Results 11 to 20 of about 69,599 (292)
Metabolism-Disrupting Chemicals and the Constitutive Androstane Receptor CAR [PDF]
Cells, 2020 During the last two decades, the constitutive androstane receptor (CAR; NR1I3) has emerged as a master activator of drug- and xenobiotic-metabolizing enzymes and transporters that govern the clearance of both exogenous and endogenous small molecules.
Jonna Niskanen +3 more
doaj +8 more sources
Constitutive Androstane Receptor: A Peripheral and a Neurovascular Stress or Environmental Sensor [PDF]
Cells, 2020 Xenobiotic nuclear receptors (NR) are intracellular players involved in an increasing number of physiological processes. Examined and characterized in peripheral organs where they govern metabolic, transport and detoxification mechanisms, accumulating data suggest a functional expression of specific NR at the neurovascular unit (NVU). Here, we focus on
Oliviero, Fabiana +6 more
doaj +10 more sources
Clinical Relevance of the Constitutive Androstane Receptor [PDF]
Drug Metabolism and Disposition, 2022 Constitutive androstane receptor (CAR) (NR1I3), a xenobiotic receptor, has long been considered a master mediator of drug disposition and detoxification. Accumulating evidence indicates that CAR also participates in various physiologic and pathophysiological pathways regulating the homeostasis of glucose, lipid, and bile acids, and contributing to cell
Sydney, Stern +2 more
europepmc +4 more sources
Activation of the Constitutive Androstane Receptor Inhibits Leukocyte Adhesiveness to Dysfunctional Endothelium [PDF]
International Journal of Molecular Sciences, 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 study investigated whether the role of CAR activation can affect this response and the underlying ...
Mireia López-Riera +7 more
europepmc +8 more sources
Transporter Gene Regulation in Sandwich Cultured Human Hepatocytes Through the Activation of Constitutive Androstane Receptor (CAR) or Aryl Hydrocarbon Receptor (AhR) [PDF]
Frontiers in Pharmacology, 2021 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 +3 more sources
The constitutive androstane receptor and pregnane X receptor in the brain [PDF]
British Journal of Pharmacology, 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. They regulate the metabolism and transport of endogenous mediators and xenobiotics in organs including the liver, intestine and ...
Francisca Espinoza +6 more
europepmc +5 more sources
Noncanonical Constitutive Androstane Receptor Signaling in Gene Regulation [PDF]
International Journal of Molecular Sciences, 2020 The constitutive androstane receptor (CAR, NR1I3) is extremely important for the regulation of many physiological processes, especially xenobiotic (drug) metabolism and transporters. CAR differs from steroid hormone receptors in that it can be activated using structurally unrelated chemicals, both through direct ligand-binding and ligand-independent ...
Yuliya A. Pustylnyak +2 more
europepmc +4 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. In this study, sixty courmarin derivatives either synthesized or purified from Artemisia capillaris were screened for CAR ...
Chen Hsi Chou +12 more
doaj +5 more sources
Constitutive Androstane Receptor Regulates Germ Cell Homeostasis, Sperm Quality, and Male Fertility via Akt‐Foxo1 Pathway [PDF]
Advanced Science, Volume 11, Issue 43, November 20, 2024.This study highlights the role of the constitutive androstane receptor (Car), a receptor of endo and xeno‐biotics, in testicular pathophysiology. The results indicate that Car inhibition impaired male fertility due to altered sperm quality, specifically histone retention, which is correlated with offspring's survival. This work demonstrates that Car is
Mélusine Monrose +16 more
wiley +3 more sources
β-catenin signaling, the constitutive androstane receptor and their mutual interactions [PDF]
Archives of Toxicology, 2020 AbstractAberrant signaling through β-catenin is an important determinant of tumorigenesis in rodents as well as in humans. In mice, xenobiotic activators of the constitutive androstane receptor (CAR), a chemo-sensing nuclear receptor, promote liver tumor growth by means of a non-genotoxic mechanism and, under certain conditions, select for ...
Albert Braeuning, Petr Pavek
europepmc +5 more sources