Results 11 to 20 of about 5,156 (193)

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   +5 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

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

PLoS 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, Tao Li, Ronald M Evans, Bruce Hammock, Robert H Tukey   +4 more
doaj   +2 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

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

Constitutive androstane receptor (CAR) functions as a tumor suppressor via regulating stemness in liver cancer [PDF]

Scientific Reports
Constitutive androstane receptor (CAR) is a xenosensor that is almost exclusively expressed in the liver. Studies in rodents suggest an oncogenic role for CAR in liver cancer, but its role in human liver cancer is unclear.
Sarah Da Won Bae, Romario Nguyen, Lawrence Yuen, Vincent Lam, Jacob George, Liang Qiao   +5 more
doaj   +2 more sources

Transcriptomic analysis across liver diseases reveals disease-modulating activation of constitutive androstane receptor in cholestasis [PDF]

JHEP Reports, 2020
Background & Aims: Liver diseases are caused by many factors, such as genetics, nutrition, and viruses. Therefore, it is important to delineate transcriptomic changes that occur in various liver diseases.
Bhoomika Mathur, Waqar Arif, Megan E. Patton, Rahiman Faiyaz, Jian Liu, Jennifer Yeh, Sanjiv Harpavat, Kristina Schoonjans, Auinash Kalsotra, Antony M. Wheatley, Sayeepriyadarshini Anakk   +10 more
doaj   +2 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