고
    • Cytochromes P-450 in the intestinal mucosa of man
    • Peters, W.H.M. and Kremers, P.G. (1989) Cytochromes P-450 in the intestinal mucosa of man. Biochem. Pharmacol. 38, 1535-1538.
    • (1989) Biochem. Pharmacol. , vol.38 , pp. 1535-1538
    • Peters, W.H.M.1    Kremers, P.G.2
  • 33
    • 0026598851 scopus 로고
    • Small intestinal cytochromes P450
    • Kaminsky, L.S. and Fasco, M.J. (1992) Small intestinal cytochromes P450. Crit. Rev. Toxicol. 21, 407-422.
    • (1992) Crit. Rev. Toxicol. , vol.21 , pp. 407-422
    • Kaminsky, L.S.1    Fasco, M.J.2
  • 34
    • 0025804183 scopus 로고
    • Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells
    • Artursson, P. and Karlsson, J. (1991) Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelial (Caco-2) cells. Biochem. Biophys. Res. Commun. 175, 880-885.
    • (1991) Biochem. Biophys. Res. Commun. , vol.175 , pp. 880-885
    • Artursson, P.1    Karlsson, J.2
  • 35
    • 0025329248 scopus 로고
    • Epithelial transport of drugs in cell culture. II: Effect of extracellular calcium concentration on the paracellular transport of drugs of different lipophilicities across monolayers of the intestinal epithelial (Caco-2) cells
    • Artursson, P. and Magnusson, C. (1990) Epithelial transport of drugs in cell culture. II: effect of extracellular calcium concentration on the paracellular transport of drugs of different lipophilicities across monolayers of the intestinal epithelial (Caco-2) cells. J. Pharm. Sci. 79, 595-600.
    • (1990) J. Pharm. Sci. , vol.79 , pp. 595-600
    • Artursson, P.1    Magnusson, C.2
  • 36
    • 0002833727 scopus 로고
    • Intestinal water and electrolyte transport
    • L.R. Johnson (Ed.). Raven Press, New York
    • Powell, D.W. (1987) Intestinal water and electrolyte transport. In: L.R. Johnson (Ed.), Physiology of the Gastrointestinal Tract. Second edition. Raven Press, New York, pp. 1267-1305.
    • (1987) Physiology of the Gastrointestinal Tract. Second Edition , pp. 1267-1305
    • Powell, D.W.1
  • 37
    • 0027441125 scopus 로고
    • The mucus layer as a barrier to drug absorption in monolayers if human intestinal epithelial HT29-H goblet cells
    • Karlsson, J., Wikman, A. and Artursson, P. (1993) The mucus layer as a barrier to drug absorption in monolayers if human intestinal epithelial HT29-H goblet cells. Int. J. Pharm. 99, 209-218.
    • (1993) Int. J. Pharm. , vol.99 , pp. 209-218
    • Karlsson, J.1    Wikman, A.2    Artursson, P.3
  • 38
    • 0027134778 scopus 로고
    • Mechanism of intestinal absorption of renitidine and ondansetron: Transport across Caco-2 cell monolayers
    • Gan, L.-S., Hsyu, P.-H., Pritchard, J.F. and Thakker, D. (1993) Mechanism of intestinal absorption of renitidine and ondansetron: transport across Caco-2 cell monolayers. Pharm. Res. 10, 1722-1725.
    • (1993) Pharm. Res. , vol.10 , pp. 1722-1725
    • Gan, L.-S.1    Hsyu, P.-H.2    Pritchard, J.F.3    Thakker, D.4
  • 39
    • 0029096972 scopus 로고
    • Ondansetron clinical pharmacokinetics
    • Roila, F. and Del Favero, A. (1995) Ondansetron clinical pharmacokinetics. Clin. Pharmacokinet. 29, 95-109.
    • (1995) Clin. Pharmacokinet. , vol.29 , pp. 95-109
    • Roila, F.1    Del Favero, A.2
  • 41
    • 0026076770 scopus 로고
    • Determination of ondansetron in plasma and its pharmacokinetics in the young and elderly
    • Colthup, P., Felgate, C., Palmer, J. and Scully, N. (1991) Determination of ondansetron in plasma and its pharmacokinetics in the young and elderly. J. Pharm. Sci. 80, 868-871.
