Results 71 to 80 of about 69,599 (292)

Triclocarban mediates induction of xenobiotic metabolism through activation of the constitutive androstane receptor and the estrogen receptor alpha.

open access: yesPLoS ONE, 2012
Triclocarban (3,4,4'-trichlorocarbanilide, TCC) is used as a broad-based antimicrobial agent that is commonly added to personal hygiene products. Because of its extensive use in the health care industry and resistance to degradation in sewage treatment ...
Mei-Fei Yueh   +4 more
doaj   +1 more source

Tonic activation of extrasynaptic NMDA receptors decreases intrinsic excitability and promotes bistability in a model of neuronal activity [PDF]

open access: yesInt J Mol Sci. 2019 Dec 27;21(1). pii: E206, 2018
NMDA receptors (NMDA-R) typically contribute to excitatory synaptic transmission in the central nervous system. While calcium influx through NMDA-R plays a critical role in synaptic plasticity, experimental evidence indicates that NMDAR-mediated calcium influx also modifies neuronal excitability through the activation of calcium-activated potassium ...
arxiv   +1 more source

An optimized protocol with a stepwise approach to identify specific nuclear receptor ligands from cultured mammalian cells

open access: yesSTAR Protocols, 2021
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  

CAR Protects Females from Diet-Induced Steatosis and Associated Metabolic Disorders

open access: yesCells, 2023
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

Neuroreceptor Activation by Vibration-Assisted Tunneling [PDF]

open access: yesScientific Reports 5, Article number: 9990 Published 2015, 2015
G protein-coupled receptors (GPCRs) constitute a large family of receptor proteins that sense molecular signals on the exterior of a cell and activate signal transduction pathways within the cell. Modeling how an agonist activates such a receptor is fundamental for an understanding of a wide variety of physiological processes and it is of tremendous ...
arxiv   +1 more source

Deciphering the roles of the constitutive androstane receptor in energy metabolism [PDF]

open access: yesActa Pharmacologica Sinica, 2014
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.
Baian Chen, Jiong Yan, Jing Lu, Wen Xie
openaire   +3 more sources

Dietary Flavonoids Activate the Constitutive Androstane Receptor (CAR) [PDF]

open access: yesJournal of Agricultural and Food Chemistry, 2010
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 ...
Yoshionobu Kiso   +10 more
openaire   +2 more sources

Tomographic docking suggests the mechanism of auxin receptor TIR1 selectivity [PDF]

open access: yesOpen Biol. 6, 160139 (2016), 2016
We study the binding of plant hormone IAA on its receptor TIR1 introducing a novel computational method that we call tomographic docking and that accounts for interactions occurring along the depth of the binding pocket. Our results suggest that selectivity is related to constraints that potential ligands encounter on their way from the surface of the ...
arxiv   +1 more source

The Nuclear Receptor PXR in Chronic Liver Disease

open access: yesCells, 2021
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

Antiepileptic Drug–Activated Constitutive Androstane Receptor Inhibits Peroxisome Proliferator–Activated Receptor α and Peroxisome Proliferator–Activated Receptor γ Coactivator 1α–Dependent Gene Expression to Increase Blood Triglyceride Levels

open access: yesMolecular Pharmacology, 2020
Long-term administration of some antiepileptic drugs often increases blood lipid levels. In this study, we investigated its molecular mechanism by focusing on the nuclear receptors constitutive active/androstane receptor (CAR) and peroxisome proliferator–
R. Shizu   +12 more
semanticscholar   +1 more source

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