Constitutive Androstane Receptor in Macrophages Regulates Toll‐Like Receptor 4‐Mediated Innate Immune Responses Against Endotoxemic Liver Injury [PDF]
Advanced ScienceMacrophage proinflammatory hyperactivation drives the pathogenesis of acute liver injury, a common complication of sepsis. The role of the nuclear receptor constitutive androstane receptor (CAR) in endotoxin‐induced liver injury remains unclear.
Renjie Cao +12 more
doaj +3 more sources
Noncanonical Constitutive Androstane Receptor Signaling in Gene Regulation. [PDF]
Int J Mol Sci, 2020 The constitutive androstane receptor (CAR, NR1I3) is extremely important for the regulation of many physiological processes, especially xenobiotic (drug) metabolism and transporters.
Pustylnyak YA +2 more
europepmc +5 more sources
The constitutive androstane receptor and pregnane X receptor in the brain. [PDF]
Br J Pharmacol, 2020 Since their discovery, the orphan nuclear receptors constitutive androstane receptor (CAR;NR1I3) and pregnane X receptor (PXR;NR1I2) have been regarded as master regulators of drug disposition and detoxification mechanisms.
Torres-Vergara P +5 more
europepmc +5 more sources
Studies of Coumarin Derivatives for Constitutive Androstane Receptor (CAR) Activation [PDF]
Molecules, 2020 Constitutive androstane receptor (CAR) activation has found to ameliorate diabetes in animal models. However, no CAR agonists are available clinically. Therefore, a safe and effective CAR activator would be an alternative option.
Shin-Hun Juang +11 more
doaj +5 more sources
DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor. [PDF]
ACS Med Chem Lett, 2019 The constitutive androstane receptor (CAR) is a xenobiotic sensor governing the transcription of genes involved in drug disposition, energy homeostasis, and cell proliferation.
Liang D +6 more
europepmc +5 more sources
Activation of the Constitutive Androstane Receptor Inhibits Leukocyte Adhesiveness to Dysfunctional Endothelium. [PDF]
Int J Mol Sci, 2021 Leukocyte cell recruitment into the vascular subendothelium constitutes an early event in the atherogenic process. As the effect of the constitutive androstane receptor (CAR) on leukocyte recruitment and endothelial dysfunction is poorly understood, this
López-Riera M +7 more
europepmc +2 more sources
Searching for Constitutive Androstane Receptor Modulators [PDF]
Drug Metabolism and Disposition, 2022 The constitutive androstane receptor (CAR; NR1I3) has been established as one of the main drug- and xenobiotic-responsive transcriptional regulators, collectively called xenosensors.
P. Honkakoski
semanticscholar +3 more sources
Yes-Associated Protein Is Crucial for Constitutive Androstane Receptor-Driven Hepatocyte Proliferation But Not for Induction of Drug Metabolism Genes in Mice. [PDF]
Hepatology, 2021 Constitutive androstane receptor (CAR) agonists, such as 1,4‐bis [2‐(3,5‐dichloropyridyloxy)] benzene (TCPOBOP), are known to cause robust hepatocyte proliferation and hepatomegaly in mice along with induction of drug metabolism genes without any ...
Bhushan B +10 more
europepmc +2 more sources
Metamizole is a Moderate Cytochrome P450 Inducer Via the Constitutive Androstane Receptor and a Weak Inhibitor of CYP1A2. [PDF]
Clin Pharmacol Ther, 2021 Metamizole is an analgesic and antipyretic drug used intensively in certain countries. Previous studies have shown that metamizole induces cytochrome (CYP) 2B6 and possibly CYP3A4.
Bachmann F +6 more
europepmc +2 more sources
Application of humanized mice to toxicology studies: Evaluation of the human relevance of the mode of action for rodent liver tumor formation by activators of the constitutive androstane receptor (CAR). [PDF]
J Toxicol Pathol, 2021 The constitutive androstane receptor (CAR)-mediated mode of action (MOA) for phenobarbital (PB)-induced rodent liver tumor formation has been established, with increased hepatocyte proliferation, which is a key event in tumor formation.
Yamada T.
europepmc +2 more sources