Rapid determination of enzyme activities of recombinant human cytochromes P450, human liver microsomes and hepatocytes
Cytochrome P450 (CYP) substrates that yield fluorescent metabolites were used for rapid screening of drug metabolism activities of 13 recombinant human cytochromes P450, human liver microsomes and human hepatocytes. Reproducible results were obtained using a fluorescent plate reader (CytoFluor) more...
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Published in | Biopharmaceutics & drug disposition Vol. 24; no. 9; pp. 375 - 384 |
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Main Authors | , , , , , , |
Format | Journal Article |
Language | English |
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Chichester, UK
John Wiley & Sons, Ltd
01.12.2003
Wiley |
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Abstract | Cytochrome P450 (CYP) substrates that yield fluorescent metabolites were used for rapid screening of drug metabolism activities of 13 recombinant human cytochromes P450, human liver microsomes and human hepatocytes. Reproducible results were obtained using a fluorescent plate reader (CytoFluor) more expediently than those generated using conventional HPLC methods. Typically, results for 96 samples were obtained with the plate reader in less than 10 min as opposed to 15–35 min/sample required by conventional HPLC. The fluorescent substrates used to measure CYP activities were as follows: 3‐cyano‐7‐ethoxycoumarin (CEC) for CYP1A1, CYP1A2, CYP2C9 and CYP2C19; 7‐ethoxyresorufin (7‐ER) for CYP1A1, CYP1A2 and CYP1B1; 3‐[2‐(N,N‐diethyl‐N‐methylammonium)ethyl]‐7‐methoxy‐4‐methylcoumarin (AMMC) for CYP2D6; dibenzylfluorescein (DBF) for CYP3A4, CYP3A5 and CYP2C8; 7‐methoxy‐4‐trifluoromethylcoumarin (7‐MFC) for CYP2E1, CYP2B6 and CYP2C18; and coumarin for CYP2A6. The chemical inhibition and correlation data indicated that the following substrates can be used as specific functional probes for individual cytochrome P450 present in human liver microsomes: coumarin for CYP2A6 (r=0.82), AMMC for CYP2D6 (r=0.83) and DBF for CYP3A4 (r=0.92). The fluorescent plate reader was found to be useful for the rapid assessment of CYP activities (positive control) in both intact cells and subcellular fractions. Copyright © 2003 John Wiley & Sons, Ltd. |
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AbstractList | Cytochrome P450 (CYP) substrates that yield fluorescent metabolites were used for rapid screening of drug metabolism activities of 13 recombinant human cytochromes P450, human liver microsomes and human hepatocytes. Reproducible results were obtained using a fluorescent plate reader (CytoFluor) more expediently than those generated using conventional HPLC methods. Typically, results for 96 samples were obtained with the plate reader in less than 10 min as opposed to 15-35 min/sample required by conventional HPLC. The fluorescent substrates used to measure CYP activities were as follows: 3-cyano-7-ethoxycoumarin (CEC) for CYP1A1, CYP1A2, CYP2C9 and CYP2C19; 7-ethoxyresorufin (7-ER) for CYP1A1, CYP1A2 and CYP1B1; 3-[2-(N,N-diethyl-N-methylammonium)ethyl]-7-methoxy-4-methylcoumarin (AMMC) for CYP2D6; dibenzylfluorescein (DBF) for CYP3A4, CYP3A5 and CYP2C8; 7-methoxy-4-trifluoromethylcoumarin (7-MFC) for CYP2E1, CYP2B6 and CYP2C18; and coumarin for CYP2A6. The chemical inhibition and correlation data indicated that the following substrates can be used as specific functional probes for individual cytochrome P450 present in human liver microsomes: coumarin for CYP2A6 (r=0.82), AMMC for CYP2D6 (r=0.83) and DBF for CYP3A4 (r=0.92). The fluorescent plate reader was found to be useful for the rapid assessment of CYP activities (positive control) in both intact cells and subcellular fractions. Cytochrome P450 (CYP) substrates that yield fluorescent metabolites were used for rapid screening of drug metabolism activities of 13 recombinant human cytochromes P450, human liver microsomes and human hepatocytes. Reproducible results were obtained using a fluorescent plate reader (CytoFluor) more expediently than those generated using conventional HPLC methods. Typically, results for 96 samples were obtained with the plate reader in less than 10 min as opposed to 15–35 min/sample required by conventional HPLC. The fluorescent