On-Line Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 inhibitors

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216224%3A14310%2F20%3A00113958" target="_blank" >RIV/00216224:14310/20:00113958 - isvavai.cz</a>

Výsledek na webu

<a href="https://link.springer.com/protocol/10.1007%2F978-1-0716-0163-1_11" target="_blank" >https://link.springer.com/protocol/10.1007%2F978-1-0716-0163-1_11</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1007/978-1-0716-0163-1_11" target="_blank" >10.1007/978-1-0716-0163-1_11</a>

Jazyk výsledku

angličtina

Název v původním jazyce

On-Line Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 inhibitors

Popis výsledku v původním jazyce

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.

Název v anglickém jazyce

On-Line Enantioselective Capillary Electrophoretic Method for Screening Cytochrome P450 3A4 inhibitors

Popis výsledku anglicky

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.

Druh

C - Kapitola v odborné knize

CEP obor

—

OECD FORD obor

10609 - Biochemical research methods

Projekt

<a href="/cs/project/GA16-06106S" target="_blank" >GA16-06106S: Vysoce efektivní systém založený na kapilární elektroforéze pro screening inhibitorů beta-sekretázy jako terapeutického cíle pro Alzheimerovu chorobu</a><br>

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace

Rok uplatnění

2020

Kód důvěrnosti údajů

S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů

Název knihy nebo sborníku

Targeting Enzymes for Pharmaceutical Development: Methods and Protocols

ISBN

9781071601624

Počet stran výsledku

12

Strana od-do

167-178

Počet stran knihy

278

Název nakladatele

Springer

Místo vydání

USA

Kód UT WoS kapitoly

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