    • (1991) J. Pharm. Sci. , vol.80 , pp. 868-871
    • Colthup, P.1    Felgate, C.2    Palmer, J.3    Scully, N.4
  • 42
    • 0020641162 scopus 로고
    • Ranitidine bioavailability and kinetics in normal male subjects
    • Gary, D., Weidler, D. and Eshelman, F. (1983) Ranitidine bioavailability and kinetics in normal male subjects. Clin. Pharmacol. Ther. 33, 445-452.
    • (1983) Clin. Pharmacol. Ther. , vol.33 , pp. 445-452
    • Gary, D.1    Weidler, D.2    Eshelman, F.3
  • 43
    • 0343217955 scopus 로고
    • Effect of apical and/or basolateral application of EDTA on the permeability of hydrophilic compounds in a human intestinal epithelial cell line (Caco-2)
    • De Boer, A., Noach, A., Roosemalen, M., Kurosaki, Y. and Breimer, D. (1991) Effect of apical and/or basolateral application of EDTA on the permeability of hydrophilic compounds in a human intestinal epithelial cell line (Caco-2). Pharm. Res. 8, S215.
    • (1991) Pharm. Res. , vol.8
    • De Boer, A.1    Noach, A.2    Roosemalen, M.3    Kurosaki, Y.4    Breimer, D.5
  • 44
    • 0005020717 scopus 로고
    • Transepithelial secretion of the histamine H2 receptor antagonist ranitidine in human intestinal epithelial Caco-2 monolayers is mediated by P-glycoprotein
    • Cook, M.J. and Hirst, B.H. (1994) Transepithelial secretion of the histamine H2 receptor antagonist ranitidine in human intestinal epithelial Caco-2 monolayers is mediated by P-glycoprotein. J. Physiol. 479, 103P.
    • (1994) J. Physiol. , vol.479
    • Cook, M.J.1    Hirst, B.H.2
  • 45
    • 26544460679 scopus 로고
    • Study of intestinal transport of glycylsarcosine and thyrotropin-releasing hormone using the in vitro Caco-2 cell culture system
    • Can, L.-S., Eads, C., Niederer, T. and Thakker, D. (1993) Study of intestinal transport of glycylsarcosine and thyrotropin-releasing hormone using the in vitro Caco-2 cell culture system. Fed. Am. Soc. Exp. Biol. J. 7, A578.
    • (1993) Fed. Am. Soc. Exp. Biol. J. , vol.7
    • Can, L.-S.1    Eads, C.2    Niederer, T.3    Thakker, D.4
  • 47
    • 0027487992 scopus 로고
    • +-coupled dipeptide (glycylsarcosine) transport across apical and basal borders of human intestinal Caco-2 cell monolayers display distinctive characteristics
    • +-coupled dipeptide (glycylsarcosine) transport across apical and basal borders of human intestinal Caco-2 cell monolayers display distinctive characteristics. Biochim. Biophys. Acta 1151, 237-245.
    • (1993) Biochim. Biophys. Acta , vol.1151 , pp. 237-245
    • Thwaites, D.1    Brown, C.2    Hirst, B.3    Simmons, N.4
  • 48
    • 0022512635 scopus 로고
    • + gradient-dependent transport of aminocephalosporins in rat intestinal brush-border membrane vesicles
    • + Gradient-dependent transport of aminocephalosporins in rat intestinal brush-border membrane vesicles. Biochem. Pharmacol. 35, 1781-1786.
    • (1986) Biochem. Pharmacol. , vol.35 , pp. 1781-1786
    • Okano, T.1    Inui, K.-I.2    Takano, M.3    Hori, R.4
  • 49
    • 0022999796 scopus 로고
    • + coupled uphill transport of aminocephalosporins via the dipeptide transport system in rabbit intestinal brush-border membranes
    • + Coupled uphill transport of aminocephalosporins via the dipeptide transport system in rabbit intestinal brush-border membranes. J. Biol. Chem. 261, 14130-14134.
    • (1986) J. Biol. Chem. , vol.261 , pp. 14130-14134
    • Okano, T.1    Inui, K.-I.2    Maegawa, H.3    Takano, M.4    Hori, R.5
  • 50
    • 0021025978 scopus 로고
    • Role of pH gradient and membrane potential in dipeptide transport in intestinal and renal brush-border membrane vesicles from the rabbit
    • Ganapathy V. and Leibach, F. (1983) Role of pH gradient and membrane potential in dipeptide transport in intestinal and renal brush-border membrane vesicles from the rabbit. J. Biol. Chem. 258, 14189-14192.