substrates used to measure CYP activities were as follows: 3‐cyano‐7‐ethoxycoumarin (CEC) for CYP1A1, CYP1A2, CYP2C9 and CYP2C19; 7‐ethoxyresorufin (7‐ER) for CYP1A1, CYP1A2 and CYP1B1; 3‐[2‐(N,N‐diethyl‐N‐methylammonium)ethyl]‐7‐methoxy‐4‐methylcoumarin (AMMC) for CYP2D6; dibenzylfluorescein (DBF) for CYP3A4, CYP3A5 and CYP2C8; 7‐methoxy‐4‐trifluoromethylcoumarin (7‐MFC) for CYP2E1, CYP2B6 and CYP2C18; and coumarin for CYP2A6. The chemical inhibition and correlation data indicated that the following substrates can be used as specific functional probes for individual cytochrome P450 present in human liver microsomes: coumarin for CYP2A6 (r=0.82), AMMC for CYP2D6 (r=0.83) and DBF for CYP3A4 (r=0.92). The fluorescent plate reader was found to be useful for the rapid assessment of CYP activities (positive control) in both intact cells and subcellular fractions. Copyright © 2003 John Wiley & Sons, Ltd. Abstract Cytochrome P450 (CYP) substrates that yield fluorescent metabolites were used for rapid screening of drug metabolism activities of 13 recombinant human cytochromes P450, human liver microsomes and human hepatocytes. Reproducible results were obtained using a fluorescent plate reader (CytoFluor) more expediently than those generated using conventional HPLC methods. Typically, results for 96 samples were obtained with the plate reader in less than 10 min as opposed to 15–35 min/sample required by conventional HPLC. The fluorescent substrates used to measure CYP activities were as follows: 3‐cyano‐7‐ethoxycoumarin (CEC) for CYP1A1, CYP1A2, CYP2C9 and CYP2C19; 7‐ethoxyresorufin (7‐ER) for CYP1A1, CYP1A2 and CYP1B1; 3‐[2‐( N , N ‐diethyl‐ N ‐methylammonium)ethyl]‐7‐methoxy‐4‐methylcoumarin (AMMC) for CYP2D6; dibenzylfluorescein (DBF) for CYP3A4, CYP3A5 and CYP2C8; 7‐methoxy‐4‐trifluoromethylcoumarin (7‐MFC) for CYP2E1, CYP2B6 and CYP2C18; and coumarin for CYP2A6. The chemical inhibition and correlation data indicated that the following substrates can be used as specific functional probes for individual cytochrome P450 present in human liver microsomes: coumarin for CYP2A6 ( r =0.82), AMMC for CYP2D6 ( r =0.83) and DBF for CYP3A4 ( r =0.92). The fluorescent plate reader was found to be useful for the rapid assessment of CYP activities (positive control) in both intact cells and subcellular fractions. Copyright © 2003 John Wiley & Sons, Ltd. |
Author | Zbaida, Shmuel Yuan, Yuan Ghosal, Anima Horne, Debra Hapangama, Neil Patrick, James E. Lu, Xiaowen |
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Keywords | Human human liver microsomes Enzyme Isozyme Cytochrome P450 Liver Microsome In vitro fluorescent probes Enzymatic activity Hepatocyte Drug-metabolizing enzyme Recombinant protein |
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update on new sequences, gene mapping, accession numbers and nomenclature publication-title: Pharmacogenetics – volume: 213 start-page: 29 year: 1993 end-page: 33 article-title: A microassay for measuring cytochrome P4501A1 and P450IIBI activities in intact human and rat hepatocytes cultured on 96‐well plates publication-title: Anal Biochem – volume: 29 start-page: 30 year: 2001 end-page: 35 article-title: Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s publication-title: Drug Metab Dispos – volume: 258 start-page: 8839 year: 1983 end-page: 8847 article-title: Regio‐ and stereoselective metabolism of two C steroids by five highly purified and reconstituted rat hepatic cytochrome P450 isozymes publication-title: J Biol Chem – volume: 248 start-page: 188 year: 1997 end-page: 190 article-title: Microtiter plate assays for the inhibition of human, drug‐metabolizing cytochromes P450 publication-title: Anal Biochem – volume: 276 start-page: 215 year: 1999 end-page: 226 article-title: Description of a 96‐well plate assay to measure cytochrome P4503A inhibition in human liver microsomes using a select fluorescent probe publication-title: Anal Biochem – volume: 25 start-page: 1130 year: 1997 end-page: 1136 article-title: In vitro comparison of cytochrome P450‐mediated metabolic activities in human, dog, cat and horse publication-title: Drug Metab Dispos – volume: 32 start-page: 188 year: 2000 article-title: Microtiter plate based assay for a rapid determination of enzyme activities of 13 P450 supersomes and human liver microsomes Abstract 103. 