Publication Cover
Xenobiotica
the fate of foreign compounds in biological systems
Volume 33, 2003 - Issue 8
154
Views
15
CrossRef citations to date
0
Altmetric
Research Article

High-throughput screening to estimate single or multiple enzymes involved in drug metabolism: microtitre plate assay using a combination of recombinant CYP2D6 and human liver microsomes

, &
Pages 823-839 | Published online: 22 Sep 2008

Reference

  • ANZENBACHEROVA, E., ANZENBACHER, P., PERLIK, F. and KVETINA, J., 2000, Use of a propafenone metabolic ratio as a measure of CYP2D6 activity. International Journal of Clinical Pharmacology and Therapeutics, 38, 426–429.
  • BALL, S. E., AHERN, D., SCATINA, J. and KAO, J., 1997, Venlafaxine: in vitro inhibition of CYP2D6 dependent imipramine and desipramine metabolism; comparative studies with selected SSRIs, and effects on human hepatic CYP3A4, CYP2C9 and CYP1A2. British Journal of Clinical Pharmacology, 43, 619–626.
  • BAPIRO, T. E., EGNELL, A. C., HASLER, J. A. and MASIMIREMBWA, C. M., 2001, Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s. Drug Metabolism and Disposition, 29, 30–35.
  • BLAKE, B. L., ROSE, R. L., MAILMAN, R. B., LEVI, P. E. and HODGSON, E., 1995, Metabolism of thioridazine by microsomal monooxygenases: relative roles of P450 and fiavin-containing monooxygenase. Xenobiotica, 25, 377–393.
  • BROLY, F. GAEDIGK, A., HEIM, M., EICHELBAUM, M., MORIKE, K. and VMEYER, U. A., 1991, Debrisoquine/sparteine hydroxylation genotype and phenotype: analysis of common mutations and alleles of CYP2D6 in a European population. DNA and Cell Biology, 10, 545–558.
  • CHAURET, N., DOBBS, B., LACKMAN, R. L., BATEMAN, K., NICOLL-GRIFFITH, D. A., STRESSER, D. M., ACKERMANN, J. M., TURNER, S. D., MILLER, V. P. and CRESPI, C. L., 2001, The Use Of 342-(N,N-diethyl-N-methyl-ammonium)ethy11-7-methoxy-4-methylcoumarin (AMMC) as a specific CYP2D6 probe in human liver microsomes. Drug Metabolism and Disposition, 29, 1196–1200.
  • CRESPI, C. L., MILLER, V. P. and PENMAN, B. W., 1997, Microtiter plate assays for inhibition of human, drug-metabolizing cytochromes P450. Analytical Biochemistry, 248, 188–190.
  • FANG, J., BOURIN, M. and BAKER, G. B., 1999, Metabolism of risperidone to 9-hydroxyrisperidone by human cytochromes P450 2D6 and 3A4. Naunyn-Schmiedebergs Archives of Pharmacology, 359, 147–151.
  • FROMM, M. F., KROEMER, H. K. and EICHELBAU M., 1997, Impact of P450 genetic polymorphism on the first-pass extraction of cardiovascular and neuroactive drugs. Advanced Drug Delivery Reviews, 27, 171–199.
  • GONZALEZ, F. J., 1988, The molecular biology of cytochrome P450s. Pharmacological Reviews, 40, 243–288.
  • GUENGERICH, F. P., 1995, Human cytochrome P450 enzymes. In P. R. Ortiz-de Montellano (ed.), Cytochrome P450 (New York: Plenum), pp. 473–535,.
  • GUENGERICH, F. P., 1996, In vitro techniques for studying drug metabolism. Journal of Pharmacokinetics and Biopharmaceutics, 24, 521–533.
  • GUENGERICH, F. P., 1997, Role of cytochrome P450 enzymes in drug—drug interactions. Advances in Pharmacology, 43, 7–35.
