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Volumn 14, Issue 1, 2013, Pages 102-111

In vitro methods to study the interplay of drug metabolism and efflux in the intestine

Author keywords

Absorption pharmacokinetics; Drug metabolism; Efflux transporters; Efflux metabolism interplay; In vitro methods; Intestinal absorption

Indexed keywords

ADENOSINE TRIPHOSPHATASE; CYCLOSPORIN A; CYTOCHROME P450 3A; DRUG METABOLITE; MIDAZOLAM; MULTIDRUG RESISTANCE PROTEIN;

EID: 84871343948     PISSN: 13892002     EISSN: 18755453     Source Type: Journal    
DOI: 10.2174/138920013804545241     Document Type: Article
Times cited : (15)

References (101)
  • 1
    • 85047683939 scopus 로고    scopus 로고
    • Maximising use of in vitro ADMET tools to predict in vivo bioavailability and safety
    • Wang, J.; Urban L.; Bojanic D. Maximising use of in vitro ADMET tools to predict in vivo bioavailability and safety. Expert Opin. Drug Metab. Toxicol., 2007, 3, 641-65.
    • (2007) Expert Opin. Drug Metab. Toxicol. , vol.3 , pp. 641-665
    • Wang, J.1    Urban, L.2    Bojanic, D.3
  • 2
    • 0345275777 scopus 로고    scopus 로고
    • The small intestine as a xenobioticmetabolizing organ
    • Kaminsky, L. S.; Zhang Q. Y. The small intestine as a xenobioticmetabolizing organ. Drug Metab. Dispos., 2003, 31, 1520-5.
    • (2003) Drug Metab. Dispos. , vol.31 , pp. 1520-1525
    • Kaminsky, L.S.1    Zhang, Q.Y.2
  • 3
    • 61749098274 scopus 로고    scopus 로고
    • The biological and clinical role of drug transporters at the intestinal barrier
    • Oostendorp, R. L.; Beijnen J. H.; Schellens J. H. The biological and clinical role of drug transporters at the intestinal barrier. Cancer Treat. Rev., 2009, 35, 137-47.
    • (2009) Cancer Treat. Rev. , vol.35 , pp. 137-147
    • Oostendorp, R.L.1    Beijnen, J.H.2    Schellens, J.H.3
  • 4
    • 68149170038 scopus 로고    scopus 로고
    • The role of transporters in the pharmacokinetics of orally administered drugs
    • Shugarts, S.; Benet L. Z. The role of transporters in the pharmacokinetics of orally administered drugs. Pharm. Res., 2009, 26, 2039-54.
    • (2009) Pharm. Res. , vol.26 , pp. 2039-2054
    • Shugarts, S.1    Benet, L.Z.2
  • 5
    • 0346728729 scopus 로고    scopus 로고
    • The ABCs of drug transport in intestine and liver: Efflux proteins limiting drug absorption and bioavailability
    • Chan, L. M.; Lowes S.; Hirst B. H. The ABCs of drug transport in intestine and liver: efflux proteins limiting drug absorption and bioavailability. Eur. J. Pharm. Sci., 2004, 21, 25-51.
    • (2004) Eur. J. Pharm. Sci. , vol.21 , pp. 25-51
    • Chan, L.M.1    Lowes, S.2    Hirst, B.H.3
  • 6
    • 68949103975 scopus 로고    scopus 로고
    • Cytochrome P450-mediated metabolism in the human gut wall
    • Thelen, K.; Dressman J. B. Cytochrome P450-mediated metabolism in the human gut wall. J. Pharm. Pharmacol., 2009, 61, 541-558.
    • (2009) J. Pharm. Pharmacol. , vol.61 , pp. 541-558
    • Thelen, K.1    Dressman, J.B.2
  • 7
    • 16444374977 scopus 로고    scopus 로고
    • Differentiation of organ availability by sequential and simultaneous analyses: Intestinal conjugative metabolism impacts on intestinal availability in humans
    • Mizuma, T.; Kawashima K.; Sakai S.; Sakaguchi S.; Hayashi M. Differentiation of organ availability by sequential and simultaneous analyses: intestinal conjugative metabolism impacts on intestinal availability in humans. J. Pharm. Sci., 2005, 94, 571-5.
    • (2005) J. Pharm. Sci. , vol.94 , pp. 571-575
    • Mizuma, T.1    Kawashima, K.2    Sakai, S.3    Sakaguchi, S.4    Hayashi, M.5
  • 8
    • 0023422908 scopus 로고
    • Review: First-pass metabolism by the gastrointestinal mucosa
    • Back, D. J.; Rogers S. M. Review: first-pass metabolism by the gastrointestinal mucosa. Aliment. Pharmacol. Ther., 1987, 1, 339-57.
    • (1987) Aliment. Pharmacol. Ther. , vol.1 , pp. 339-357
    • Back, D.J.1    Rogers, S.M.2
  • 10
    • 28044457103 scopus 로고    scopus 로고
    • Functional interactions between P-glycoprotein and CYP3A in drug metabolism
    • Christians, U.; Schmitz V.; Haschke M. Functional interactions between P-glycoprotein and CYP3A in drug metabolism. Expert Opin. Drug Metab. Toxicol., 2005, 1, 641-54.
    • (2005) Expert Opin. Drug Metab. Toxicol. , vol.1 , pp. 641-654
    • Christians, U.1    Schmitz, V.2    Haschke, M.3
  • 12
    • 80052002510 scopus 로고    scopus 로고
    • Physiologically-based pharmacokinetic modeling of intestinal first-pass metabolism of CYP3A substrates with high intestinal extraction
    • Gertz, M.; Houston J. B.; Galetin A. Physiologically-based pharmacokinetic modeling of intestinal first-pass metabolism of CYP3A substrates with high intestinal extraction. Drug Metab. Dispos., 2011, 39(9), 1633-42.
