TOWARDS CYTOCHROME P450 IMER FOR KINETICS AND INHIBITION STUDIES USING CAPILLARY ELECTROPHORESIS IN ONLINE CONFIGURATION

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Authors

SCHEJBAL Jan ŘEMÍNEK Roman GLATZ Zdeněk

Year of publication 2014
Type Article in Proceedings
Conference 11 th International Interdisciplinary Meeting on Bioanalysis CECE 2014
MU Faculty or unit

Central European Institute of Technology

Citation
Field Biochemistry
Keywords kapilární elektroforéza; metabolismus léčiv; cytochrom P450 2C9; IMER; diclofenac; sulfafenazol; kinetika; inhibice;
Description The enzyme superfamily of cytochromes P450 (CYP) plays a key role in xenobiotic biotransformation and thusly in drug metabolism. Therefore assessment of the interaction between candidate drugs and CYP isoforms is an integral part of preclinical stage of the drug development process, where high throughput and cost effectiveness is a priority. Capillary electrophoresis (CE) offers a number of features which are suitable for these purposes, those being the low sample consumption, short analysis time and parallel analyses using multicapillary systems, what more integration of immobilized enzyme microreactor (IMER) into the separation capillary enables full automation and repeated use of the enzyme. A new online method for inhibition studies based on cytochrome P450 2C9 isoform IMER integrated into CE system is thus presented.
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