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Reversal of P-glycoprotein-mediated multidrug resistance by a potent cyclopropyldibenzosuberane modulator, LY335979.
Overexpression of P-glycoprotein (Pgp) by tumors results in multidrug resistance (MDR) to structurally unrelated oncolytics. MDR cells may be sensitized to these oncolytics when treated with a PgpExpand
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Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities.
Overexpression of ATP-dependent drug efflux pumps, P-glycoprotein (Pgp) or multidrug resistance-associated protein (MRP), confers multidrug resistance to tumor cells. Modulators of multidrugExpand
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The multidrug resistance protein 5 (ABCC5) confers resistance to 5-fluorouracil and transports its monophosphorylated metabolites
5′-Fluorouracil (5-FU), used in the treatment of colon and breast cancers, is converted intracellularly to 5′-fluoro-2′-deoxyuridine (5-FUdR) by thymidine phosphorylase and is subsequentlyExpand
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Three-dimensional quantitative structure-activity relationships of inhibitors of P-glycoprotein.
P-glycoprotein (P-gp) is an efflux transporter involved in limiting the oral bioavailability and tissue penetration of a variety of structurally divergent molecules. A better understanding of theExpand
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Uptake of the cephalosporin, cephalexin, by a dipeptide transport carrier in the human intestinal cell line, Caco-2.
The transport of the orally absorbed cephalosporin, cephalexin, was examined in the human epithelial cell line, Caco-2 that possesses intestinal enterocyte-like properties when cultured. InExpand
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Application of three-dimensional quantitative structure-activity relationships of P-glycoprotein inhibitors and substrates.
Using in vitro data, we previously built Catalyst 3-dimensional quantitative structure activity relationship (3D-QSAR) models that qualitatively rank and predict IC(50) values for P-glycoproteinExpand
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Modulation of P‐glycoprotein but not MRP1‐ or BCRP‐mediated drug resistance by LY335979
Our study examines the ability of LY335979 (Zosuquidar trihydrochloride) to modulate 3 distinct ABC transporters that are mechanisms of drug resistance: P‐glycoprotein (Pgp, ABCB1), multidrugExpand
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Considerations in the design and development of transport inhibitors as adjuncts to drug therapy.
With the realization of the importance of drug efflux transporters in disease processes and treatment, development of inhibitors to these transporters has been sought for use as adjuncts to therapy.Expand
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Mechanism and Kinetics of Transcellular Transport of a New β-Lactam Antibiotic Loracarbef Across an Intestinal Epithelial Membrane Model System (Caco-2)
Various processes involved in the transcellular transport (TT) of loracarbef (LOR) were studied in the Caco-2 cell monolayer, a cell culture model of the small intestinal epithelium. The resultsExpand
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Association of intestinal peptide transport with a protein related to the cadherin superfamily.
The first step in oral absorption of many medically important peptide-based drugs is mediated by an intestinal proton-dependent peptide transporter. This transporter facilitates the oral absorptionExpand
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