    • (2011) Drug Metab. Dispos. , vol.39 , Issue.9 , pp. 1633-1642
    • Gertz, M.1    Houston, J.B.2    Galetin, A.3
  • 13
    • 77953777072 scopus 로고    scopus 로고
    • Quantitative prediction of intestinal metabolism in humans from a simplified intestinal availability model and empirical scaling factor
    • Kadono, K.; Akabane T.; Tabata K.; Gato K.; Terashita S.; Teramura T. Quantitative prediction of intestinal metabolism in humans from a simplified intestinal availability model and empirical scaling factor. Drug Metab. Dispos., 2010, 38, 1230-7.
    • (2010) Drug Metab. Dispos. , vol.38 , pp. 1230-1237
    • Kadono, K.1    Akabane, T.2    Tabata, K.3    Gato, K.4    Terashita, S.5    Teramura, T.6
  • 14
  • 16
    • 17644380257 scopus 로고    scopus 로고
    • Predicting drug disposition via application of BCS: Transport/absorption/ elimination interplay and development of a biopharmaceutics drug disposition classification system
    • Wu, C. Y.; Benet L. Z. Predicting drug disposition via application of BCS: transport/absorption/elimination interplay and development of a biopharmaceutics drug disposition classification system. Pharm. Res., 2005, 22, 11-23.
    • (2005) Pharm. Res. , vol.22 , pp. 11-23
    • Wu, C.Y.1    Benet, L.Z.2
  • 19
  • 21
    • 79955783384 scopus 로고    scopus 로고
    • A critical analysis of the interplay between cytochrome P450 3A and P-glycoprotein: Recent insights from knockout and transgenic mice
    • van Waterschoot, R. A.; Schinkel A. H. A Critical Analysis of the Interplay between Cytochrome P450 3A and P-Glycoprotein: Recent Insights from Knockout and Transgenic Mice. Pharmacol. Rev., 2011, 63, 390-410.
    • (2011) Pharmacol. Rev. , vol.63 , pp. 390-410
    • Van Waterschoot, R.A.1    Schinkel, A.H.2
  • 22
    • 80053471751 scopus 로고    scopus 로고
    • In silico, in vitro and in situ models to assess interplay between CYP3A and P-gp
    • Mudra, D. R.; Desai P. V.; Desino K. E. In silico, In vitro and In situ Models to Assess Interplay Between CYP3A and P-gp. Curr. Drug Metab., 2011, 12, 750-73.
    • (2011) Curr. Drug Metab. , vol.12 , pp. 750-773
    • Mudra, D.R.1    Desai, P.V.2    Desino, K.E.3
  • 23
    • 0345866819 scopus 로고    scopus 로고
    • CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: Studies with sirolimus and midazolam
    • Cummins, C. L.; Jacobsen W.; Christians U.; Benet L. Z. CYP3A4-transfected Caco-2 cells as a tool for understanding biochemical absorption barriers: studies with sirolimus and midazolam. J. Pharmacol. Exp. Ther., 2004, 308, 143-55.
    • (2004) J. Pharmacol. Exp. Ther. , vol.308 , pp. 143-155
    • Cummins, C.L.1    Jacobsen, W.2    Christians, U.3    Benet, L.Z.4
  • 24
    • 0037382316 scopus 로고    scopus 로고
    • In vivo modulation of intestinal CYP3A metabolism by P-glycoprotein: Studies using the rat single-pass intestinal perfusion model
    • Cummins, C. L.; Salphati L.; Reid M. J.; Benet L. Z. In vivo modulation of intestinal CYP3A metabolism by P-glycoprotein: studies using the rat single-pass intestinal perfusion model. J. Pharmacol. Exp. Ther., 2003, 305, 306-14.
    • (2003) J. Pharmacol. Exp. Ther. , vol.305 , pp. 306-314
    • Cummins, C.L.1    Salphati, L.2    Reid, M.J.3    Benet, L.Z.4
  • 25
    • 71949106600 scopus 로고    scopus 로고
    • The drug transporter-metabolism alliance: Uncovering and defining the interplay
    • Benet, L. Z. The drug transporter-metabolism alliance: uncovering and defining the interplay. Mol. Pharm., 2009, 6, 1631-43.
    • (2009) Mol. Pharm. , vol.6 , pp. 1631-1643
    • Benet, L.Z.1
  • 26
    • 84871271046 scopus 로고    scopus 로고
    • Pharmacokinetic interplay of phase II metabolism and transport: A theoretical study
    • Wu, B. Pharmacokinetic interplay of phase II metabolism and transport: A theoretical study. J. Pharm. Sci., 2011.
    • (2011) J. Pharm. Sci.
    • Wu, B.1
  • 28
    • 24944529235 scopus 로고    scopus 로고
    • Coupling of conjugating enzymes and efflux transporters: Impact on bioavailability and drug interactions
    • Jeong, E. J.; Liu X.; Jia X.; Chen J.; Hu M. Coupling of conjugating enzymes and efflux transporters: impact on bioavailability and drug interactions. Curr. Drug Metab., 2005, 6, 455-68.
    • (2005) Curr. Drug Metab. , vol.6 , pp. 455-468
    • Jeong, E.J.1    Liu, X.2    Jia, X.3    Chen, J.4    Hu, M.5
  • 29
    • 38749138848 scopus 로고    scopus 로고
    • Product inhibition of UDP-glucuronosyltransferase (UGT) enzymes by UDP obfuscates the inhibitory effects of UGT substrates
    • Fujiwara, R.; Nakajima M.; Yamanaka H.; Katoh M.; Yokoi T. Product inhibition of UDP-glucuronosyltransferase (UGT) enzymes by UDP obfuscates the inhibitory effects of UGT substrates. Drug Metab. Dispos., 2008, 36, 361-7.
