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Literature DB >> 19661996

High-throughput fluorescence assay of cytochrome P450 3A4.

Qian Cheng¹, Christal D Sohl, F Peter Guengerich.

Abstract

Cytochrome P450 mono-oxygenases (P450s) are the principal enzymes involved in the oxidative metabolism of drugs and other xenobiotics. In this protocol, we describe a fluorescence-based, high-throughput assay for measuring the activity of P450 3A4, one of the key enzymes involved in drug metabolism. The assay involves the oxidative debenzylation of a substituted coumarin, yielding an increase in fluorescence on reaction. The entire procedure can be accomplished in 1 h or less.

Entities: Chemical Disease Gene Species

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Year: 2009 PMID： 19661996 PMCID： PMC3843962 DOI： 10.1038/nprot.2009.123

Source DB: PubMed Journal: Nat Protoc ISSN： 1750-2799 Impact factor: 13.491

16 in total

1. Coumarin substrates for cytochrome P450 2D6 fluorescence assays.

Authors: K Nakamura; I H Hanna; H Cai; Y Nishimura; K M Williams; F P Guengerich
Journal: Anal Biochem Date: 2001-05-15 Impact factor: 3.365

2. Drug metabolism by Escherichia coli expressing human cytochromes P450.

Authors: A Parikh; E M Gillam; F P Guengerich
Journal: Nat Biotechnol Date: 1997-08 Impact factor: 54.908

3. Multiple P450 substrates in a single run: rapid and comprehensive in vitro interaction assay.

Authors: Miia Turpeinen; Jouko Uusitalo; Uusitalo Jouko; Jorma Jalonen; Jalonen Jorma; Olavi Pelkonen; Pelkeonen Olavi
Journal: Eur J Pharm Sci Date: 2005-01 Impact factor: 4.384

Review 4. In vitro evaluation of reversible and irreversible cytochrome P450 inhibition: current status on methodologies and their utility for predicting drug-drug interactions.

Authors: Stephen Fowler; Hongjian Zhang
Journal: AAPS J Date: 2008-08-07 Impact factor: 4.009

5. Microtiter plate assays for inhibition of human, drug-metabolizing cytochromes P450.

Authors: C L Crespi; V P Miller; B W Penman
Journal: Anal Biochem Date: 1997-05-15 Impact factor: 3.365

Review 6. Luminogenic cytochrome P450 assays.

Authors: James J Cali; Dongping Ma; Mary Sobol; Daniel J Simpson; Susan Frackman; Troy D Good; William J Daily; David Liu
Journal: Expert Opin Drug Metab Toxicol Date: 2006-08 Impact factor: 4.481

7. Design, synthesis, and characterization of 7-methoxy-4-(aminomethyl)coumarin as a novel and selective cytochrome P450 2D6 substrate suitable for high-throughput screening.

Authors: R C Onderwater; J Venhorst; J N Commandeur; N P Vermeulen
Journal: Chem Res Toxicol Date: 1999-07 Impact factor: 3.739

8. An automated, high-throughput, 384 well Cytochrome P450 cocktail IC50 assay using a rapid resolution LC-MS/MS end-point.

Authors: Kuresh A Youdim; Richard Lyons; Leon Payne; Barry C Jones; Kenneth Saunders
Journal: J Pharm Biomed Anal Date: 2008-05-17 Impact factor: 3.935

Review 9. Drug-drug interactions for UDP-glucuronosyltransferase substrates: a pharmacokinetic explanation for typically observed low exposure (AUCi/AUC) ratios.

Authors: J Andrew Williams; Ruth Hyland; Barry C Jones; Dennis A Smith; Susan Hurst; Theunis C Goosen; Vincent Peterkin; Jeffrey R Koup; Simon E Ball
Journal: Drug Metab Dispos Date: 2004-08-10 Impact factor: 3.922

10. In vitro assessment of cytochrome P450 inhibition: strategies for increasing LC/MS-based assay throughput using a one-point IC(50) method and multiplexing high-performance liquid chromatography.

Authors: Tong Lin; Kristine Pan; Joyce Mordenti; Lin Pan
Journal: J Pharm Sci Date: 2007-09 Impact factor: 3.534

8 in total

1. Pharmacogenomic Next-Generation DNA Sequencing: Lessons from the Identification and Functional Characterization of Variants of Unknown Significance in CYP2C9 and CYP2C19.

Authors: Sandhya Devarajan; Irene Moon; Ming-Fen Ho; Nicholas B Larson; Drew R Neavin; Ann M Moyer; John L Black; Suzette J Bielinski; Steven E Scherer; Liewei Wang; Richard M Weinshilboum; Joel M Reid
Journal: Drug Metab Dispos Date: 2019-02-11 Impact factor: 3.922

2. Multisite phosphorylation of human liver cytochrome P450 3A4 enhances Its gp78- and CHIP-mediated ubiquitination: a pivotal role of its Ser-478 residue in the gp78-catalyzed reaction.

Authors: YongQiang Wang; Shenheng Guan; Poulomi Acharya; Yi Liu; Ranjit K Thirumaran; Relly Brandman; Erin G Schuetz; Alma L Burlingame; Maria Almira Correia
Journal: Mol Cell Proteomics Date: 2011-11-17 Impact factor: 5.911

3. Identification of Intestinal UDP-Glucuronosyltransferase Inhibitors in Green Tea (Camellia sinensis) Using a Biochemometric Approach: Application to Raloxifene as a Test Drug via In Vitro to In Vivo Extrapolation.

Authors: Dan-Dan Tian; Joshua J Kellogg; Neşe Okut; Nicholas H Oberlies; Nadja B Cech; Danny D Shen; Jeannine S McCune; Mary F Paine
Journal: Drug Metab Dispos Date: 2018-02-21 Impact factor: 3.922

8. Dynamic interaction between membrane-bound full-length cytochrome P450 and cytochrome b5 observed by solid-state NMR spectroscopy.

Authors: Kazutoshi Yamamoto; Ulrich H N Dürr; Jiadi Xu; Sang-Choul Im; Lucy Waskell; Ayyalusamy Ramamoorthy
Journal: Sci Rep Date: 2013 Impact factor: 4.379