Cytochrome P450 in vitro reaction phenotyping: A re-evaluation of approaches used for P450 isoform identification

Drug Metabolism and Disposition

Volumn 31, Issue 4, 2003, Pages 345-350

  Lu, Anthony Y H ^a   Wang, Regina W ^b   Lin, Jiunn H ^b  

^a RUTGERS UNIVERSITY   (United States)

^b MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

4 HYDROXYDEBRISOQUINE; ACYLTRANSFERASE; AMINE OXIDASE (FLAVIN CONTAINING); AZAMULIN; BUFURALOL; CYTOCHROME P450; CYTOCHROME P450 1A1; CYTOCHROME P450 2D6; CYTOCHROME P450 INHIBITOR; CYTOCHROME P450 ISOENZYME; DEBRISOQUINE; DIMETHYLANILINE MONOOXYGENASE; DRUG METABOLITE; EPOXIDE HYDROLASE; GLUCURONOSYLTRANSFERASE; GLUTATHIONE TRANSFERASE; LOSARTAN; MARKER; MEPHENYTOIN; METHYLTRANSFERASE; MONOCLONAL ANTIBODY; PHENANTHRENE; PLEUROMUTILIN; POLYCLONAL ANTIBODY; PYRROLE DERIVATIVE; QUINIDINE; RECOMBINANT ENZYME; SULFOTRANSFERASE; TAMOXIFEN; UNCLASSIFIED DRUG;

ANALYTIC METHOD; ANTIBODY BLOOD LEVEL; BIOTRANSFORMATION; CATALYSIS; CONCENTRATION RESPONSE; CORRELATION ANALYSIS; CROSS REACTION; DEMETHYLATION; DRUG CLEARANCE; DRUG INFORMATION; DRUG METABOLISM; DRUG SELECTIVITY; ENZYME ACTIVITY; ENZYME INHIBITION; EVALUATION; GENOTYPE; HOMOZYGOSITY; HUMAN; HYDROXYLATION; IN VITRO STUDY; IN VIVO STUDY; LIVER MICROSOME; NONHUMAN; PHENOTYPE; PRIORITY JOURNAL; PROTEIN ANALYSIS; PROTEIN EXPRESSION; PUBLICATION; RELIABILITY; REVIEW; TECHNIQUE; TITRIMETRY;

ANTIBODIES; BIOLOGICAL MARKERS; CYTOCHROME P-450 CYP1A1; CYTOCHROME P-450 CYP2D6; CYTOCHROME P-450 ENZYME SYSTEM; ENZYME INHIBITORS; HUMANS; ISOENZYMES; RECOMBINANT PROTEINS;

EID: 0037379318     PISSN: 00909556     EISSN: None     Source Type: Journal    
DOI: 10.1124/dmd.31.4.345     Document Type: Review

References (48)