    • (2008) Drug Metab. Dispos. , vol.36 , pp. 361-367
    • Fujiwara, R.1    Nakajima, M.2    Yamanaka, H.3    Katoh, M.4    Yokoi, T.5
  • 30
    • 1842536833 scopus 로고    scopus 로고
    • Human udpglucuronosyltransferases: Isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid
    • Uchaipichat, V.; Mackenzie P. I.; Guo X. H.; Gardner-Stephen D.; Galetin A.; Houston J. B.; Miners J. O. Human udpglucuronosyltransferases: isoform selectivity and kinetics of 4-methylumbelliferone and 1-naphthol glucuronidation, effects of organic solvents, and inhibition by diclofenac and probenecid. Drug Metab. Dispos., 2004, 32, 413-23.
    • (2004) Drug Metab. Dispos. , vol.32 , pp. 413-423
    • Uchaipichat, V.1    Mackenzie, P.I.2    Guo, X.H.3    Gardner-Stephen, D.4    Galetin, A.5    Houston, J.B.6    Miners, J.O.7
  • 31
    • 70449535545 scopus 로고    scopus 로고
    • Caco-2 cell monolayers as a tool to study simultaneous phase II metabolism and metabolite efflux of indomethacin, paracetamol and 1-naphthol
    • Siissalo, S.; Laine L.; Tolonen A.; Kaukonen A. M.; Finel M.; Hirvonen J. Caco-2 cell monolayers as a tool to study simultaneous phase II metabolism and metabolite efflux of indomethacin, paracetamol and 1-naphthol. Int. J. Pharm., 2010, 383, 24-29.
    • (2010) Int. J. Pharm. , vol.383 , pp. 24-29
    • Siissalo, S.1    Laine, L.2    Tolonen, A.3    Kaukonen, A.M.4    Finel, M.5    Hirvonen, J.6
  • 32
    • 81855173545 scopus 로고    scopus 로고
    • Raloxifene glucuronidation in human intestine, kidney and liver microsomes and in human liver microsomes genotyped for the UGT1A1*28 polymorphism
    • Epub ahead of Print
    • Trdan Lusin, T.; Trontelj J.; Mrhar A. Raloxifene Glucuronidation in Human Intestine, Kidney and Liver Microsomes and in Human Liver Microsomes Genotyped for the UGT1A1*28 Polymorphism. Drug Metab. Dispos., 2011. [Epub ahead of Print].
    • (2011) Drug Metab. Dispos.
    • Trdan Lusin, T.1    Trontelj, J.2    Mrhar, A.3
  • 33
    • 78649660582 scopus 로고    scopus 로고
    • HIV protease inhibitors: Garlic supplements and first-pass intestinal metabolism impact on the therapeutic efficacy
    • Berginc, K.; Trdan T.; Trontelj J.; Kristl A. HIV protease inhibitors: garlic supplements and first-pass intestinal metabolism impact on the therapeutic efficacy. Biopharm Drug Dispos., 2010, 31, 495-505.
    • (2010) Biopharm Drug Dispos. , vol.31 , pp. 495-505
    • Berginc, K.1    Trdan, T.2    Trontelj, J.3    Kristl, A.4
  • 35
    • 33646490425 scopus 로고    scopus 로고
    • New technologies for assessing UDP-glucuronosyltransferase (UGT) metabolism in drug discovery and development
    • Patten, C. J. New technologies for assessing UDP-glucuronosyltransferase (UGT) metabolism in drug discovery and development. Drug Discov. Today Technol, 2006, 3, 73-78.
    • (2006) Drug Discov. Today Technol , vol.3 , pp. 73-78
    • Patten, C.J.1
  • 36
    • 0033674502 scopus 로고    scopus 로고
    • Comparison between cytochrome P450 (CYP) content and relative activity approaches to scaling from cDNA-expressed cyps to human liver microsomes: Ratios of accessory proteins as sources of discrepancies between the approaches
    • Venkatakrishnan, K.; von Moltke L. L.; Court M. H.; Harmatz J. S.; Crespi C. L.; Greenblatt D. J. Comparison between Cytochrome P450 (CYP) Content and Relative Activity Approaches to Scaling from cDNA-Expressed CYPs to Human Liver Microsomes: Ratios of Accessory Proteins as Sources of Discrepancies between the Approaches. Drug Metab. Dispos., 2000, 28, 1493-1504.
    • (2000) Drug Metab. Dispos. , vol.28 , pp. 1493-1504
    • Venkatakrishnan, K.1    Von Moltke, L.L.2    Court, M.H.3    Harmatz, J.S.4    Crespi, C.L.5    Greenblatt, D.J.6
  • 37
    • 0027242397 scopus 로고
    • Validation and use of cloned, expressed human drug-metabolizing enzymes in heterologous cells for analysis of drug metabolism and drug-drug interactions
    • Remmel, R. P.; Burchell B. Validation and use of cloned, expressed human drug-metabolizing enzymes in heterologous cells for analysis of drug metabolism and drug-drug interactions. Biochem. Pharmacol, 1993, 46, 559-566.
    • (1993) Biochem. Pharmacol , vol.46 , pp. 559-566
    • Remmel, R.P.1    Burchell, B.2
  • 38
    • 1542344547 scopus 로고    scopus 로고
    • Predicting drug clearance from recombinantly expressed CYPs: Intersystem extrapolation factors
    • Proctor, N. J.; Tucker G. T.; Rostami-Hodjegan A. Predicting drug clearance from recombinantly expressed CYPs: intersystem extrapolation factors. Xenobiotica, 2004, 34, 151-78.
    • (2004) Xenobiotica , vol.34 , pp. 151-178
    • Proctor, N.J.1    Tucker, G.T.2    Rostami-Hodjegan, A.3
  • 40
    • 61649118149 scopus 로고    scopus 로고
    • Development of an optimized procedure for the preparation of rat intestinal microsomes: Comparison of hepatic and intestinal microsomal cytochrome P450 enzyme activities in two rat strains
    • Bruyere, A.; Decleves X.; Bouzom F.; Proust L.; Martinet M.; Walther B.; Parmentier Y. Development of an optimized procedure for the preparation of rat intestinal microsomes: comparison of hepatic and intestinal microsomal cytochrome P450 enzyme activities in two rat strains. Xenobiotica, 2009, 39, 22-32.