  • HORAI, Y., NANO, M., ISHIZAKI, T., ISHIKAWA, K., ZHOU, H. H., ZHOU, B. I., LIAO, C. L. and ZHANG, L. M., 1989, Metoprolol and mephenytoin oxidation polymorphisms in Far Eastern Oriental subjects: Japanese versus mainland Chinese. Clinical Pharmacology and Therapeutics, 46, 198–207.
  • Ism', Y., NAKAMURA, K., TSUTSUMI, K., KOTEGAWA, T., NAKANO, S. and NAKATSUKA, K., 2000, Drug interaction between cimetidine and timolol ophthalmic solution: effect on heart rate and intraocular pressure in healthy Japanese volunteers. Journal of Clinical Pharmacology, 40, 193–199.
  • KOYAMA, E., CHIBA, K., TANI, M. and ISHIZAKI, T., 1996, Identification of human cytochrome P450 isoforms involved in the stereoselective metabolism of mianserin enantiomers. Journal of Pharmacology and Experimental Therapeutics, 278, 21–30.
  • KOYAMA, E., CHIBA, K., TANI, M. and IsHizmo, T., 1997, Reappraisal of human CYP isoforms involved in imipramine N-demethylation and 2-hydroxylation: a study using microsomes obtained from putative extensive and poor metabolizers of S-mephenytoin and eleven recombinant human CYPs. Journal of Pharmacology and Experimental Therapeutics, 281, 1199–1210.
  • LEWIS, D. F. V., EDDERSHAW, P. J., GOIDAFARB, P. S. and TARBIT, M. H., 1997, Molecular modelling of cytochrome P4502D6 (CYP2D6) based on an alignment with CYP102; structural studies on specific CYP2D6 substrate metabolism. Xenobiotica, 27, 319–340.
  • LINNET, K. and OLESEN, 0. V., 1997, Metabolism of clozapine by cDNA-expressed human cytochrome P450 enzymes. Drug Metabolism and Disposition, 25, 1379–1382.
  • MANKOWSKI, D. C., 1999, The role of CYP2C19 in the metabolism of (+/—) bufuralol, the prototypic substrate of CYP2D6. Drug Metabolism and Disposition, 27, 1024–1028.
  • MCGINNITY, D. F., PARKER, A. J., SOARS, M. and RILEY, R. J., 2000, Automated definition of the enzymology of drug oxidation by the major human drug metabolizing cytochrome P450s. Drug Metabolism and Disposition, 28, 1327–1334.
  • MICHALETS, E. L., 1998, Update: clinically significant cytochrome P-450 drug interactions. Pharmacotherapy, 18, 84–112.
  • MILLER, V. P., STRESSER, D. M., BLANCHARD, A. P., TURNER, S. and CRESPI, C. L., 2000, Fluorometric high-throughput screening for inhibitions of cytochrome P450. Annals New York Academy of Sciences, 919, 26–32.
  • NIELSEN, F., RosHoLm, J. U. and BROSEN, K., 1995, Lack of relationship between quinidine pharmacokinetics and the sparteine oxidation polymorphism. European Journal of Clinical Pharmacology, 48, 501–504.
  • NIELSEN, K. K., FLINOIS, J. P., BEAUNE, P. and BROSEN, K., 1996, The biotransformation of clomipramine in vitro, identification of the cytochrome P450s responsible for the separate metabolic pathways. Journal of Pharmacology and Experimental Therapeutics, 277, 1659–1664.
  • NOMEIR, A. A., RUEGG, C., SHOEMEKER, M., FAVREAU, L. V., PALAMANDA, J. R., SILBER, P. and LIN, C. C., 2001, Inhibition of CYP3A4 in a rapid microtiter plate assay using recombinant enzyme and in human liver microsomes using conventional substrates. Drug Metabolism and Disposition, 29, 748–753.
  • OLESEN, 0. V. and LINNET, K., 2000, Identification of the human cytochrome P450 isoforms mediating in vitro N-dealkylation of perphenazine. British Journal of Clinical Pharmacology, 50, 563–571.
