P-Glycoprotein (P-gp) Mediated Efflux in Caco-2 Cell Monolayers: The Influence of Culturing Conditions and Drug Exposure on P-gp Expression Levels
References and Notes (22)
- et al.
Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. Kinetics of vinblastine secretion and interaction with modulators
J. Biol. Chem.
(1993) - et al.
Transepithelial transport of drugs by the multidrug transporter in cultured Madin-Darby canine kidney cell epithelia
J. Biol. Chem.
(1989) - et al.
Evidence for a polarized efflux system for peptides in the apical membrane of Caco-2 cells
Biochem. Biophys. Res. Commun.
(1993) - et al.
Role of P-glycoprotein in dolastatin 10 resistance
Biochem. Pharmacol.
(1994) - et al.
Polarized transport of docetaxel and vinblastine mediated by P-glycoprotein in human intestinal epithelial cell monolayers
Biochem. Pharmacol.
(1994) - et al.
A second groEL-like gene, organized in a groESL operon is present in the genome of Synechocystis sp. PCC 6803
J. Biol. Chem.
(1993) - et al.
Possible involvement of multiple P-glycoprotein-mediated efflux systems in the transport of verapamil and other organic cations across rat intestine
Pharm. Res.
(1995) - et al.
Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers
Pharm. Res.
(1993) - et al.
Transport of Daunomycin in Caco-2 cells. What is the contribution of the mdr-1-gene product to the transepithelial fluxes
H. Presented at the 13th European Intestinal Transport Group (EITG) Congress
(1996) - et al.
M.; Ziemniak J.; Artursson, P. Transport of celiprolol across human intestinal epithelial (Caco-2) cells. Mediation of secretion by multiple transporters including P-glycoprotein. Brit. J
Pharmacol
(1993)
Evidence for intestinal secretion as an additional clearance pathway of talinolol enantiomers. concentration- and dose-dependent absorption in vitro and in vivo. Pharm
Res
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Cytotoxicity and intestinal permeability of phycotoxins assessed by the human Caco-2 cell model
2023, Ecotoxicology and Environmental SafetyCitation Excerpt :For example, the tight junctions of the Caco-2 cell monolayers are markedly stronger than those of the human intestine, resulting in poor penetration of water-soluble chemicals into Caco-2 monolayers (Artursson et al., 2001). In addition, overexpression of P-glycoprotein in the Caco-2 cell model may increase the secretion rate and thus indirectly decrease cellular uptake (Anderle et al., 1998). To improve the overall performance of the Caco-2 cell model, the establishment of co-culture cell models such as Caco-2 cells with mucus-secreting HT29 cells, M-cells and enteric glial cells (EGC) has been gradually developed to mimic the human intestine (Wu et al., 2019; Reale et al., 2021a, 2021b; Cabellos et al., 2017).
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Department of Pharmacy, ETH.
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Institute of Biomedical Engineering, ETH.
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Genentech.
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Martin Luther University.
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Astra Hassle AB, 43183 Mölndal, Sweden.