    • (2009) Xenobiotica , vol.39 , pp. 22-32
    • Bruyere, A.1    Decleves, X.2    Bouzom, F.3    Proust, L.4    Martinet, M.5    Walther, B.6    Parmentier, Y.7
  • 41
    • 33747599176 scopus 로고    scopus 로고
    • Intestinal and hepatic metabolic activity of five cytochrome P450 enzymes: Impact on prediction of firstpass metabolism
    • Galetin, A.; Houston J. B. Intestinal and hepatic metabolic activity of five cytochrome P450 enzymes: impact on prediction of firstpass metabolism. J. Pharmacol. Exp. Ther., 2006, 318, 1220-9.
    • (2006) J. Pharmacol. Exp. Ther. , vol.318 , pp. 1220-1229
    • Galetin, A.1    Houston, J.B.2
  • 42
    • 33746295389 scopus 로고    scopus 로고
    • Interspecies comparison of 7-hydroxycoumarin glucuronidation and sulfation in liver S9 fractions
    • Wang, Q.; Ye C.; Jia R.; Owen A. J.; Hidalgo I. J.; Li J. Interspecies comparison of 7-hydroxycoumarin glucuronidation and sulfation in liver S9 fractions. In vitro Cell Dev. Biol. Anim., 2006, 42, 8-12.
    • (2006) Vitro Cell Dev. Biol. Anim. , vol.42 , pp. 8-12
    • Wang, Q.1    Ye, C.2    Jia, R.3    Owen, A.J.4    Hidalgo, I.J.5    Li, J.6
  • 43
    • 0034807892 scopus 로고    scopus 로고
    • Optimizing drug development: Strategies to assess drug metabolism/transporter interaction potential-toward a consensus
    • Tucker, G. T.; Houston J. B.; Huang S. M. Optimizing drug development: strategies to assess drug metabolism/transporter interaction potential-toward a consensus. Pharm. Res., 2001, 18, 1071-80.
    • (2001) Pharm. Res. , vol.18 , pp. 1071-1080
    • Tucker, G.T.1    Houston, J.B.2    Huang, S.M.3
  • 44
    • 0026768856 scopus 로고
    • Transport properties of P-glycoprotein in plasma membrane vesicles from multidrug-resistant Chinese hamster ovary cells
    • Doige, C. A.; Sharom F. J. Transport properties of P-glycoprotein in plasma membrane vesicles from multidrug-resistant Chinese hamster ovary cells. Biochim. Biophys. Acta., 1992, 1109, 161-71.
    • (1992) Biochim. Biophys. Acta. , vol.1109 , pp. 161-171
    • Doige, C.A.1    Sharom, F.J.2
  • 45
    • 0026722467 scopus 로고
    • Expression of the human multidrug resistance cDNA in insect cells generates a high activity drug-stimulated membrane ATPase
    • Sarkadi, B.; Price E. M.; Boucher R. C.; Germann U. A.; Scarborough G. A. Expression of the human multidrug resistance cDNA in insect cells generates a high activity drug-stimulated membrane ATPase. J. Biol. Chem., 1992, 267, 4854-4858.
    • (1992) J. Biol. Chem. , vol.267 , pp. 4854-4858
    • Sarkadi, B.1    Price, E.M.2    Boucher, R.C.3    Germann, U.A.4    Scarborough, G.A.5
  • 49
    • 81855183743 scopus 로고    scopus 로고
    • Development of a highly sensitive method using LC-MRM to quantify membrane P-glycoprotein in biological matrices and relationship to transport function
    • Miliotis, T.; Ali L.; Palm J. E.; Lundqvist A. J.; Ahnoff M.; Andersson T. B.; Hilgendorf C. Development of a Highly Sensitive Method using LC-MRM to Quantify Membrane P-glycoprotein in Biological Matrices and Relationship to Transport Function. Drug Metab. Dispos., 2011, 39, 2440-2449.
    • (2011) Drug Metab. Dispos. , vol.39 , pp. 2440-2449
    • Miliotis, T.1    Ali, L.2    Palm, J.E.3    Lundqvist, A.J.4    Ahnoff, M.5    Andersson, T.B.6    Hilgendorf, C.7
  • 50
    • 77954078835 scopus 로고    scopus 로고
    • Differences in the expression of endogenous efflux transporters in MDR1-transfected versus wildtype cell lines affect P-glycoprotein mediated drug transport
    • Kuteykin-Teplyakov, K.; Luna-Tortos C.; Ambroziak K.; Loscher W. Differences in the expression of endogenous efflux transporters in MDR1-transfected versus wildtype cell lines affect P-glycoprotein mediated drug transport. Br. J. Pharmacol., 2010, 160, 1453-63.
    • (2010) Br. J. Pharmacol. , vol.160 , pp. 1453-1463
    • Kuteykin-Teplyakov, K.1    Luna-Tortos, C.2    Ambroziak, K.3    Loscher, W.4
  • 51
    • 0345299165 scopus 로고    scopus 로고
    • Drug resistance and ATP-dependent conjugate transport mediated by the apical multidrug resistance protein, MRP2, permanently expressed in human and canine cells
    • Cui, Y.; Konig J.; Buchholz J. K.; Spring H.; Leier I.; Keppler D. Drug resistance and ATP-dependent conjugate transport mediated by the apical multidrug resistance protein, MRP2, permanently expressed in human and canine cells. Mol. Pharmacol., 1999, 55, 929-37.
    • (1999) Mol. Pharmacol. , vol.55 , pp. 929-937
    • Cui, Y.1    Konig, J.2    Buchholz, J.K.3    Spring, H.4    Leier, I.5    Keppler, D.6
  • 52
    • 0013508682 scopus 로고
    • A retrovirus carrying an MDR1 cDNA confers multidrug resistance and polarized expression of P-glycoprotein in MDCK cells
    • Pastan, I.; Gottesman M. M.; Ueda K.; Lovelace E.; Rutherford A. V.; Willingham M. C. A retrovirus carrying an MDR1 cDNA confers multidrug resistance and polarized expression of P-glycoprotein in MDCK cells. Proc. Nat. Acad. Sci. USA, 1988, 85, 4486-90.