1. Brosen K, Gram LF, Haghfelt T, and Bertisson L (1987) Extensive metabolizers of debrisoquine become poor metabolizers during quinidine treatment. Pharmacol Toxicol 60:312-314.
2. Burchell B, Brierley CH, and Rance D (1995) Specificity of human UDP-glucuronosyl-transferases and xenobiotic glucuronidation. Life Sci 20:1819-1831.
3. Crespi CL and Miller VP (1999) The use of heterologously expressed drug-metabolizing enzymes-state of the art and prospects for the future. Pharmacol Ther 84:121-131.
4. Crespi CL, Steimel DT, Penman BW, Korzekwa KR, Fernandez-Salguero P, Buters JTM, Gelboin HV, Gonzalez FJ, Idle JR and Daly AK (1995) Comparison of substrate metabolism by wild type CYP2D6 protein and a variant containing methionine, not valine, at position 374. Pharmacogenetics 5:234-243.
5. Crewe HK, Ellis W, Lennard MS, and Tucker GT (1997) Variable contribution of cytochrome P4502D6. 2C9 and 3A4 to the 4-hydroxylation of tamoxifen by human liver microsomes. Biochem Pharmacol 53:171-178.
6. Dahl ML (2002) Cytochrome P450 phenotyping/genotyping in patients receiving antipsychotics: Useful aid to prescribing? Clin Pharmacokinet 41:453-470.
7. Dahl ML, Johansson I, Bertilsson L, Ingelman-Sundberg M, and Sjoqvist F (1995) Ultrarapid hydroxylation of debrisoquine in a Swedish population: analysis of the molecular genetic basis. J Pharmacol Exp Ther 274:516-520.
8. Dalen P, Dahl ML, Eichelbaum M, Bertilsson L, and Wilkinson GR (1999) Disposition of debrisoquine in caucasians with different CYP2D6-genotypes including those with multiple genes. Pharmacogenetics 9:697-706.
9. Eichelbaum M and Gross AS (1990) The genetic polymorphism of debrisoquine/sparteine metabolism-clinical aspects. Pharmacol Ther 46:377-394.
10. Gelboin HV, Krausz KW, Gonzalez FJ, and Yang TJ (1999) Inhibitory monoclonal antibodies to human cytochrome P450 enzymes: a new avenue for drug discovery. Trends Pharmacol Sci 20:432-438.
11. Gelboin HV, Krausz KW, Shou M, Gonzalez FJ, and Yang TJ (1997) A monoclonal antibody inhibitory to human P450 2D6: a paradigm for use in combinatorial determination of individual P450 role in specific drug tissue metabolism. Pharmacogenetics 7:469-477.
12. Granvil CP, Krausz KW, Gelboin HV, Idle JR, and Gonzalez FJ (2002) 4-hydroxylation of debrisoquine by human CYP1A1 and its inhibition by quinidine and quinine. J Pharmacol Exp Ther 301:1025-1032.
13. Guengerich FP (1988) Oxidation of 17a-ethynylestradiol by human liver cytochrome P450. Mol Pharmacol 33:500-508.
14. Guengerich FP and Shimada T (1991) Oxidation of toxic and carcinogenic chemicals by human cytochrome P450 enzymes. Chem Res Toxicol 4:391-407.
15. Heyn H, White RB, and Stevens JC (1996) Catalytic role of cytochrome P4502B6 in the N-demethylation of S-mephenytoin. Drug Metab Dispos 24:948-954.
16. Idle JR and Smith RL (1979) Polymorphisms of oxidation at carbon centers of drugs and their clinical significance. Drug Metab Rev 9:301-317.
17. Karanam BV, Vincent SH, Newton DJ, Wang RW, and Chiu SHL (1994) FK506 metabolism in human liver microsomes: investigation of the involvement of cytochrome P450 isozymes other than CYP3A4. Drug Metab Dispos 22:811-814.
18. Krausz KW, Goldfarb I, Buters JTM, Yang TJ, Gonzalez FJ, and Gelboin HV (2001) Monoclonal antibodies specific and inhibitory to human cytochromes P450 2C8. 2C9 and 2C19. Drug Metab Dispos 29:1410-1423.
19. Kronbach T, Mathys D, Umeno M, Gonzalez FJ, and Meyer UA (1989) Oxidation of midazolam and triazolam by human liver cytochrome P4503A4. Mol Phannacol 36:89-96.
20. Lin JH and Lu AYH (1998) Inhibition and induction of cytochrome P450 and the clinical implications. Clin Pharmacokinet 35:361-390.
21. Madan A, Usuki E, Burton LA, Ogilvie BW, and Parkinson A (2001) In vitro approaches for studying the inhibition of drug-metabolizing enzymes and identifying the drug-metabolizing enzymes responsible for the metabolism of drugs, in "Drug-Drug Interactions" (Rodrigues AD ed) pp 217-294, Marcel Dekker, New York.
22. Mahgoub A, Idle JR, Dring LG, Lancaster R, and Smith RL (1977) Polymorphic hydroxylation of debrisoquine in man. Lancet 2:584-586.
23. m of the enzyme for bufuralol but not debrisoquine hydroxylation. J Biol Chem 265:17197-17201.
24. McCrea JB, Cribb A, Rushmore T, Osbome B, Gillen L, Lo MW, Waldman S, Bjomsson T, Spielberg S, and Goldberg MR (1999) Phenotypic and genotypic investigations of a healthy volunteer deficient in the conversion of losartan to its active metabolite EXP3174. Clin Pharmacol Ther 65:348-352.
25. Mei Q, Tang C, Assang C, Lin Y, Slaughter D, Rodrigues D, Baillie TA, Rushmore TH, and Shou M (1999) Role of a potent inhibitory monoclonal antibody to cytochrome P450 in assessment of human drug metabolism. J Pharmacol Exp Ther 291:749-759.
