Drug-drug interactions by azole antifungals: Beyond a dogma of CYP3A4 enzyme activity inhibition

Kód výsledku v IS VaVaI

<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F61989592%3A15310%2F11%3A33119053" target="_blank" >RIV/61989592:15310/11:33119053 - isvavai.cz</a>

Výsledek na webu

<a href="http://dx.doi.org/10.1016/j.toxlet.2011.01.027" target="_blank" >http://dx.doi.org/10.1016/j.toxlet.2011.01.027</a>

DOI - Digital Object Identifier

<a href="http://dx.doi.org/10.1016/j.toxlet.2011.01.027" target="_blank" >10.1016/j.toxlet.2011.01.027</a>

Jazyk výsledku

angličtina

Název v původním jazyce

Drug-drug interactions by azole antifungals: Beyond a dogma of CYP3A4 enzyme activity inhibition

Popis výsledku v původním jazyce

Azoles antifungals are widespread used drugs for various medicinal indications. These drugs are well known for their numerous drug-drug interactions, which are believed to occur via inhibition of CYP3A4 enzymatic activity and consequently altering pharmacokinetic of co-administered drugs. In the current communication a complex view on the molecular interactions between azoles antimycotics and CYP3A4 is presented. Beside inhibition of CYP3A4 catalytic activity, azoles influence transcriptional activity of pregnane X receptor (PXR) and consequently expression of drug-metabolizing enzymes, including CYP3A4. Interactions between azoles and PXR occur by multiple mechanisms, including modulation of ligand-dependent activation of PXR (agonism, antagonism) oraffecting recruitment of PXR co-activators SRC-1 (steroid receptorco-activator 1)and HNF4 alpha (hepatocyte nuclear factor 4 alpha). Miconazole and ketoconazole are antagonists of glucocorticoid receptor (GR), therefore these drugs inhibi

Název v anglickém jazyce

Drug-drug interactions by azole antifungals: Beyond a dogma of CYP3A4 enzyme activity inhibition

Popis výsledku anglicky

Azoles antifungals are widespread used drugs for various medicinal indications. These drugs are well known for their numerous drug-drug interactions, which are believed to occur via inhibition of CYP3A4 enzymatic activity and consequently altering pharmacokinetic of co-administered drugs. In the current communication a complex view on the molecular interactions between azoles antimycotics and CYP3A4 is presented. Beside inhibition of CYP3A4 catalytic activity, azoles influence transcriptional activity of pregnane X receptor (PXR) and consequently expression of drug-metabolizing enzymes, including CYP3A4. Interactions between azoles and PXR occur by multiple mechanisms, including modulation of ligand-dependent activation of PXR (agonism, antagonism) oraffecting recruitment of PXR co-activators SRC-1 (steroid receptorco-activator 1)and HNF4 alpha (hepatocyte nuclear factor 4 alpha). Miconazole and ketoconazole are antagonists of glucocorticoid receptor (GR), therefore these drugs inhibi

Druh

J_x - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)

CEP obor

FR - Farmakologie a lékárnická chemie

OECD FORD obor

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Projekt

Výsledek vznikl pri realizaci vícero projektů. Více informací v záložce Projekty.

Návaznosti

P - Projekt vyzkumu a vyvoje financovany z verejnych zdroju (s odkazem do CEP)

Rok uplatnění

2011

Kód důvěrnosti údajů

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

Název periodika

Toxicology Letters

ISSN

0378-4274

e-ISSN

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Svazek periodika

202

Číslo periodika v rámci svazku

2

Stát vydavatele periodika

IE - Irsko

Počet stran výsledku

4

Strana od-do

129-132

Kód UT WoS článku

000289708000007

EID výsledku v databázi Scopus

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