10th North American ISSX Meeting, Indianapolis publication-title: Drug Metabolism Review – volume: 29 start-page: 1196 year: 2001 end-page: 1200 article-title: The use of 3‐[2‐( , ‐diethyl‐ ‐methylammonium)ethyl]‐7‐methoxy‐4‐methylcoumarin (AMMC) as a specific CYP2D6 probe in human liver microsomes publication-title: Drug Metab Dispos – ident: e_1_2_1_7_2 doi: 10.1006/abio.1999.4348 – volume: 25 start-page: 1130 year: 1997 ident: e_1_2_1_11_2 article-title: In vitro comparison of cytochrome P450‐mediated metabolic activities in human, dog, cat and horse publication-title: Drug Metab Dispos contributor: fullname: Chauret N – volume: 32 start-page: 188 year: 2000 ident: e_1_2_1_13_2 article-title: Microtiter plate based assay for a rapid determination of enzyme activities of 13 P450 supersomes and human liver microsomes Abstract 103. 10th North American ISSX Meeting, Indianapolis publication-title: Drug Metabolism Review contributor: fullname: Ghosal A – volume: 28 start-page: 567 year: 2000 ident: e_1_2_1_14_2 article-title: Substrate‐dependent effect of acetonitrile on human liver microsomal cytochrome P450 2C9 (CYP2C9) activity publication-title: Drug Metab Dispos contributor: fullname: Tang C – volume: 27 start-page: 1117 year: 1999 ident: e_1_2_1_16_2 article-title: Heterologous expression and kinetic characterization of human cytochromes P‐450: validation of a pharmaceutical tool for drug metabolism research publication-title: Drug Metab Dispos contributor: fullname: Masimirembwa CM – ident: e_1_2_1_2_2 doi: 10.1097/00008571-199602000-00002 – ident: e_1_2_1_12_2 doi: 10.1124/dmd.30.7.845 – volume: 29 start-page: 30 year: 2001 ident: e_1_2_1_9_2 article-title: Application of higher throughput screening (HTS) inhibition assays to evaluate the interaction of antiparasitic drugs with cytochrome P450s publication-title: Drug Metab Dispos contributor: fullname: Bapiro TE – volume: 2 start-page: 15 year: 1999 ident: e_1_2_1_3_2 article-title: Higher‐throughput screening with human cytochromes P450 publication-title: Curr Opin Drug Discovery Develop contributor: fullname: Crespi CL – volume: 29 start-page: 617 year: 1997 ident: e_1_2_1_10_2 article-title: Oxidation of xenobiotics by recombinant human cytochrome P450 1B1 publication-title: Drug Metab Dispos contributor: fullname: Shimada T – ident: e_1_2_1_6_2 doi: 10.1006/abio.1993.1381 – volume: 29 start-page: 1196 year: 2001 ident: e_1_2_1_15_2 article-title: 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 publication-title: Drug Metab Dispos contributor: fullname: Chauret N – volume: 36 start-page: 89 year: 1989 ident: e_1_2_1_4_2 article-title: Oxidation of midazolam and triazolam by human liver cytochrome P450IIIA4 publication-title: Mol Pharmacol contributor: fullname: Kronbach DM – ident: e_1_2_1_8_2 doi: 10.1006/abio.1997.2145 – volume: 258 start-page: 8839 year: 1983 ident: e_1_2_1_5_2 article-title: Regio‐ and stereoselective metabolism of two C19 steroids by five highly purified and reconstituted rat hepatic cytochrome P450 isozymes publication-title: J Biol Chem doi: 10.1016/S0021-9258(18)32132-X contributor: fullname: Wood AW |
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Snippet | Cytochrome P450 (CYP) substrates that yield fluorescent metabolites were used for rapid screening of drug metabolism activities of 13 recombinant human... Abstract Cytochrome P450 (CYP) substrates that yield fluorescent metabolites were used for rapid screening of drug metabolism activities of 13 recombinant... |
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SubjectTerms | Analytical, structural and metabolic biochemistry Biological and medical sciences Cytochrome P-450 Enzyme System - chemistry Cytochrome P-450 Enzyme System - metabolism cytochrome P450 Enzymes and enzyme inhibitors fluorescent probes Fluorometry Fundamental and applied biological sciences. Psychology Hepatocytes - enzymology human liver microsomes Humans In Vitro Techniques Kinetics Microsomes, Liver - enzymology Oxidoreductases Recombinant Proteins - chemistry Recombinant Proteins - metabolism |
Title | Rapid determination of enzyme activities of recombinant human cytochromes P450, human liver microsomes and hepatocytes |
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