Activation of the Constitutive Androstane Receptor by Monophthalates [PDF]
Humans in industrialized areas are continuously exposed to phthalate plasticizers, prompting concerns of their potential toxicities. Previous studies from our laboratory and others have shown that various phthalates activate several mammalian nuclear receptors, in particular the constitutive androstane receptor (CAR), the pregnane X receptor (PXR), and
Elizabeth M, Laurenzana +4 more
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MicroRNA-122 down-regulation is involved in phenobarbital-mediated activation of the constitutive androstane receptor. [PDF]
Constitutive androstane receptor (CAR) is a nuclear receptor that regulates the transcription of target genes, including CYP2B and 3A. Phenobarbital activates CAR, at least in part, in an AMP-activated protein kinase (AMPK)-dependent manner. However, the
Ryota Shizu +3 more
doaj +1 more source
Signaling control of the constitutive androstane receptor (CAR) [PDF]
The constitutive androstane receptor (CAR, NR1I3) plays a crucial role in the regulation of drug metabolism, energy homeostasis, and cancer development through modulating the transcription of its numerous target genes. Different from prototypical nuclear receptors, CAR can be activated by either direct ligand binding or ligand-independent (indirect ...
Yang, Hui, Wang, Hongbing
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AhR, PXR and CAR: From Xenobiotic Receptors to Metabolic Sensors
Traditionally, xenobiotic receptors are known for their role in chemical sensing and detoxification, as receptor activation regulates the expression of various key enzymes and receptors.
Leonida Rakateli +2 more
doaj +1 more source
A novel panel of mouse models to evaluate the role of human pregnane X receptor and constitutive androstane receptor in drug response [PDF]
The pregnane X receptor (PXR) and the constitutive androstane receptor (CAR) are closely related orphan nuclear hormone receptors that play a critical role as xenobiotic sensors in mammals.
Anja Rode +19 more
core +4 more sources
Small-molecule modulators of the constitutive androstane receptor [PDF]
The constitutive androstane receptor (CAR) induces drug-metabolizing enzymes for xenobiotic metabolism.This review covers recent advances in elucidating the biological functions of CAR and its modulation by a growing number of agonists and inhibitors.Extrapolation of animal CAR function to that of humans should be carefully scrutinized, particularly ...
Milu T, Cherian +2 more
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Modulation of Xenobiotic Receptors by Steroids
Nuclear receptors (NRs) are ligand-activated transcription factors that regulate the expression of their target genes. NRs play important roles in many human diseases, including metabolic diseases and cancer, and are therefore a key class of therapeutic ...
Delira Robbins +2 more
doaj +1 more source
Unsaturated fatty acid regulation of cytochrome P450 expression via a CAR-dependent pathway. [PDF]
The liver is responsible for key metabolic functions, including control of normal homoeostasis in response to diet and xenobiotic metabolism/detoxification.
Finn, Robert +3 more
core +4 more sources
Dietary Flavonoids Activate the Constitutive Androstane Receptor (CAR) [PDF]
The constitutive androstane receptor (CAR) is known as a xeno-sensor that regulates genes involved in xenobiotic excretion and energy metabolism. This study tested a variety of polyphenols for their ability to modulate CAR activity. HepG2 cells were transfected with a CAR expression plasmid and a reporter plasmid containing the human CYP2B6 regulatory ...
Ruiquing, Yao +10 more
openaire +2 more sources
The nuclear receptors and xenosensors constitutive androstane receptor (CAR, NR1I3) and pregnane X receptor (PXR, NR1I2) induce the expression of xenobiotic metabolizing enzymes and transporters, which also affects various endobiotics.
Marianne Mathäs +6 more
doaj +1 more source