    • (1988) Proc. Nat. Acad. Sci. USA , vol.85 , pp. 4486-4490
    • Pastan, I.1    Gottesman, M.M.2    Ueda, K.3    Lovelace, E.4    Rutherford, A.V.5    Willingham, M.C.6
  • 53
    • 0035668339 scopus 로고    scopus 로고
    • Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein
    • Adachi, Y.; Suzuki H.; Sugiyama Y. Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-glycoprotein. Pharm. Res., 2001, 18, 1660-1668.
    • (2001) Pharm. Res. , vol.18 , pp. 1660-1668
    • Adachi, Y.1    Suzuki, H.2    Sugiyama, Y.3
  • 54
    • 0033407050 scopus 로고    scopus 로고
    • Expression of multidrug resistance protein-3 (multispecific organic anion transporter-D) in human embryonic kidney 293 cells confers resistance to anticancer agents
    • Zeng, H.; Bain L. J.; Belinsky M. G.; Kruh G. D. Expression of multidrug resistance protein-3 (multispecific organic anion transporter-D) in human embryonic kidney 293 cells confers resistance to anticancer agents. Cancer Res., 1999, 59, 5964-7.
    • (1999) Cancer Res. , vol.59 , pp. 5964-5967
    • Zeng, H.1    Bain, L.J.2    Belinsky, M.G.3    Kruh, G.D.4
  • 55
    • 27144464932 scopus 로고    scopus 로고
    • Effect of the modulation of the membrane lipid composition on the localization and function of P-glycoprotein in MDR1-MDCK cells
    • Kamau, S.; Krämer S.; Günthert M.; Wunderli-Allenspach H. Effect of the modulation of the membrane lipid composition on the localization and function of P-glycoprotein in MDR1-MDCK cells. In vitro Cell Dev. Biol. Anim., 2005, 41, 207-216.
    • (2005) Vitro Cell Dev. Biol. Anim. , vol.41 , pp. 207-216
    • Kamau, S.1    Krämer, S.2    Günthert, M.3    Wunderli-Allenspach, H.4
  • 56
    • 0025102678 scopus 로고
    • Thse use of cultured epithelial and endothelial cells for drug transport and metabolism studies
    • Audus, K. L.; Bartel R. L.; Hidalgo I. J.; Borchardt R. T. Thse use of cultured epithelial and endothelial cells for drug transport and metabolism studies. Pharm. Res., 1990, 7, 435-51.
    • (1990) Pharm. Res. , vol.7 , pp. 435-451
    • Audus, K.L.1    Bartel, R.L.2    Hidalgo, I.J.3    Borchardt, R.T.4
  • 57
    • 38449084547 scopus 로고    scopus 로고
    • Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers
    • Hubatsch, I.; Ragnarsson E. G.; Artursson P. Determination of drug permeability and prediction of drug absorption in Caco-2 monolayers. Nat. Protoc., 2007, 2, 2111-2119.
    • (2007) Nat. Protoc. , vol.2 , pp. 2111-2119
    • Hubatsch, I.1    Ragnarsson, E.G.2    Artursson, P.3
  • 58
    • 33747090656 scopus 로고    scopus 로고
    • Variability in mRNA expression of ABC-and SLC-transporters in human intestinal cells: Comparison between human segments and Caco-2 cells
    • Seithel, A.; Karlsson J.; Hilgendorf C.; Bjorquist A.; Ungell A. L. Variability in mRNA expression of ABC-and SLC-transporters in human intestinal cells: comparison between human segments and Caco-2 cells. Eur. J. Pharm. Sci., 2006, 28, 291-299.
    • (2006) Eur. J. Pharm. Sci. , vol.28 , pp. 291-299
    • Seithel, A.1    Karlsson, J.2    Hilgendorf, C.3    Bjorquist, A.4    Ungell, A.L.5
  • 59
    • 54349123557 scopus 로고    scopus 로고
    • The expression of most UDP-glucuronosyltransferases (UGTs) is increased significantly during Caco-2 cell differentiation, whereas UGT1A6 is highly expressed also in undifferentiated cells
    • Siissalo, S.; Zhang H.; Stilgenbauer E.; Kaukonen A. M.; Hirvonen J.; Finel M. The expression of most UDP-glucuronosyltransferases (UGTs) is increased significantly during Caco-2 cell differentiation, whereas UGT1A6 is highly expressed also in undifferentiated cells. Drug Metab. Dispos., 2008, 36, 2331-6.
    • (2008) Drug Metab. Dispos. , vol.36 , pp. 2331-2336
    • Siissalo, S.1    Zhang, H.2    Stilgenbauer, E.3    Kaukonen, A.M.4    Hirvonen, J.5    Finel, M.6
  • 60
    • 0036805724 scopus 로고    scopus 로고
    • Comparison of human duodenum and Caco-2 gene expression profiles for 12, 000 gene sequences tags and correlation with permeability of 26 drugs
    • Sun, D.; Lennernas H.; Welage L. S.; Barnett J. L.; Landowski C. P.; Foster D.; Fleisher D.; Lee K. D.; Amidon G. L. Comparison of human duodenum and Caco-2 gene expression profiles for 12, 000 gene sequences tags and correlation with permeability of 26 drugs. Pharm. Res., 2002, 19, 1400-16.
    • (2002) Pharm. Res. , vol.19 , pp. 1400-1416
    • Sun, D.1    Lennernas, H.2    Welage, L.S.3    Barnett, J.L.4    Landowski, C.P.5    Foster, D.6    Fleisher, D.7    Lee, K.D.8    Amidon, G.L.9
  • 61
    • 38749138122 scopus 로고    scopus 로고
    • Sulfotransferase forms expressed in human intestinal Caco-2 and TC7 cells at varying stages of differentiation and role in benzo [a]pyrene metabolism
    • Meinl, W.; Ebert B.; Glatt H.; Lampen A. Sulfotransferase forms expressed in human intestinal Caco-2 and TC7 cells at varying stages of differentiation and role in benzo [a]pyrene metabolism. Drug Metab. Dispos., 2008, 36, 276-83.
