Results 11 to 20 of about 4,340 (154)

Constitutive androstane receptor and pregnane X receptor genotype influence efavirenz plasma concentration and CYP2B6 enzyme activity [PDF]

Scientific Reports, 2022
Efavirenz is metabolized by CYP2B6, an inducible enzyme whose expression is regulated by the constitutive androstane receptor and pregnane X receptor nuclear receptors. CAR and PXR are encoded by genetically polymorphic NR1I2 and NR1I3, respectively.
Zelalem Petros, Abiy Habtewold, Eyasu Makonnen, Eleni Aklillu   +3 more
doaj   +2 more sources

Pharmacological activation of constitutive androstane receptor induces female-specific modulation of hepatic metabolism [PDF]

JHEP Reports
Background & Aims: The constitutive androstane receptor (CAR) is a nuclear receptor that binds diverse xenobiotics and whose activation leads to the modulation of the expression of target genes involved in xenobiotic detoxification and energy ...
Marine Huillet, Frédéric Lasserre, Marie-Pierre Gratacap, Beatrice Engelmann, Justine Bruse, Arnaud Polizzi, Tiffany Fougeray, Céline Marie Pauline Martin, Clémence Rives, Anne Fougerat, Claire Naylies, Yannick Lippi, Géraldine Garcia, Elodie Rousseau-Bacquie, Cécile Canlet, Laurent Debrauwer, Ulrike Rolle-Kampczyk, Martin von Bergen, Bernard Payrastre, Elisa Boutet-Robinet, Laurence Gamet-Payrastre, Hervé Guillou, Nicolas Loiseau, Sandrine Ellero-Simatos   +23 more
doaj   +2 more sources

Gadd45b is required in part for the anti-obesity effect of constitutive androstane receptor (CAR) [PDF]

Acta Pharmaceutica Sinica B, 2021
Crosstalk between xenobiotic metabolism and energy metabolism in the liver has provided a potential opportunity to target xenobiotic receptors to treat metabolic diseases. Activation of constitutive androstane receptor (CAR), a xenobiotic-sensing nuclear
Xinran Cai, Ye Feng, Meishu Xu, Chaohui Yu, Wen Xie   +4 more
doaj   +2 more sources

Constitutive Androstane Receptor-Mediated Inhibition of Metformin on Phase II Metabolic Enzyme SULT2A1 [PDF]

International Journal of Endocrinology, 2021
Background. Metformin, as a first-line treatment for diabetes, interacts with many protein kinases and transcription factors which affect the expression of downstream target genes governing drug metabolism.
Xiaowen Hu, Mengsiyu Li, Chunxue Zhang, Shuguang Pang   +3 more
doaj   +2 more sources

Constitutive androstane receptor induced-hepatomegaly and liver regeneration is partially via yes-associated protein activation [PDF]

Acta Pharmaceutica Sinica B, 2021
The constitutive androstane receptor (CAR, NR3I1) belongs to nuclear receptor superfamily. It was reported that CAR agonist TCPOBOP induces hepatomegaly but the underlying mechanism remains largely unknown.
Yue Gao, Shicheng Fan, Hua Li, Yiming Jiang, Xinpeng Yao, Shuguang Zhu, Xiao Yang, Ruimin Wang, Jianing Tian, Frank J. Gonzalez, Min Huang, Huichang Bi   +11 more
doaj   +2 more sources

The Use of the LanthaScreen TR-FRET CAR Coactivator Assay in the Characterization of Constitutive Androstane Receptor (CAR) Inverse Agonists

Sensors, 2015
The constitutive androstane receptor (CAR) is a critical nuclear receptor in the gene regulation of xenobiotic and endobiotic metabolism. The LanthaScreenTM TR-FRET CAR coactivator assay provides a simple and reliable method to analyze the affinity of a ...
Alejandro Carazo, Petr Pávek
doaj   +3 more sources

Liver matrin-3 protects mice against hepatic steatosis and stress response via constitutive androstane receptor [PDF]

Molecular Metabolism
Objective: The prevalence of metabolic dysfunction-associated steatotic liver disease (MASLD) continues to rise with the increasing obesity epidemic. Rezdiffra as an activator of a thyroid hormone receptor-beta is the only Food and Drug Administration ...
Xiao Cheng, Vijaya Bhaskar Baki, Matthew Moran, Baolong Liu, Jiujiu Yu, Miaoyun Zhao, Qingsheng Li, Jean-Jack Riethoven, Channabasavaiah B. Gurumurth, Edward N. Harris, Xinghui Sun   +10 more
doaj   +2 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. However, currently available human CAR (hCAR) agonists are nonselective, which commonly activate hCAR along with other nuclear receptors, especially the closely related human ...
Liang D, Li L, Lynch C, Diethelm-Varela B, Xia M, Xue F, Wang H.   +6 more
europepmc   +4 more sources

Binding modes and interaction mechanism of bisphenol A and its analogs in constitutive androstane receptor [PDF]

Scientific Reports
Environmental pollutants, such as bisphenol A (BPA) and its analogs, are key molecules in the production of commercial products that are used in daily life, posing a threat to human health.
Manikandan Jayaraman, Vijayakumar Gosu, Maharaja Muthuvairam Subbulakshmi, Jeong Woong Park, Jeyakanthan Jeyaraman, Donghyun Shin   +5 more
doaj   +2 more sources

β-catenin signaling, the constitutive androstane receptor and their mutual interactions. [PDF]

Arch Toxicol, 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 ...
Braeuning A, Pavek P.
europepmc   +4 more sources