    • (1983) J. Biol. Chem. , vol.258 , pp. 14189-14192
    • Ganapathy, V.1    Leibach, F.2
  • 51
    • 0023716170 scopus 로고
    • + coupled transport of p.o. cephalosporins via dipeptide carrier in rabbit intestinal brush-border membranes: Difference of transport characteristics between cefixime and cephradine
    • + Coupled transport of p.o. cephalosporins via dipeptide carrier in rabbit intestinal brush-border membranes: difference of transport characteristics between cefixime and cephradine. J. Pharmacol. Exp. Ther. 247, 235-241.
    • (1988) J. Pharmacol. Exp. Ther. , vol.247 , pp. 235-241
    • Inui, K.-I.1    Okano, T.2    Maegawa, H.3    Kato, M.4    Hori, R.5
  • 52
    • 33645830172 scopus 로고
    • A surface glycoprotein modulating drug permeability Chinese hamster ovary cell mutants
    • Juliano, R.L. and Ling, V. (1976) A surface glycoprotein modulating drug permeability Chinese hamster ovary cell mutants. Biochim. Biophys. Acta 455, 152-162.
    • (1976) Biochim. Biophys. Acta , vol.455 , pp. 152-162
    • Juliano, R.L.1    Ling, V.2
  • 53
    • 0027218689 scopus 로고
    • Biochemistry of multidrug resistance mediated by the multidrug transporter
    • Gottesman, M.M. and Pastan, I. (1993) Biochemistry of multidrug resistance mediated by the multidrug transporter. Annu. Rev. Biochem. 62, 385-427.
    • (1993) Annu. Rev. Biochem. , vol.62 , pp. 385-427
    • Gottesman, M.M.1    Pastan, I.2
  • 55
    • 0024576304 scopus 로고
    • Immunohistochemical localization in normal tissues of different epitopes in the multidrug transport protein P170: Evidence for localization in brain capillaries and cross reactivity of on antibody with a muscle protein
    • Thiebaut, F., Tsuruo, T., Hamada, H., Gottesman, M.M., Pastan, I. and Willingham, M.C. (1989) Immunohistochemical localization in normal tissues of different epitopes in the multidrug transport protein P170: evidence for localization in brain capillaries and cross reactivity of on antibody with a muscle protein. J. Histochem. Cytochem. 37, 159-164.
    • (1989) J. Histochem. Cytochem. , vol.37 , pp. 159-164
    • Thiebaut, F.1    Tsuruo, T.2    Hamada, H.3    Gottesman, M.M.4    Pastan, I.5    Willingham, M.C.6
  • 56
    • 0025991880 scopus 로고
    • P-glycoprotein content and mediation of vincristine efflux: Correlation with the level of differentiation in luminal epithelium of mouse small intestine
    • Meyers, M.B., Scotto, K.W. and Sirotnak, F.M. (1991) P-glycoprotein content and mediation of vincristine efflux: correlation with the level of differentiation in luminal epithelium of mouse small intestine. Cancer Commun. 3, 159-165.
    • (1991) Cancer Commun. , vol.3 , pp. 159-165
    • Meyers, M.B.1    Scotto, K.W.2    Sirotnak, F.M.3
  • 57
    • 0025912228 scopus 로고
    • Epithelial secretion of vinblastine by human intestinal adenocarcinoma cell (HCT-8 and T84) layers expressing P-glycoprotein
    • Hunter, J., Hirst, B.H. and Simmons, N.L. (1991) Epithelial secretion of vinblastine by human intestinal adenocarcinoma cell (HCT-8 and T84) layers expressing P-glycoprotein. Br. J. Cancer 64, 437-444.
    • (1991) Br. J. Cancer , vol.64 , pp. 437-444
    • Hunter, J.1    Hirst, B.H.2    Simmons, N.L.3
  • 58
    • 0027267598 scopus 로고
    • Evidence for a polarized efflux system for peptides in the apical membrane of Caco-2 cells
    • Burton, P.S., Conradi, R.A., Hilgers, A.R. and Ho, N.F.H. (1993) Evidence for a polarized efflux system for peptides in the apical membrane of Caco-2 cells. Biochem. Biophys. Res. Commun. 190, 760-766.