    • (2008) Drug Metab. Dispos. , vol.36 , pp. 276-283
    • Meinl, W.1    Ebert, B.2    Glatt, H.3    Lampen, A.4
  • 62
    • 20044371666 scopus 로고    scopus 로고
    • The Caco-2 cell line as a model of the intestinal barrier: Influence of cell and culture-related factors on Caco-2 cell functional characteristics
    • Sambuy, Y.; De Angelis I.; Ranaldi G.; Scarino M. L.; Stammati A.; Zucco F. The Caco-2 cell line as a model of the intestinal barrier: influence of cell and culture-related factors on Caco-2 cell functional characteristics. Cell Biol. Toxicol., 2005, 21, 1-26.
    • (2005) Cell Biol. Toxicol. , vol.21 , pp. 1-26
    • Sambuy, Y.1    De Angelis, I.2    Ranaldi, G.3    Scarino, M.L.4    Stammati, A.5    Zucco, F.6
  • 63
    • 0030945754 scopus 로고    scopus 로고
    • Expression of enzymatically active CYP3A4 by Caco-2 cells grown on extracellular matrix-coated permeable supports in the presence of 1alpha, 25-dihydroxyvitamin D3
    • Schmiedlin-Ren, P.; Thummel K. E.; Fisher J. M.; Paine M. F.; Lown K. S.; Watkins P. B. Expression of enzymatically active CYP3A4 by Caco-2 cells grown on extracellular matrix-coated permeable supports in the presence of 1alpha, 25-dihydroxyvitamin D3. Mol. Pharmacol., 1997, 51, 741-54.
    • (1997) Mol. Pharmacol. , vol.51 , pp. 741-754
    • Schmiedlin-Ren, P.1    Thummel, K.E.2    Fisher, J.M.3    Paine, M.F.4    Lown, K.S.5    Watkins, P.B.6
  • 71
    • 19344364551 scopus 로고    scopus 로고
    • Correlation of in vitro cytotoxicity with paracellular permeability in Caco-2 cells
    • Konsoula, R.; Barile F. A. Correlation of in vitro cytotoxicity with paracellular permeability in Caco-2 cells. Toxicol. In vitro, 2005, 19, 675-84.
    • (2005) Toxicol. In Vitro , vol.19 , pp. 675-684
    • Konsoula, R.1    Barile, F.A.2
  • 73
    • 0037457790 scopus 로고    scopus 로고
    • In vitro and in vivo models for assessing drug efflux transporter activity
    • Zhang, Y.; Bachmeier C.; Miller D. W. In vitro and in vivo models for assessing drug efflux transporter activity. Adv. Drug Deliv. Rev., 2003, 55, 31-51.
    • (2003) Adv. Drug Deliv. Rev. , vol.55 , pp. 31-51
    • Zhang, Y.1    Bachmeier, C.2    Miller, D.W.3
  • 74
    • 0029558244 scopus 로고
    • A biophysical model of passive and polarized active transport processes in Caco-2 cells: Approaches to uncoupling apical and basolateral membrane events in the intact cell
    • Ho, N. F.; Burton P. S.; Conradi R. A.; Barsuhn C. L. A biophysical model of passive and polarized active transport processes in Caco-2 cells: approaches to uncoupling apical and basolateral membrane events in the intact cell. J. Pharm. Sci., 1995, 84, 21-27.
    • (1995) J. Pharm. Sci. , vol.84 , pp. 21-27
    • Ho, N.F.1    Burton, P.S.2    Conradi, R.A.3    Barsuhn, C.L.4
  • 76
    • 79955064061 scopus 로고    scopus 로고
    • Pancreatoduodenectomy as a source of human small intestine for Ussing chamber investigations and comparative studies with rat tissue
    • Haslam, I. S.; O'Reilly D. A.; Sherlock D. J.; Kauser A.; Womack C.; Coleman T. Pancreatoduodenectomy as a source of human small intestine for Ussing chamber investigations and comparative studies with rat tissue. Biopharm. Drug Dispos., 2011, 32, 210-21.
    • (2011) Biopharm. Drug Dispos. , vol.32 , pp. 210-221
    • Haslam, I.S.1    O'Reilly, D.A.2    Sherlock, D.J.3    Kauser, A.4    Womack, C.5    Coleman, T.6
  • 77
    • 0014561779 scopus 로고
    • Organ culture of mucosal biopsies of human small intestine
    • Browning, T. H.; Trier J. S. Organ culture of mucosal biopsies of human small intestine. J. Clin. Invest., 1969, 48, 1423-32.
    • (1969) J. Clin. Invest. , vol.48 , pp. 1423-1432
    • Browning, T.H.1    Trier, J.S.2
  • 79
    • 6544259277 scopus 로고
    • The use of sacs of everted small intestine for the study of the transference of substances from the mucosal to the serosal surface
    • Wilson, T. H.; Wiseman G. The use of sacs of everted small intestine for the study of the transference of substances from the mucosal to the serosal surface. J. Physiol., 1954, 123, 116-25.
    • (1954) J. Physiol. , vol.123 , pp. 116-125
    • Wilson, T.H.1    Wiseman, G.2
  • 81
    • 40849104960 scopus 로고    scopus 로고
    • Induction of metabolism and transport in human intestine: Validation of precision-cut slices as a tool to study induction of drug metabolism in human intestine in vitro
    • van de Kerkhof, E. G.; de Graaf I. A. M.; Ungell A.-L. B.; Groothuis G. M. M. Induction of Metabolism and Transport in Human Intestine: Validation of Precision-Cut Slices as a Tool to Study Induction of Drug Metabolism in Human Intestine in vitro. Drug Metab. Dispos., 2008, 36, 604-613.
