A method for the simultaneous evaluation of the activities of seven major human drug-metabolizing cytochrome P450s using an in vitro cocktail of probe substrates and fast gradient liquid chromatography tandem mass spectrometry

Drug Metabolism and Disposition

Volumn 29, Issue 1, 2001, Pages 23-29

  Dierks, Elizabeth A ^b   Stams, Karen R ^b   Lim, Heng Keang ^b   Cornelius, Georgia ^b   Zhang, Honglu ^b   Ball, Simon E ^a,b  

^a BRISTOL MYERS SQUIBB PHARMACEUTICAL RESEARCH INSTITUTE   (United States)

^b PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

BUFURALOL; COUMARIN; CYTOCHROME P450 ISOENZYME; DICLOFENAC; ETHOXYRESORUFIN; FURAFYLLINE; KETOCONAZOLE; MEPHENYTOIN; METHOXSALEN; MIDAZOLAM; PACLITAXEL; QUERCETIN; QUINIDINE; SULFAPHENAZOLE; TRANYLCYPROMINE;

ARTICLE; ENZYME ACTIVITY; ENZYME ANALYSIS; ENZYME SUBSTRATE; ESCHERICHIA COLI; LIQUID CHROMATOGRAPHY; NONHUMAN; PRIORITY JOURNAL; TANDEM MASS SPECTROMETRY;

CHROMATOGRAPHY, LIQUID; CYTOCHROME P-450 ENZYME SYSTEM; DRUG EVALUATION, PRECLINICAL; HUMANS; MASS SPECTROMETRY; SUBSTRATE SPECIFICITY;

EID: 0035157254     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (37)

1. Application of a genetic fast gradient liquid chromatography tandem mass spectrometry method for the analysis of cytochrome P450 probe substrates
2. Ketoconazole and sulphaphenazole as the respective selective inhibitors of P4503A and 2C9
3. Venlafaxine: In vitro inhibition of CYP2D6 dependent imipramine and desipramine metabolism; comparative studies with selected SSRIs, and effects on human hepatic CYP3A4, CYP2C9, and CYPIA2
4. Coexpression of a human P450 (CYP3A4) and P450 reductase generates a highly functional monooxygenase system in Escherichia coli
5. Cytochrome P450 isoform inhibitors as a tool for the investigation of metabolic reactions catalyzed by human liver microsomes
6. A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding
7. Potent inhibition of yeast-expressed CYP2D6 by dihydroquinidine, quinidine, and its metabolites
8. Microtiter plate assays for inhibition of human, drug-metabolizing cytochromes P450
9. Use of cDNA-expressed human cytochrome P450 enzymes to study potential drug-drug interactions
10. Differential selectivity of cytochrome P450 inhibitors against probe substrates in human and rat liver microsomes
11. In vitro forecasting of drugs which may interfere with the biotransformation of midazolam
12. Expression of modified human cytochrome-P450 3A4 in Escherichia coli and purification and reconstitution of the enzyme
13. Evaluation of the selectivitiy of in vitro probes and suitability of organic solvents for the measurement of human cytochrome P450 monooxygenase activities
14. Terfenadine-ketoconazole interaction: Pharmacokinetic and electrocardiographic consequences
15. Putative active site template model for cytochrome P4502C9 (tolbutamide hydroxylase)
16. Identification of amino acid substitutions that confer a high affinity for sulfaphenazole binding and a high catalytic efficiency for warfarin metabolism to P450 2C19
17. The role of CYP2D6 in primary and secondary oxidative metabolism of dextromethorphan: In vitro studies using human liver microsomes
18. Evaluation of omeprazole and lansoprazole as inhibitors of cytochrome P450 isoforms
19. Preparation and characterization of microsomal fractions for studies on xenobiotic metabolism
20. Competition between cytochrome P-450 isozymes for NADPH-cytochrome P-450 oxidoreductase affects drug metabolism
21. An improvement of the coomassie blue dye binding method allowing an equal sensitivity to various proteins: Application to cerebrospinal fluid
22. Diclofenac and its derivatives as tools for studying human cytochromes P450 active sites: Particular efficiency and regioselectivity of P450 2Cs
23. Interaction of sulfaphenazole derivatives with human liver cytochromes P450 2C: Molecular origin of the specific inhibitory effects of sulfaphenazole on CYP2C9 and consequences for the substrate binding site topology of CYP2C9
24. The role of CYP2C19 in the metabolism of (+/-) bufuralol, the prototypic substrate of CYP2D6
25. Heterologous expression and kinetic characterization of human cytochromes P-450: Validation of a pharmaceutical tool for drug metabolism research
26. Fully automated analysis of activities catalysed by the major human liver cytochrome P450 (CYP) enzymes: Assessment of human CYP inhibition potential
27. Cytochrome P450 inhibitors. Evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes
28. The carbon monoxide binding pigment of liver microsomes
29. Specificity of substrate and inhibitor probes for cytochrome P450s: Evaluation of in vitro metabolism using cDNA-expressed human P450s and human liver microsomes
30. Inhibition of human hepatic and placental xenobiotic monooxygenases by imidazole antimycotics
31. Inhibitor panel studies of human hepatic and placental cytochrome P-450 associated monooxygenase activities
32. Understanding consequences of concurrent therapies
33. Functional co-expression of CYP2D6 and human NADPH-cytochrome P450 reductase in Escherichia coli
34. A general strategy for the expression of recombinant human cytochrome P450s in Escherichia coli using bacterial signal peptides: Expression of CYP3A4, CYP2A6, and CYP2E1
35. Selective biotransformation of Taxol to 6α-hydroxytaxol by human cytochrome P450 2C8
36. Inhibition of cytochrome P-450 activity in rat liver microsomes by the naturally occurring flavonoid, quercetin
37. CYP2C19 participates in tolbutamide hydroxylation by human liver microsomes