Are MDCK cells transfected with the human MDR1 gene a good model of the human intestinal mucosa?

Pharmaceutical Research

Volumn 19, Issue 6, 2002, Pages 765-772

  Tang, Fuxing ^a,b   Horie, Kazutoshi ^a   Borchardt, Ronald T ^a  

^a UNIVERSITY OF KANSAS   (United States)

^b FOREST RESEARCH INSTITUTE   (United States)

Author keywords

Caco 2; Kinetics; MDCK MDR1; P glycoprotein; Transporter

Indexed keywords

CARBON 14; CYCLOSPORIN A; DAUNORUBICIN; DIGOXIN; ELACRIDAR; ETOPOSIDE; GLYCOPROTEIN P; MANNITOL; PROBENECID; QUINIDINE; RESERPINE; TRITIUM; VERAPAMIL; VINBLASTINE; VINCRISTINE;

ANIMAL CELL; ARTICLE; CELL STRAIN CACO 2; DRUG DELIVERY SYSTEM; DRUG TRANSPORT; GENETIC TRANSFECTION; HUMAN; HUMAN CELL; INTESTINE ABSORPTION; INTESTINE MUCOSA; KIDNEY CELL; MICHAELIS CONSTANT; MONOLAYER CULTURE; MULTIDRUG RESISTANCE; NONHUMAN; PRIORITY JOURNAL;

ANIMALS; CACO-2 CELLS; CELL LINE; DIGOXIN; DOGS; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG EVALUATION, PRECLINICAL; GENES, MDR; HUMANS; INTESTINAL MUCOSA; P-GLYCOPROTEIN; TRANSFECTION;

EID: 0036293772     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1016140429238     Document Type: Article

References (52)

1. Caco-2 monolayers in experimental and theoretical predictions of drug transport
2. The application of cell culture systems in drug discovery and development
3. The use of the intestinal epithelial cell culture model, Caco-2, in pharmaceutical development
4. Intestinal drug absorption and metabolism in cell cultures: Caco-2 and beyond
5. Association of intestinal peptide transport with a protein related to the cadherin superfamily
6. Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. Kinetics of vinblastine secretion and interaction with modulators
7. Active secretion and enterocytic drug metabolism barriers to drug absorption
8. Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery
9. Characterization of the human MDR3 P-glycoprotein and its recognition by P-glycoprotein-specific monoclonal antibodies
10. A surface glycoprotein modulating drug permeability in Chinese hamster ovary cell mutants
11. Multidrug resistance and the role of P-glycoprotein knockout mice
12. Age-dependent expression of P-glycoprotein gp170 in Caco-2 cell monolayers
13. Transport of the flavonoid chrysin and its conjugated metabolites by the human intestinal cell line Caco-2
14. Evidence for a polarized efflux system for peptides in the apical membrane of Caco-2 cells
15. P-Glycoprotein (P-gp) mediated efflux in Caco-2 cell monolayers: The influence of culturing conditions and drug exposure on P-gp expression levels
16. Characterization of the efflux transporter(s) responsible for restricting intestinal mucosa permeation of a coumarinic acid-based cyclic prodrug of the opioid peptide DADLE
17. The Madin Darby canine kidney (MDCK) epithelial cell monolayer as a model cellular transport barrier
18. MDCK (Madin-Darby canine kidney) cells: A tool for membrane permeability screening
19. Transport of glutathione prostaglandin A conjugates by the multidrug resistance protein 1
20. The multidrug resistance protein family
21. P-Glycoprotein in cell cultures: A combined approach to study expression, localisation, and functionality in the confocal microscope
22. Active transport of the angiotensin-II antagonist losartan and its main metabolite EXP 3174 across MDCK-MDR1 and caco- 2 cell monolayers
23. A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco- 2 cells
24. Transport of digoxin into brain microvessels and choroid plexuses isolated from guinea pig
25. Normal viability and altered pharmacokinetics in mice lacking mdr1-type (drug-transporting) P-glycoproteins
26. Effect of PSC 833, a P-glycoprotein modulator, on the disposition of vincristine and digoxin in rats
27. Effects of a potent and specific P-glycoprotein inhibitor on the blood-brain barrier distribution and antinociceptive effect of morphine in the rat
28. Dose-dependent pharmacokinetics of cyclosporin A in rats: Events in tissues
29. Availability of PSC833, a substrate and inhibitor of P-glycoproteins, in various concentrations of serum
30. Expression of the apical conjugate export pump, Mrp2, in the polarized hepatoma cell line, WIF-B
31. MDR 1 activation is the predominant resistance mechanism selected by vinblastine in MES-SA cells
32. Disruption of the mouse mdr1a P-glycoprotein gene leads to a deficiency in the blood-brain barrier and to increased sensitivity to drugs
33. Multidrug-resistance phenotype in Chinese hamster ovary cells
34. Basolateral localization and export activity of the human multidrug resistance-associated protein in polarized pig kidney cells
35. In vitro and in vivo reversal of multidrug resistance by GF 120918, an acridonecarboxamide derivative
36. Reversal of resistance by GF120918 in cell lines expressing the ABC half-transporter, MXR
37. Sorting of newly synthesized galactosphingolipids to the two surface domains of epithelial cells
38. Epithelial sphingolipid sorting allows for extensive variation of the fatty acyl chain and the sphingosine backbone
39. Two strains of the Madin-Darby canine kidney (MDCK) cell line have distinct glycosphingolipid compositions
40. Characterization of the ATPase activity of P-glycoprotein from multidrug-resistant Chinese hamster ovary cells
41. The functional purification of P-glycoprotein is dependent on maintenance of a lipid-protein interface
42. Analysis of the tangled relationships between P-glycoprotein-mediated multidrug resistance and the lipid phase of the cell membrane
43. Interaction of P-glycoprotein with defined phospholipid bilayers: A differential scanning calorimetric study
44. The membrane lipid environment modulates drug interactions with the P- glycoprotein multidrug transporter
45. P-glycoprotein-mediated Hoechst 33342 transport out of the lipid bilayer
46. Photosensitized labeling of a functional multidrug transporter in living drug-resistant tumor cells
47. Unidirectional fluxes of rhodamine 123 in multidrug-resistant cells: Evidence against direct drug extrusion from the plasma membrane
48. Kinetic evidence suggesting that the multidrug transporter differentially handles influx and efflux of its substrates
49. Relationship between expression level of P-glycoprotein and daunorubicin transport in LLC-PK1 cells transfected with human MDR1 gene
50. Partitioning of local anesthetics into membranes: Surface charge effects monitored by the phospholipid head-group