  • OTTON, S. V., CREWE, H. K., LENNARD, M. S., TUCKER, G. T. and WOODS, H. F., 1988, Use of quinidine inhibition to define the role of the sparteine/debrisoquine cytochrome P450 in metoprolol oxidation by human liver microsomes. Journal of Pharmacology and Experimental Therapeutics, 247, 242–247.
  • RENDIC, S. and DI CARLO, F. J., 1997, Human cytochrome P450 enzymes: a status report summarizing their reactions, substrates, inducers, and inhibitors. Drug Metabolism Reviews, 29, 413–580.
  • SHIMADA, T., YAMAZAKI, H., MIMURA, M., INUI, Y. and GUERGERICH, F. P., 1994, Interindividual variations in human liver cytochrome p-450 enzymes involved in the oxidation of drugs, carcinogens and toxic chemicals: studies with liver microsomes of 30 Japanese and 30 Caucasians. Journal of Pharmacology and Experimental Therapeutics, 270, 414–423.
  • SORELLE, R., 1998, Withdrawal of posicor from market. Circulation, 98, 831–832.
  • STRESSER, D. M., TURNER, S. D., BLANCHARD, A. P., MILLER, V. P. and CRESPI, C. L., 2002, Cytochrome P450 fiuorometric substrates: identification of isoform-selective probes for rat CYP2D2 and human CYP3A4. Drug Metabolism and Disposition, 30, 845–852.
  • VENKATAKRISHNAN, K., VON MOLTKE, L. L. and GREENBLATT, D. J., 1999, Nortriptyline E-10-hydroxylation in vitro is mediated by human CYP2D6 (high affinity) and CYP3A4 (low affinity): implications for interactions with enzyme-inducing drugs. Journal of Clinical Pharmacology, 39, 567–577.
  • VENKATAKRISHNAN, K., VON MOLTKE, L. L. and GREENBLATT, D. J., 2001, Application of the relative activity factor approach in scaling from heterologously expressed cytochromes p450 to human liver microsomes: studies on amitriptyline as a model substrate. Journal of Pharmacology and Experimental Therapeutics, 297, 326–337.
  • VON MOLTKE, L. L., GREENBLATT, D. J., DUAN, S. X., HARMATZ, J. S. and SHADER, R. I., 1994, In vitro prediction of the terfenadine-ketoconazole pharmacokinetic interaction. Journal of Clinical Pharmacology, 34, 1222–1227.
  • VON MOLTKE, L. L., GREENBLATT, D. J., DUAN, S. X., HARMATZ, J. S. and SHADER, R. I., 1998, Inhibition of desipramine hydroxylation (cytochrome P450-2D6) in vitro by quinidine and by viral protease inhibitors: relation to drug interactions in vivo. Journal of Pharmaceutical Sciences, 87, 1184–1189.
  • YAMAMOTO, T., Suzuxi, A. and KOHNO, Y., 2002, Application of microtiter plate assay to evaluate inhibitory effects of various compounds on nine cytochrome P450 isoforms and to estimate their inhibitory patterns. Drug Metabolism and Pharmacokinetics, 17, 437–448.
  • YANG, T. J., KRAUSZ, K. W., SAI, Y., GONZALEZ, F. J. and GELBOIN, H. V., 1999, Eight inhibitory monoclonal antibodies define the role of individual P-450s in human liver microsomal diazepam, 7-ethoxycoumarin, and imipramine metabolism. Drug Metabolism and Disposition, 27, 102-109. K., KOBAYASHI, K., Tsumup, M., TANI, M., SHIMADA, N. and CHIBA, K., 2000, Identification of human cytochrome P450 isoforms involved in the 7-hydroxylation of chlorpromazine by human liver microsomes. Life Science, 67, 175–184.
  • YOSHIMOTO, K., ECHIZEN, H., CHIBA, K., TANI, M. and IsRizAxi, T., 1995, Identification of human CYP isoforms involved in the metabolism of propranolol enantiomers — N-desisopropylation is mediated mainly by CYP1A2. British Journal of Clinical Pharmacology, 39, 421–431.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.