Deciphering the roles of the constitutive androstane receptor in energy metabolism [PDF]
The constitutive androstane receptor (CAR) is initially defined as a xenobiotic nuclear receptor that protects the liver from injury. Detoxification of damaging chemicals is achieved by CAR-mediated induction of drug-metabolizing enzymes and transporters.
Jiong, Yan +3 more
openaire +2 more sources
Role of metabolic nuclear receptors in acute liver injury and drug-induced hepatotoxicity
Metabolic nuclear receptors (NRs) are ligand-activated transcription factors central to metabolic homeostasis and detoxification. While their roles in chronic liver diseases have been reviewed, comprehensive reviews specifically addressing the role of ...
Liangliang Nie +4 more
doaj +1 more source
CAR Protects Females from Diet-Induced Steatosis and Associated Metabolic Disorders
Non-Alcoholic Fatty Liver Disease (NAFLD) is the most common cause of chronic liver disease worldwide, affecting 70–90% of obese individuals. In humans, a lower NAFLD incidence is reported in pre-menopausal women, although the mechanisms affording this ...
Fabiana Oliviero +8 more
doaj +1 more source
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
Constitutive Androstane Receptor 1 is Constitutively Bound to Chromatin and 'Primed' for Transactivation in Hepatocytes [PDF]
The constitutive androstane receptor (CAR) is a xenobiotic sensor expressed in hepatocytes that activates genes involved in drug metabolism, lipid homeostasis, and cell proliferation. Much progress has been made in understanding the mechanism of activation of human CAR by drugs and xenobiotics.
McMahon, Michael +8 more
openaire +3 more sources
The Nuclear Receptor PXR in Chronic Liver Disease
Pregnane X receptor (PXR), a nuclear receptor known for modulating the transcription of drug metabolizing enzymes and transporters (DMETs), such as cytochrome P450 3A4 and P-glycoprotein, is functionally involved in chronic liver diseases of different ...
Katia Sayaf +4 more
doaj +1 more source
Stereoselective Biotransformation: Transfer of Learning to Advance Drug Metabolism and Biocatalysis
Understanding stereoselective biotransformations has implications for predicting drug disposition and response and may also inspire novel biocatalytic and biomimetic strategies to address challenges in metabolite and API synthesis. ABSTRACT Chirality is an important determinant of drug action, as enantiomers can exhibit markedly different ...
Grace A. Okunlola, Godwin A. Aleku
wiley +2 more sources
This study introduces a modular microfluidic platform that connects liver cells with live microbes to mimic key aspects of the gut–liver interaction in steatosis. Using this system, both microbial metabolites and live bacteria significantly reduced fat accumulation in liver cells, but live microbes triggered inflammation and broader metabolic changes ...
Hsih‐Yin Tan +7 more
wiley +1 more source
Characterization of DNA Complexes Formed by the Nuclear Receptor Constitutive Androstane Receptor [PDF]
The nuclear receptor constitutive androstane receptor (CAR) acts as a xenobiotic sensor and regulates the expression of enzymes, such as several cytochromes P450s and the UDP-glucuronosyltransferase (UGT) type 1A1. CAR binds as a heterodimer with the retinoid X receptor (RXR) to specific DNA sites, called response elements (REs).
Christian, Frank +4 more
openaire +2 more sources
Transactivation Assays to Assess Canine and Rodent Pregnane X Receptor (PXR) and Constitutive Androstane Receptor (CAR) Activation. [PDF]
The pregnane X receptor (PXR/SXR, NR1I2) and constitutive androstane receptor (CAR, NR1I3) are nuclear receptors (NRs) involved in the regulation of many genes including cytochrome P450 enzymes (CYPs) and transporters important in metabolism and uptake ...
Marija Pinne, Elsa Ponce, Judy L Raucy
doaj +1 more source

