A functional assay for quantitation of the apparent affinities of ligands of P-glycoprotein in Caco-2 cells

Pharmaceutical Research

Volumn 18, Issue 2, 2001, Pages 171-176

  Gao, Jinnian ^a   Murase, Osamu ^a   Schowen, Richard L ^a   Aubé, Jeffrey ^a   Borchardt, Ronald T ^a  

^a UNIVERSITY OF KANSAS   (United States)

Author keywords

Apparent affinity; Caco 2 cells; Michaelis Menten constant; P glycoprotein; Transport

Indexed keywords

CELIPROLOL; CYCLOSPORIN A; DAUNORUBICIN; DOXORUBICIN; ETOPOSIDE; GLYCOPROTEIN P; PACLITAXEL; QUINIDINE; VINBLASTINE;

ARTICLE; BINDING AFFINITY; BINDING SITE; CELL STRAIN CACO 2; CLINICAL PROTOCOL; DRUG DETERMINATION; HUMAN; HUMAN CELL; LIGAND BINDING; LIQUID SCINTILLATION COUNTING; MOLECULAR INTERACTION; PRIORITY JOURNAL; QUANTITATIVE ASSAY; TRANSPORT KINETICS;

ANTINEOPLASTIC AGENTS, PHYTOGENIC; BIOLOGICAL TRANSPORT; BIOLOGICAL TRANSPORT, ACTIVE; CACO-2 CELLS; DRUG INTERACTIONS; HUMANS; LIGANDS; MODELS, THEORETICAL; P-GLYCOPROTEIN; PACLITAXEL; TRITIUM;

EID: 0034960419     PISSN: 07248741     EISSN: None     Source Type: Journal    
DOI: 10.1023/A:1011076217118     Document Type: Article

References (28)

1. Functional expression of P-glycoprotein in apical membranes of human intestinal Caco-2 cells. Kinetics of vinblastine secretion and interaction with modulators
2. Intestinal secretion of drugs. The role of P-glycoprotein and related drug efflux systems in limiting oral drug absorption
3. Drug absorption limited by P-glycoprotein-mediated secretory drug transport in human intestinal epithelial Caco-2 cell layers
4. P-glycoprotein: A defense mechanism limiting oral bioavailability and CNS accumulation of drugs
5. Hepatobiliary elimination of cationic drugs: The role of P-glycoproteins and other ATP-dependent transporters
6. Role of blood-brain barrier P-glycoprotein in limiting brain accumulation and sedative side-effects of asimadoline, a peripherally acting analgaesic drug
7. Role of P-glycoprotein in drug disposition
8. Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor
9. P-glycoprotein system as a determinant of drug interactions: The case of digoxin-verapamil
10. The contribution of P-glycoprotein to pharmacokinetic drug-drug interactions
11. Taxol: Mechanisms of action and resistance
12. 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
13. Taxol transport by human intestinal epithelial Caco-2 cells
14. Transepithelial transport of vinblastine by kidney-derived cell lines. Application of a new kinetic model to estimate in situ KM of the pump
15. Transport of celiprolol across human intestinal epithelial (Caco-2) cells: Mediation of secretion by multiple transporters including P-glycoprotein
16. Radioligand-binding assay employing P-glycoprotein-overexpressing cells: Testing drug affinities to the secretory intestinal multidrug transporter
17. Use of membrane vesicles to investigate drug interactions with transporter proteins, P-glycoprotein and multidrug resistance-associated protein
18. Development of an immobilized P-glycoprotein stationary phase for online liquid chromatographic determination of drug-binding affinities
19. Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability
20. Metabolism, uptake, and transepithelial transport of Val-Val-Val in the human intestinal cell line, Caco-2
21. Reversal mechanism of multidrug resistance by verapamil: Direct binding of verapamil to P-glycoprotein on specific sites and transport of verapamil outward across the plasma membrane of K562/ADM cells
22. Probenecid reverses multidrug resistance in multidrug resistance-associated protein-overexpressing HL60/AR and H69/AR cells but not in P-glycoprotein-overexpressing HL60/Tax and P388/ADR cells
23. Interaction of bioactive hydrophobic peptides with the human multidrug transporter
24. Kinetics of daunorubicin transport by P-glycoprotein of intact cancer cells
25. Characterization of the regional intestinal kinetics of drug efflux in rat and human intestine and in Caco-2 cells
26. Positively cooperative sites for drug transport by P-glycoprotein with distinct drug specificities
27. Stimulation of P-glycoprotein-mediated drug transport by prazosin and progesterone. Evidence for a third drug-binding site
28. Characterization of binding properties to human P-glycoprotein: Development of a [3H]verapamil radioligand-binding assay