    • (2008) Drug Metab. Dispos. , vol.36 , pp. 604-613
    • Van De Kerkhof, E.G.1    De Graaf, I.A.M.2    Ungell, B.A.-L.3    Groothuis, G.M.M.4
  • 82
    • 79960175548 scopus 로고    scopus 로고
    • In vivo-in vitro-in silico pharmacokinetic modelling in drug development: Current status and future directions
    • Pelkonen, O.; Turpeinen M.; Raunio H. In vivo-In vitro-In Silico Pharmacokinetic Modelling in Drug Development: Current Status and Future Directions. Clin. Pharmacokinet., 2011, 50, 483-491.
    • (2011) Clin. Pharmacokinet. , vol.50 , pp. 483-491
    • Pelkonen, O.1    Turpeinen, M.2    Raunio, H.3
  • 83
    • 77953737073 scopus 로고    scopus 로고
    • Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data
    • Gertz, M.; Harrison A.; Houston J. B.; Galetin A. Prediction of human intestinal first-pass metabolism of 25 CYP3A substrates from in vitro clearance and permeability data. Drug Metab. Dispos., 2010, 38, 1147-58.
    • (2010) Drug Metab. Dispos. , vol.38 , pp. 1147-1158
    • Gertz, M.1    Harrison, A.2    Houston, J.B.3    Galetin, A.4
  • 85
    • 84855219592 scopus 로고    scopus 로고
    • Prediction of the intestinal first-pass metabolism of CYP3A and UGT substrates in humans from in vitro data
    • Nishimuta, H.; Sato K.; Yabuki M.; Komuro S. Prediction of the intestinal first-pass metabolism of CYP3A and UGT substrates in humans from in vitro data. Drug Metab. Pharmacokinet., 2011, 26(6), 592-601.
    • (2011) Drug Metab. Pharmacokinet. , vol.26 , Issue.6 , pp. 592-601
    • Nishimuta, H.1    Sato, K.2    Yabuki, M.3    Komuro, S.4
  • 86
    • 58149164868 scopus 로고    scopus 로고
    • In vitro-in vivo correlation in p-glycoprotein mediated transport in intestinal absorption
    • Del Amo, E. M.; Heikkinen A. T.; Mönkkönen J. In vitro-in vivo correlation in p-glycoprotein mediated transport in intestinal absorption. Eur. J. Pharm. Sci., 2009, 36, 200-211.
    • (2009) Eur. J. Pharm. Sci. , vol.36 , pp. 200-211
    • Del Amo, E.M.1    Heikkinen, A.T.2    Mönkkönen, J.3
  • 87
    • 68249144520 scopus 로고    scopus 로고
    • Simulations of the nonlinear dose dependence for substrates of influx and efflux transporters in the human intestine
    • Bolger, M. B.; Lukacova V.; Woltosz W. S. Simulations of the Nonlinear Dose Dependence for Substrates of Influx and Efflux Transporters in the Human Intestine. AAPS. J., 2009, 11, 353-363.
    • (2009) AAPS. J. , vol.11 , pp. 353-363
    • Bolger, M.B.1    Lukacova, V.2    Woltosz, W.S.3
  • 88
    • 73949146951 scopus 로고    scopus 로고
    • Physiologically based predictions of the impact of inhibition of intestinal and hepatic metabolism on human pharmacokinetics of CYP3A substrates
    • Fenneteau, F.; Poulin P.; Nekka F. Physiologically based predictions of the impact of inhibition of intestinal and hepatic metabolism on human pharmacokinetics of CYP3A substrates. J. Pharm. Sci., 2010, 99, 486-514.
    • (2010) J. Pharm. Sci. , vol.99 , pp. 486-514
    • Fenneteau, F.1    Poulin, P.2    Nekka, F.3
  • 90
    • 43049114146 scopus 로고    scopus 로고
    • Quantitative atlas of membrane transporter proteins: Development and application of a highly sensitive simultaneous LC/MS/MS method combined with novel in-silico peptide selection criteria
    • Kamiie, J.; Ohtsuki S.; Iwase R.; Ohmine K.; Katsukura Y.; Yanai K.; Sekine Y.; Uchida Y.; Ito S.; Terasaki T. Quantitative atlas of membrane transporter proteins: development and application of a highly sensitive simultaneous LC/MS/MS method combined with novel in-silico peptide selection criteria. Pharm. Res., 2008, 25, 1469-83.
    • (2008) Pharm. Res. , vol.25 , pp. 1469-1483
    • Kamiie, J.1    Ohtsuki, S.2    Iwase, R.3    Ohmine, K.4    Katsukura, Y.5    Yanai, K.6    Sekine, Y.7    Uchida, Y.8    Ito, S.9    Terasaki, T.10
  • 91
    • 78650054715 scopus 로고    scopus 로고
    • Simultaneous absolute quantification of 11 cytochrome P450 isoforms in human liver microsomes by liquid chromatography tandem mass spectrometry with in silico target peptide selection
    • Kawakami, H.; Ohtsuki S.; Kamiie J.; Suzuki T.; Abe T.; Terasaki T. Simultaneous absolute quantification of 11 cytochrome P450 isoforms in human liver microsomes by liquid chromatography tandem mass spectrometry with in silico target peptide selection. J. Pharm. Sci., 2010, 100, 341-52.
    • (2010) J. Pharm. Sci. , vol.100 , pp. 341-352
    • Kawakami, H.1    Ohtsuki, S.2    Kamiie, J.3    Suzuki, T.4    Abe, T.5    Terasaki, T.6
  • 92
    • 80054792485 scopus 로고    scopus 로고
    • Blood-Brain Barrier (BBB) pharmacoproteomics (PPx): Reconstruction of in vivo brain distribution of 11 P-glycoprotein substrates based on the BBB transporter protein concentration, in vitro intrinsic transport activity, and unbound fraction in plasma and brain in mice
    • Epub ahead of Print
    • Uchida, Y.; Ohtsuki S.; Kamiie J.; Terasaki T. Blood-Brain Barrier (BBB) Pharmacoproteomics (PPx): Reconstruction of In vivo Brain Distribution of 11 P-glycoprotein Substrates based on the BBB Transporter Protein Concentration, In vitro Intrinsic Transport Activity, and Unbound Fraction in Plasma and Brain in Mice. J. Pharmacol. Exp. Ther., 2011. [Epub ahead of Print].
