C 2020

Online Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 Inhibitors

ŘEMÍNEK, Roman, Zdeněk GLATZ and Wolfgang THORMANN

Basic information

Original name

Online Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 Inhibitors

Name in Czech

Online enantioselektivní kapilárně elektroforetická metoda pro screening inhibitorů cytochromu P450 3A4

Authors

ŘEMÍNEK, Roman (203 Czech Republic, belonging to the institution), Zdeněk GLATZ (203 Czech Republic, guarantor, belonging to the institution) and Wolfgang THORMANN (756 Switzerland)

Edition

1. vyd. USA, Targeting Enzymes for Pharmaceutical Development: Methods and Protocols, p. 167-178, 12 pp. Targeting Enzymes for Pharmaceutical Development, 2020

Publisher

Springer

Other information

Language

English

Type of outcome

Kapitola resp. kapitoly v odborné knize

Field of Study

10609 Biochemical research methods

Country of publisher

United States of America

Confidentiality degree

není předmětem státního či obchodního tajemství

Publication form

printed version "print"

References:

RIV identification code

RIV/00216224:14310/20:00113958

Organization unit

Faculty of Science

ISBN

978-1-0716-0162-4

UT WoS

000650966200012

Keywords (in Czech)

Kapilární elektroforéza; Enantioselektivní separace; Cytochrom P450; CYP3A4; Ketamin

Keywords in English

Capillary electrophoresis; Enantioselective separation; Cytochrome P450; CYP3A4; Ketamine

Tags

International impact, Reviewed
Změněno: 16/8/2021 12:46, Mgr. Marie Šípková, DiS.

Abstract

V originále

The market share of single-enantiomer drugs is steadily increasing. The pharmacodynamics and pharmacokinetics of individual enantiomers can differ considerably. Thus, their characteristics have to be addressed as early as possible in the development process of new pharmaceuticals. Capillary electrophoresis is a promising technique for enantioselective drug metabolism studies due to highly effective separations, minuscule consumption of sample and reagents, compatibility with a variety of detection techniques, high-throughput via automation, and the implementation of on-line procedures. An on-line method comprised of the diffusion-based mixing of cytochrome P450 3A4 with racemic ketamine, incubation of the enzyme reaction, separation of the reaction products S- and R-norketamine and their quantification is presented in this chapter. Since diffusion is an inherent property of all molecules, the method enables the addition of virtually any compound to the reaction mixture without the need for additional optimization of the mixing conditions, and thus can be favorably used for the rapid screening of putative cytochrome P450 3A4 inhibitors.

In Czech

Byl publikován protokol pro screening inhibitorů cytochromu P450 3A4 pomocí on-line enantioselektivní metody založené na kapilární elektroforéze.

Links

GA16-06106S, research and development project
Name: Vysoce efektivní systém založený na kapilární elektroforéze pro screening inhibitorů beta-sekretázy jako terapeutického cíle pro Alzheimerovu chorobu (Acronym: Alzheimer)
Investor: Czech Science Foundation