Cytochrome P450 fluorometric substrates: Identification of isoform-selective probes for rat CYP2D2 and human CYP3A4

Drug Metabolism and Disposition

Volumn 30, Issue 7, 2002, Pages 845-852

  Stresser, David M ^a   Turner, Stephanie D ^a   Blanchard, Andrew P ^a   Miller, Vaughn P ^a   Crespi, Charles L ^a  

^a BD Biosciences   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

3 [2 (N,N DIETHYL N METHYLAMINO)ETHYL] 7 METHOXY 4 METHYLCOUMARIN; 3 [2 (N,N DIETHYL N METHYLAMINO)ETHYL] 7 METHOXY 4 TRIFLUOROMETHYLCOUMARIN; 3 CYANO 7 ETHOXYCOUMARIN; 3 CYANO 7 METHOXYCOUMARIN; 7 BENZYLOXY 4 TRIFLUOROMETHYLCOUMARIN; 7 BENZYLOXYQUINOLINE; 7 METHOXY 4 TRIFLUOROMETHYLCOUMARIN; BENZYLOXYRESORUFIN; COUMARIN DERIVATIVE; CYTOCHROME P450; CYTOCHROME P450 2D2; CYTOCHROME P450 3A4; FLUORESCEIN; QUINOLINE DERIVATIVE; UNCLASSIFIED DRUG; CYP2D2 PROTEIN, RAT; CYP3A PROTEIN, HUMAN; CYP3A4 PROTEIN, HUMAN; FLUORESCENT DYE; ISOENZYME; UNSPECIFIC MONOOXYGENASE;

ARTICLE; CORRELATION ANALYSIS; DEALKYLATION; DEMETHYLATION; DRUG METABOLISM; ENZYME ACTIVE SITE; ENZYME ACTIVITY; ENZYME KINETICS; ENZYME SPECIFICITY; FLUOROMETRY; HUMAN; LIVER MICROSOME; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; REACTION ANALYSIS; SIGNAL TRANSDUCTION; ANIMAL; CATALYSIS; CHEMISTRY; ENZYMOLOGY; FEMALE; MALE; METABOLISM; PHYSIOLOGY; RAT; SPRAGUE DAWLEY RAT;

ANIMAL; ARYL HYDROCARBON HYDROXYLASES; CATALYSIS; CYTOCHROME P-450 ENZYME SYSTEM; FEMALE; FLUORESCENT DYES; HUMAN; ISOENZYMES; MALE; MICROSOMES, LIVER; RATS; RATS, SPRAGUE-DAWLEY; SUBSTRATE SPECIFICITY; ANIMALS; HUMANS;

AGOUTI;

EID: 0035987896     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: 10.1124/dmd.30.7.845     Document Type: Article

References (27)

1. Cytochrome P450 isoform inhibitors as a tool for the investigation of metabolic reactions catalyzed by human liver microsomes
2. Ethoxypentoxy- and benzyloxyphenoxazones and homologues: A series of substrates to distinguish between different induced cytochromes P-450
3. Cytochrome P450 specificities of alkoxyresorufin O-dealkylation in human and rat liver
4. A highly sensitive tool for the assay of cytochrome P450 enzyme activity in rat, dog and man. Direct fluorescence monitoring of the deethylation of 7-ethoxy-4-trifluoromethylcoumarin
5. The use of 3-[2-(N,N-diethyl-N-methylammonium)ethyl]-7-methoxy-4-methylcoumarin (AMMC) as a specific CYP2D6 probe in human liver microsomes
6. Description of a 96-well plate assay to measure cytochrome P4503A inhibition in human liver microsomes using a selective fluorescent probe
7. Microtiter plate assays for inhibition of human, drug-metabolizing cytochromes P450
8. High throughput screening for inhibition of cytochrome P450 metabolism
9. A direct, highly sensitive assay for cytochrome P-450 catalyzed O-deethylation using a novel coumarin analog
10. Debrisoquine 4-hydroxylase: Characterization of a new P450 gene subfamily, regulation, chromosomal mapping and molecular analysis of the DA rat polymorphism
11. In vitro-in vivo scaling of CYP kinetic data not consistent with the classical Michaelis-Menten model
12. Genomic cloning and protein expression of a novel rat brain cytochrome P-450 CYP2DI8 catalyzing imipramine N-demethylation
13. Simultaneous measurement of cytochrome P4501A catalytic activity and total protein concentration with a fluorescence plate reader
14. The rat P450 IID subfamily: Complete sequences of four closely linked genes and evidence that gene conversions maintained sequence homogeneity at the heme-binding region of the cytochrome P450 active site
15. The CYP2D gene subfamily: Analysis of the molecular basis of the debrisoquine 4-hydroxylase deficiency in DA rats
16. 7-Alkoxyquinolines: New fluorescent substrates for cytochrome P450 monooxygenases
17. Design, synthesis and characterization of 7-methoxy-4-(aminomethyl)coumarin as a novel and selective cytochrome P450 2D6 substrate suitable for high-throughput screening
18. CYP isoform induction screening in 96-well plates: Use of 7-benzyloxy-4-trifluoromethylcoumarin as a substrate for studies with rat hepatocytes
19. Metabolism of 2,5- bis(trifluoromethyl)-7-benzyloxy-4-trifluoromethylcoumarin by human hepatic CYP isoforms: Evidence for selectivity towards CYP3A4
20. Metabolism of 7-benzyloxy-4-trifluoromethyl-coumarin by human hepatic cytochrome P450 isoforms
21. Expression and characterization of canine cytochrome P450 2D15
22. Polymorphic debrisoquine 4-hydroxylase activity in the rat is due to differences in CYP2D2 expression
23. Substrate-dependent modulation of CYP3A4 catalytic activity: Analysis of 27 test compounds with four fluorometric substrates
24. The O-dealkylation of 7-ethoxycoumarin by liver microsomes. A direct fluorometric test
25. A continuous fluorometric assay for cytochrome P-450-dependent mixed function oxidases using 3-cyano-7-ethoxycoumarin
26. Molecular basis of the Dark Agouti rat drug oxidation polymorphism: Importance of CYP2DI and CYP2D2