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 ...
Jenni Küblbeck +2 more
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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 ...
Fabiana Oliviero +6 more
doaj +9 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
Clinical Relevance of the Constitutive Androstane Receptor. [PDF]
Drug Metab Dispos, 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
Stern S, Kurian R, Wang H.
europepmc +4 more sources
Constitutive androstane receptor, liver pathophysiology and chemical contaminants: current evidence and perspectives [PDF]
Frontiers in EndocrinologyIntroductionThe Constitutive Androstane Receptor (CAR) (NR1I3), a pivotal member of the xenosensor family, plays a key role in the hepatic detoxification of xenobiotic and endobiotic chemicals through the induction of the expression of drug-metabolizing ...
Francesca De Battistis +4 more
doaj +2 more sources
Small-molecule modulators of the constitutive androstane receptor [PDF]
Expert Opinion on Drug Metabolism and Toxicology, 2015 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 ...
Taosheng Chen, Sérgio C Chai
exaly +3 more sources
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 +2 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. They regulate the metabolism and transport of endogenous mediators and xenobiotics in organs including the liver, intestine and ...
Torres-Vergara P +5 more
europepmc +4 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. CAR differs from steroid hormone receptors in that it can be activated using structurally unrelated chemicals, both through direct ligand-binding and ligand-independent ...
Pustylnyak YA +2 more
europepmc +4 more sources
Constitutive Androstane Receptor Regulates Germ Cell Homeostasis, Sperm Quality, and Male Fertility via Akt‐Foxo1 Pathway [PDF]
Advanced ScienceMale sexual function can be disrupted by exposure to exogenous compounds that cause testicular physiological alterations. The constitutive androstane receptor (Car) is a receptor for both endobiotics and xenobiotics involved in detoxification.
Mélusine Monrose +16 more
doaj +2 more sources