26. Meyer UA and Zanger UM (1997) Molecular mechanisms of genetic polymorphisms of drug metabolism. Annu Rev Pharmacol Toxicol 37:269-296.
27. Murray BP, Edwards RJ, Murray S, Singleton AM, Davies DS, and Boobis AR (1993) Human hepatic CYP1A1 ad CYP1A2 content, determined with specific anti-peptide antibodies, correlates with the mutagenic activation of PhIP. Carcinogenesis 14:585-592.
28. Newton DJ, Wang RW, and Lu AYH (1995) Cytochrome P450 inhibitors: evaluation of specificities in the in vitro metabolism of therapeutic agents by human liver microsomes. Drug Metab Dispos 23:154-158.
29. Pastrakuljic A, Tang BK, Roberts EA, and Kalow W (1997) Distinction of CYP1A1 and CYP1A2 activity by selective inhibition using fluvoxamine and isosafrole. Biochem Pharmacol 53:531-538.
30. Remmel RP (2001) Review of human UDP-glucuronosyltransferases and their role in drug-drug interactions, in "Drug-Drug Interactions" (Rodrigues AD ed) pp 89-114, Marcel Dekker, New York.
31. Rendic S (2002) Summary of information on human CYP enzymes: human P450 metabolism data. Drug Metab Rev 34:83-448.
32. Rodrigues AD (1999) Integrated cytochrome P450 reaction phenotyping: attempting to bridge the gap between cDNA-expressed cytochrome P450 and native human liver microsomes. Biochem Pharmacol 57:465-480.
33. Rodrigues AD, Roberts EM, Mulford DJ, Yao Y, and Ouellet D (1997) Oxidative metabolism of clarithromycin in the presence of human liver microsomes: major role for the cytochrome P4503A subfamily. Drug Metab Dispos 25:623-630.
34. Schweikl H, Taylor JA, Kitareewan S, Linko P, Nagorney D and Goldstein JA (1993) Expression of CYP1A1 and CYP1A2 genes in human liver. Pharmacogenetics 3:239-249.
35. Sloan TP, Lancaster R, Shah RR, Idle JR, and Smith RL (1983) Genetically determined oxidation capacity and the disposition of debrisoquine. Br J Clin Pharmacol 15:443-450.
36. Sloan TP, Mahgoub A, Lancaster R, Idle JR, and Smith RL (1978) Polymorphism of carbon oxidation of drugs and clinical implications. Br Med J 2:655-657.
37. Stearns RA, Chakravarty PK, Chen R, and Chiu SHL (1995) Biotransformation of losartan to its active carboxylic acid metabolite in human liver microsomes: role of cytochrome P4502C and 3A subfamily members. Drug Metab Dispos 23:207-215.
38. Stevens JC, White RB, Hsu SH, and Martinet M (1997) Human liver CYP2B6-catalyzed hydroxylation of RP73401. J Pharmacol Exp Ther 282:1389-1395.
39. Stresser DM, Turner SD, Blanchard AP, Miller VP, and Crespi CL (2002) Cytochrome P450 fluorometric substrates: identification of isoform-selective probes for rat CYP2D2 and human CYP3A4. Drug Metab Dispos 30:845-852.
40. Sullivan-Klose TH, Ghanayem BI, Bell DA, Zhang ZY, Kaminsky LS, Shenfield GM, Miners JO, Birkett DJ, and Goldstein JA (1996) The role of CYP2C9-leu359 allelic variant in the tolbutamide polymorphism Pharmacogenetics 6:341-349.
41. Tucker GT, Houston JB, and Huang SM (2001) Optimizing drug development: strategies to assess drug metabolism/transporter interaction potential-toward a consensus. Clin Pharmacol Ther 70:103-114.
42. Venkatakrishnan K, von Moltke LL, and Greenblatt DJ (2001) Application of the relative activity factor approach in scaling from heterologously expressed cytochrome P450 to human liver microsomes: studies on amitriptyline as a model substrate. J Pharmacol Exp Ther 297:326-337.
43. Wang RW and Lu AYH (1997) Inhibitory anti-peptide antibody against human CYP3A4. Drug Metab Dispos 25:762-767.
44. Weaver RJ, Dickins M, and Burke MD (1995) Hydroxylation of the antimalarial drug 58C80 by CYP2C9 in human liver microsomes: comparison with mephenytoin and tolbutamide hydroxylations. Biochem Pharmacol 49:997-1004.
45. Yamazaki H, Inoue K, Shaw PM, Checovich WJ, Guengerich FP, and Schimada T (1997) Different contributions of cytochrome P450 2C19 and 3A4 in the oxidation of omeprazole by human liver microsomes: effects of contents of these two forms in individual human samples. J Pharmacol Exp Ther 283:434-442.
46. Yang TJ, Krausz KW, Shou M, Yang SK, Buters JTM, Gonzalez FJ, and Gelboin HV (1998) Inhibitory monoclonal antibody to human cytochrome P450 2B6. Biochem Pharmacol 55: 1633-1640.
47. Yasar U, Tybring G, Hidestrand M, Oscarson M, Ingelman-Sunberg M, Dahl ML, and Eliasson E (2001) Role of CYP2C9 polymorphism in losartan oxidation. Drug Metab Dispos 29:1051-1056.
48. Yun CH, Lee HS, Lee H, Rho JK, Jeong HG, and Guengerich FP (1995) Oxidation of the angiotensin II receptor antagonist losartan (DUP753) in human liver microsomes: role of cytochrome P4503A(4) in formation of the active metabolite EXP3174. Drug Metab Dispos 23:285-289.