scholarly journals In Vitro Characterization of Ertugliflozin Metabolism by UDP-Glucuronosyltransferase and Cytochrome P450 Enzymes

2020 ◽  
Vol 48 (12) ◽  
pp. 1350-1363
Author(s):  
Kimberly Lapham ◽  
Ernesto Callegari ◽  
Julie Cianfrogna ◽  
Jian Lin ◽  
Mark Niosi ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 Enzymes ◽  
In Vitro Characterization ◽  
Udp Glucuronosyltransferase

IN VITRO CHARACTERIZATION OF CLOBAZAM METABOLISM BY RECOMBINANT CYTOCHROME P450 ENZYMES: IMPORTANCE OF CYP2C19

2004 ◽  
Vol 32 (11) ◽  
pp. 1279-1286 ◽  
Author(s):  
Carole Giraud ◽  
Agnès Tran ◽  
Elisabeth Rey ◽  
Jean Vincent ◽  
Jean-Marc Tréluyer ◽  
...  
Keyword(s):  
Cytochrome P450 ◽  
Cytochrome P450 Enzymes ◽  
In Vitro Characterization

scholarly journals Highly Miniaturized Formats for In Vitro Drug Metabolism Assays Using Vivid® Fluorescent Substrates and Recombinant Human Cytochrome P450 Enzymes

2005 ◽  
Vol 10 (1) ◽  
pp. 56-66 ◽  
Author(s):  
Olga V. Trubetskoy ◽  
Jasmin R. Gibson ◽  
Bryan D. Marks
Keyword(s):  
Cytochrome P450 ◽  
High Throughput Screening ◽  
Cytochrome P450 Enzymes ◽  
Fluorogenic Substrates ◽  
Detailed Characterization ◽  
Human Cytochrome ◽  
Screening Assays ◽  
Well Assay

Highly miniaturized P450 screening assays designed to enable facile analysis of P450 drug interactions in a 1536-well plate format with the principal human cytochrome P450 enzymes (CYP3A4, 2D6, 2C9, 2C19, and 1A2) and Vivid® fluorogenic substrates were developed. The detailed characterization of the assays included stability, homogeneity, and reproducibility of the recombinant P450 enzymes and the kinetic parameters of their reactions with Vivid® fluorogenic substrates, with a focus on the specific characteristics of each component that enable screening in a low-volume 1536-well plate assay format. The screening assays were applied for the assessment of individual cytochrome P450 inhibition profiles with a panel of selected assay modifiers, including isozyme-specific substrates and inhibitors. IC50 values obtained for the modifiers in 96- and 1536-well plate formats were similar and comparable with values obtained in assays with conventional substrates. An overall examination of the 1536-well assay statistics, such as signal-to-background ratio and Z′ factor, demonstrated that these assays are a robust, successful, and reliable tool to screen for cytochrome P450 metabolism and inhibition in an ultra-high-throughput screening format. ( Journal of Biomolecular Screening 2005:56-66)

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