    • (1993) Biochem. Biophys. Res. Commun. , vol.190 , pp. 760-766
    • Burton, P.S.1    Conradi, R.A.2    Hilgers, A.R.3    Ho, N.F.H.4
  • 60
    • 0027180795 scopus 로고
    • Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers
    • Hunter, J., Hirst, B.H. and Simmons, N.L. (1993) Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers. Pharm. Res. 10, 743-749.
    • (1993) Pharm. Res. , vol.10 , pp. 743-749
    • Hunter, J.1    Hirst, B.H.2    Simmons, N.L.3
  • 61
    • 0025887582 scopus 로고
    • Factors influencing the pharmacokinetics of cyclosporine in man
    • Lindholm, A. (1991) Factors influencing the pharmacokinetics of cyclosporine in man. Therap. Drug Monit. 13, 465-477.
    • (1991) Therap. Drug Monit. , vol.13 , pp. 465-477
    • Lindholm, A.1
  • 63
    • 0021012807 scopus 로고
    • Cyclosporine: Pharmacokinetics, metabolism, and drug interactions
    • Wood, A.J., Maurer, G., Niederberger, W. and Beveridge, T. (1983) Cyclosporine: pharmacokinetics, metabolism, and drug interactions. Transplant. Proc. XV, 2409-2412.
    • (1983) Transplant. Proc. , vol.15 , pp. 2409-2412
    • Wood, A.J.1    Maurer, G.2    Niederberger, W.3    Beveridge, T.4
  • 66
    • 0024512139 scopus 로고
    • Clinical pharmacokinetics of cyclosporin
    • McMillan, M.A. (1989) Clinical pharmacokinetics of cyclosporin. Pharmacol. Ther. 42, 135-156.
    • (1989) Pharmacol. Ther. , vol.42 , pp. 135-156
    • McMillan, M.A.1
  • 69
    • 0026457407 scopus 로고
    • Bioavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic enzyme induction
    • Herbert, MF., Roberts, J.P., Prueksaritanont, T. and Benet, L.Z. (1992) Bioavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic enzyme induction. Clin. Pharmacol. Ther. 52, 453-457.
    • (1992) Clin. Pharmacol. Ther. , vol.52 , pp. 453-457
    • Herbert, M.F.1    Roberts, J.P.2    Prueksaritanont, T.3    Benet, L.Z.4
  • 70
    • 85034892163 scopus 로고
    • Glutathione S-transferase, cytochrome P450, and uridine 5′-diphosphate-glucuronosyltranferase in human small intestine and liver
    • Peters, W.H.M., Nagengast, F.M. and van Tongeren, J.H.M. (1989) Glutathione S-transferase, cytochrome P450, and uridine 5′-diphosphate-glucuronosyltranferase in human small intestine and liver. Gastroenterology 96, 783-789.
    • (1989) Gastroenterology , vol.96 , pp. 783-789
    • Peters, W.H.M.1    Nagengast, F.M.2    Van Tongeren, J.H.M.3
  • 71
    • 0025922048 scopus 로고
    • Biotransformation enzymes in human intestine: Critical low levels in the colon
    • Peters, W.H.M., Kock, L., Nagengast, F.M. and Kremers, P.G. (1991) Biotransformation enzymes in human intestine: critical low levels in the colon. Gut 32, 408-412.
    • (1991) Gut , vol.32 , pp. 408-412
    • Peters, W.H.M.1    Kock, L.2    Nagengast, F.M.3    Kremers, P.G.4
  • 73
    • 0342348353 scopus 로고
    • Peptidases of the small intestinal brush border membrane
    • J. Kopecek (Ed.), Controlled Release Soc., Deerfield, IL
    • Erickson, R.H. (1992) Peptidases of the small intestinal brush border membrane. Proc. 19th Int. Symp. Controlled Release Bioact. Mater. 4-5, J. Kopecek (Ed.), Controlled Release Soc., Deerfield, IL.
    • (1992) Proc. 19th Int. Symp. Controlled Release Bioact. Mater. , pp. 4-5
    • Erickson, R.H.1
  • 74
    • 0028197288 scopus 로고
    • Absorption of peptide and peptidomimetic drugs
    • Amidon G.L. and Lee H.J. (1994) Absorption of peptide and peptidomimetic drugs. Annu. Rev. Pharmacol. Toxicol. 34, 321-341.
