Diazepam Promotes Translocation of Human Constitutive Androstane Receptor (CAR) via Direct Interaction with the Ligand-Binding Domain

Diazepam Promotes Translocation of Human Constitutive Androstane Receptor (CAR) via Direct Interaction with the Ligand-Binding Domain

The constitutive androstane receptor (CAR) is the essential regulator of genes involved both in xenobiotic and endobiotic metabolism. Diazepam has been shown as a potent stimulator of CAR nuclear translocation and is assumed as an indirect CAR activator not interacting with the CAR cavity. In this s...

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Bibliographic Details
Main Authors: Josef Skoda, Jan Dusek, Martin Drastik, Alzbeta Stefela, Klara Dohnalova, Karel Chalupsky, Tomas Smutny, Stanislav Micuda, Sabine Gerbal-Chaloin, Petr Pavek
Format: Article
Language:English
Published: MDPI AG 2020-11-01
Series:Cells
Subjects:
diazepam
gene regulation
CAR
NR1I3
cytochrome P450
drug interaction
Online Access:https://www.mdpi.com/2073-4409/9/12/2532

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