Rational use of in vitro P-glycoprotein assays in drug discovery

Journal of Pharmacology and Experimental Therapeutics

Volumn 299, Issue 2, 2001, Pages 620-628

  Polli, Joseph W ^a   Wring, Stephen A ^a   Humphreys, Joan E ^a   Huang, Liyue ^a   Morgan, Jonathon B ^a   Webster, Lindsey O ^a   Serabjit Singh, Cosette S ^a  

^a GLAXOSMITHKLINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ADENOSINE TRIPHOSPHATASE; CALCEIN; GLYCOPROTEIN P;

ARTICLE; BINDING AFFINITY; ENZYME ACTIVITY; LIQUID CHROMATOGRAPHY; MEMBRANE PERMEABILITY; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN DETERMINATION; TANDEM MASS SPECTROMETRY;

ADENOSINE TRIPHOSPHATASES; ANIMALS; CELLS, CULTURED; CHROMATOGRAPHY, LIQUID; ENZYME INHIBITORS; FLUORESCEINS; FLUORESCENT DYES; HUMANS; MASS SPECTROMETRY; P-GLYCOPROTEIN; PHARMACOLOGY; SPODOPTERA;

EID: 0034763005     PISSN: 00223565     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (24)

1. Reversal of multidrug resistance derivatives of acrivastine: A study of structure-activity relationships of P-glycoprotein inhibitors in vitro and in vivo
2. Drug export activity of the human canalicular multispecific organic anion transporter in polarized kidney MDCK cells expressing cMOAT (MRP2) cDNA
3. The role of passive transbilayer drug movement in multidrug resistance and its modulation
4. Analysis of the tangled relationships between P-glycoprotein-mediated multidrug resistance and the lipid phase of the cell membrane
5. P-glycoprotein A defense mechanism limiting oral bioavailability and CNS accumulation of drugs
6. The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors
7. Influence of passive permeability on apparent P-glycoprotein kinetics
8. Microfluorometric evaluation of calcein acetoxymethyl ester as a probe for P-glycoprotein-mediated resistance: Effects of cyclosporin A and its nonimmunosuppressive analogue SDZ PSC 833
9. Structure-activity relationships of P-glycoprotein interacting drugs: Kinetic characterization of their effects on ATPase activity
10. Role of intestinal P-glycoprotein (mdr1) in interpatient variation in the oral bioavailability of cyclosporine
11. Characterization of the major metabolites of verapamil as substrates and inhibitors of P-glycoprotein
12. Comparison of MDCK and bovine brain endothelial cells (BBECs) as a blood-brain barrier screen
13. Role of P-glycoprotein on the CNS disposition of amprenavir (141W94), an HIV protease inhibitor
14. P-glycoprotein substrates and antagonists cluster into two distinct groups
15. Drug-stimulated ATPase activity of the human P-glycoprotein
16. P-glycoprotein, a gatekeeper in the blood-brain barrier
17. Structure-activity relationship studies of propafenone analogs based on P-glycoprotein ATPase activity measurements
18. P-glycoprotein inhibitor erythromycin increases oral bioavailability of talinolol in humans
19. A general pattern for substrate recognition of P-glycoprotein
20. The P-glycoprotein efflux pump: How does it transport drugs?
21. Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine
22. Ranking of P-glycoprotein substrates and inhibitors by calcein-AM fluorometry screening assay
23. P-glycoprotein system as a determinant of drug interactions: The case of digoxin-verapamil
24. Automated dual LC/MS/MS with cassette analysis markedly increases throughput and accelerates drug discovery