    • (1994) Annu. Rev. Pharmacol. Toxicol. , vol.34 , pp. 321-341
    • Amidon, G.L.1    Lee, H.J.2
  • 75
    • 0022385582 scopus 로고
    • Metabolism of cyclosporine
    • Maurer, G. (1985) Metabolism of cyclosporine. Transplant. Proc. XVII, 19-26.
    • (1985) Transplant. Proc. , vol.17 , pp. 19-26
    • Maurer, G.1
  • 76
    • 0021012807 scopus 로고
    • Cyclosporine: Pharmacokinetics, metabolism, and drug interactions
    • Wood, A.J., Maurer, G., Niederberger, W. and Beveridge, T. (1983) Cyclosporine: pharmacokinetics, metabolism, and drug interactions. Transplant. Proc. XV, 2409-2412.
    • (1983) Transplant. Proc. , vol.15 , pp. 2409-2412
    • Wood, A.J.1    Maurer, G.2    Niederberger, W.3    Beveridge, T.4
  • 77
    • 0025647855 scopus 로고
    • The role of cytochromes P-450 in cyclosporine metabolism
    • Watkins, P. (1990) The role of cytochromes P-450 in cyclosporine metabolism. J. Am. Acad. Dermatol. 6, 1301-1311.
    • (1990) J. Am. Acad. Dermatol. , vol.6 , pp. 1301-1311
    • Watkins, P.1
  • 78
    • 0026034777 scopus 로고
    • Cyclosporin metabolism by the gastrointestinal mucosa
    • Tjia, J.F., Webber, I.R. and Back, D.J. (1991) Cyclosporin metabolism by the gastrointestinal mucosa. Br. J. Clin. Pharmacol. 31, 344-346.
    • (1991) Br. J. Clin. Pharmacol. , vol.31 , pp. 344-346
    • Tjia, J.F.1    Webber, I.R.2    Back, D.J.3
  • 79
    • 0026443864 scopus 로고
    • Cyclosporin A metabolism in human liver, kidney, and intestine slices, comparison to rat and dog slices and human cell lines
    • Vickers, A.E.M., Fisher, V., Connors, S., Fisher, R.L., Baldeck, J.-P., Maurer, G. and Brendel, K. (1992) Cyclosporin A metabolism in human liver, kidney, and intestine slices, comparison to rat and dog slices and human cell lines. Drug Metab. Dispos. 20, 802-809.
    • (1992) Drug Metab. Dispos. , vol.20 , pp. 802-809
    • Vickers, A.E.M.1    Fisher, V.2    Connors, S.3    Fisher, R.L.4    Baldeck, J.-P.5    Maurer, G.6    Brendel, K.7
  • 80
    • 0025719746 scopus 로고
    • First-pass metabolism of cyclosporin by the gut
    • Kolars, J.C., Awni, W.M., Merion, R.M. and Watkins, P.B. (1991) First-pass metabolism of cyclosporin by the gut. Lancet 338, 1488-1490.
    • (1991) Lancet , vol.338 , pp. 1488-1490
    • Kolars, J.C.1    Awni, W.M.2    Merion, R.M.3    Watkins, P.B.4
  • 81
    • 0029012009 scopus 로고
    • CYP3A4 expressed by insect cells infected with a recombinant Baculovirus containing both CYP3A4 and human NADPH-cytochrome P450 reductase is catalytically similar to human liver microsomal CYP3A4
    • Lee, C.A., Kadwell, S.H., Kost, T.A. and Serabjit-Singh, C.J. (1995) CYP3A4 Expressed by insect cells infected with a recombinant Baculovirus containing both CYP3A4 and human NADPH-cytochrome P450 reductase is catalytically similar to human liver microsomal CYP3A4. Arch. Biochem. Biophys. 319, 157-167.
    • (1995) Arch. Biochem. Biophys. , vol.319 , pp. 157-167
    • Lee, C.A.1    Kadwell, S.H.2    Kost, T.A.3    Serabjit-Singh, C.J.4
  • 83
    • 0026642306 scopus 로고
    • Glucuronidation and its role in regulation of biological activity of drugs
    • Mulder, G.J. (1992) Glucuronidation and its role in regulation of biological activity of drugs. Annu. Rev. Pharmarcol. Toxicol. 32, 25-49.
    • (1992) Annu. Rev. Pharmarcol. Toxicol. , vol.32 , pp. 25-49
    • Mulder, G.J.1


* 이 정보는 Elsevier사의 SCOPUS DB에서 KISTI가 분석하여 추출한 것입니다.