    • (2011) J. Pharmacol. Exp. Ther.
    • Uchida, Y.1    Ohtsuki, S.2    Kamiie, J.3    Terasaki, T.4
  • 93
    • 77957344287 scopus 로고    scopus 로고
    • Prediction of human metabolic clearance from in vitro systems: Retrospective analysis and prospective view
    • Hallifax, D.; Foster J. A.; Houston J. B. Prediction of human metabolic clearance from in vitro systems: retrospective analysis and prospective view. Pharm. Res., 2010, 27, 2150-61.
    • (2010) Pharm. Res. , vol.27 , pp. 2150-2161
    • Hallifax, D.1    Foster, J.A.2    Houston, J.B.3
  • 94
    • 77950562355 scopus 로고    scopus 로고
    • Effects of experimental setup on the apparent concentration dependency of active efflux transport in in vitro cell permeation experiments
    • Heikkinen, A. T.; Korjamo T.; Lepikkö V.; Mönkkönen J. Effects of Experimental Setup on the Apparent Concentration Dependency of Active Efflux Transport in in vitro Cell Permeation Experiments. Mol. Pharm., 2010, 7, 605-617.
    • (2010) Mol. Pharm. , vol.7 , pp. 605-617
    • Heikkinen, A.T.1    Korjamo, T.2    Lepikkö, V.3    Mönkkönen, J.4
  • 96
    • 44349185775 scopus 로고    scopus 로고
    • A catenary model to study transport and conjugation of baicalein, a bioactive flavonoid, in the Caco-2 cell monolayer: Demonstration of substrate inhibition
    • Sun, H.; Zhang L.; Chow E. C.; Lin G.; Zuo Z.; Pang K. S. A catenary model to study transport and conjugation of baicalein, a bioactive flavonoid, in the Caco-2 cell monolayer: demonstration of substrate inhibition. J. Pharmacol. Exp. Ther., 2008, 326, 117-126.
    • (2008) J. Pharmacol. Exp. Ther. , vol.326 , pp. 117-126
    • Sun, H.1    Zhang, L.2    Chow, E.C.3    Lin, G.4    Zuo, Z.5    Pang, K.S.6
  • 97
    • 25144511902 scopus 로고    scopus 로고
    • The steadystate Michaelis-Menten analysis of P-glycoprotein mediated transport through a confluent cell monolayer cannot predict the correct Michaelis constant Km
    • Bentz, J.; Tran T. T.; Polli J. W.; Ayrton A.; Ellens H. The steadystate Michaelis-Menten analysis of P-glycoprotein mediated transport through a confluent cell monolayer cannot predict the correct Michaelis constant Km. Pharm. Res., 2005, 22, 1667-1677.
    • (2005) Pharm. Res. , vol.22 , pp. 1667-1677
    • Bentz, J.1    Tran, T.T.2    Polli, J.W.3    Ayrton, A.4    Ellens, H.5
  • 98
    • 77149142588 scopus 로고    scopus 로고
    • Modelling of drug disposition kinetics in in vitro intestinal absorption cell models
    • Heikkinen, A. T.; Korjamo T.; Mönkkönen J. Modelling of Drug Disposition Kinetics in In vitro Intestinal Absorption Cell Models. Basic Clin. Pharmacol. Toxicol., 2010, 106, 180-188.
    • (2010) Basic Clin. Pharmacol. Toxicol. , vol.106 , pp. 180-188
    • Heikkinen, A.T.1    Korjamo, T.2    Mönkkönen, J.3
  • 99
    • 71949116668 scopus 로고    scopus 로고
    • Mechanistic modeling of hepatic transport from cells to whole body: Application to napsagatran and fexofenadine
    • Poirier, A.; Funk C.; Scherrmann J. M.; Lave T. Mechanistic modeling of hepatic transport from cells to whole body: application to napsagatran and fexofenadine. Mol. Pharm., 2009, 6, 1716-33.
    • (2009) Mol. Pharm. , vol.6 , pp. 1716-1733
    • Poirier, A.1    Funk, C.2    Scherrmann, J.M.3    Lave, T.4
  • 100
    • 0037336533 scopus 로고    scopus 로고
    • Prediction of the oral absorption of low-permeability drugs using small intestine-like 2/4/A1 cell monolayers
    • Tavelin, S.; Taipalensuu J.; Soderberg L.; Morrison R.; Chong S.; Artursson P. Prediction of the oral absorption of low-permeability drugs using small intestine-like 2/4/A1 cell monolayers. Pharm. Res., 2003, 20, 397-405.
    • (2003) Pharm. Res. , vol.20 , pp. 397-405
    • Tavelin, S.1    Taipalensuu, J.2    Soderberg, L.3    Morrison, R.4    Chong, S.5    Artursson, P.6
  • 101
    • 77955914314 scopus 로고    scopus 로고
    • Preparation and incubation of precision-cut liver and intestinal slices for application in drug metabolism and toxicity studies
    • de Graaf, I. A.; Olinga P.; de Jager M. H.; Merema M. T.; de Kanter R.; van de Kerkhof E. G.; Groothuis G. M. Preparation and incubation of precision-cut liver and intestinal slices for application in drug metabolism and toxicity studies. Nat. Protoc., 2010, 5, 1540-51.
    • (2010) Nat. Protoc. , vol.5 , pp. 1540-1551
    • De Graaf, I.A.1    Olinga, P.2    De Jager, M.H.3    Merema, M.T.4    De Kanter, R.5    Van De Kerkhof, E.G.6    Groothuis, G.M.7


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