Constitutive androstane receptor (CAR) functions as a tumor suppressor via regulating stemness in liver cancer [PDF]
Constitutive androstane receptor (CAR) is a xenosensor that is almost exclusively expressed in the liver. Studies in rodents suggest an oncogenic role for CAR in liver cancer, but its role in human liver cancer is unclear.
Sarah Da Won Bae +5 more
doaj +2 more sources
Transcriptomic analysis across liver diseases reveals disease-modulating activation of constitutive androstane receptor in cholestasis [PDF]
Background & Aims: Liver diseases are caused by many factors, such as genetics, nutrition, and viruses. Therefore, it is important to delineate transcriptomic changes that occur in various liver diseases.
Bhoomika Mathur +10 more
doaj +2 more sources
Activation of the Constitutive Androstane Receptor Inhibits Leukocyte Adhesiveness to Dysfunctional Endothelium [PDF]
Laura Piqueras +2 more
exaly +2 more sources
Summary: Here, we describe an optimized protocol to identify specific nuclear receptor ligands. First, to rule out any compound interference with luciferase activity per se, we describe an in vitro assay assessing potential inhibition or activation of ...
Alexandre Berthier +2 more
doaj +1 more source
Searching for Constitutive Androstane Receptor Modulators [PDF]
The constitutive androstane receptor (CAR; NR1I3) has been established as one of the main drug- and xenobiotic-responsive transcriptional regulators, collectively called xenosensors. CAR activates the expression of several oxidative, hydrolytic, and conjugative drug-metabolizing enzymes and drug transporters, and therefore, it contributes to drug and ...
openaire +2 more sources
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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The induction potentials of ligand-activated nuclear receptors on metabolizing enzyme genes are routinely tested for new chemical entities. However, regulations of drug transporter genes by the nuclear receptor ligands are underappreciated, especially in
Congrong Niu, Bill Smith, Yurong Lai
doaj +1 more source
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
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
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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