Discovery of Novel Human Constitutive Androstane Receptor Agonists with the Imidazo[1,2-a]pyridine Structure

Targeting CAR-Nrf2 improves cyclophosphamide bioactivation while reducing doxorubicin-induced cardiotoxicity in triple-negative breast cancer treatment

(2022) Sydney Stern et al.   JCI Insight

(E)-7-Ethylidene-lithocholic Acid (7-ELCA) Is a Potent Dual Farnesoid X Receptor (FXR) Antagonist and GPBAR1 Agonist Inhibiting FXR-Induced Gene Expression in Hepatocytes and Stimulating Glucagon-like Peptide-1 Secretion From Enteroendocrine Cells

(2021) Alzbeta Stefela et al.   Frontiers in Pharmacology

Diazepam Promotes Translocation of Human Constitutive Androstane Receptor (CAR) via Direct Interaction with the Ligand-Binding Domain

(2020) Josef Skoda et al.   Cells

Drug discovery technologies to identify and characterize modulators of the pregnane X receptor and the constitutive androstane receptor

(2019) Sergio C. Chai et al.   DRUG DISCOVERY TODAY

Identification of novel agonists by high-throughput screening and molecular modelling of human constitutive androstane receptor isoform 3

(2019) Oliver Keminer et al.   ARCHIVES OF TOXICOLOGY

DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor

(2019) Dongdong Liang et al.   ACS Medicinal Chemistry Letters

High-content analysis of constitutive androstane receptor (CAR) translocation identifies mosapride citrate as a CAR agonist that represses gluconeogenesis

(2019) Bryan Mackowiak et al.   BIOCHEMICAL PHARMACOLOGY

Human constitutive androstane receptor agonist DL5016: A novel sensitizer for cyclophosphamide-based chemotherapies

(2019) Dongdong Liang et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Stilbene compound trans-3,4,5,4´-tetramethoxystilbene, a potential anticancer drug, regulates constitutive androstane receptor (Car) target genes, but does not possess proliferative activity in mouse liver

(2019) Jan Dusek et al.   TOXICOLOGY LETTERS

CITCO Directly Binds to and Activates Human Pregnane X Receptor

(2019) Wenwei Lin et al.   MOLECULAR PHARMACOLOGY

Cytochrome P450 Induction and Xeno-Sensing Receptors Pregnane X Receptor, Constitutive Androstane Receptor, Aryl Hydrocarbon Receptor and Peroxisome Proliferator-Activated Receptor α at the Crossroads of Toxicokinetics and Toxicodynamics

(2018) Jukka Hakkola et al.   BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY

The Roles of Xenobiotic Receptors: Beyond Chemical Disposition

(2018) Bryan Mackowiak et al.   DRUG METABOLISM AND DISPOSITION

Steviol, an aglycone of steviol glycoside sweeteners, interacts with the pregnane X (PXR) and aryl hydrocarbon (AHR) receptors in detoxification regulation

(2017) Jan Dusek et al.   FOOD AND CHEMICAL TOXICOLOGY

Mechanisms of xenobiotic receptor activation: Direct vs. indirect

(2016) Bryan Mackowiak et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

Small-molecule modulators of PXR and CAR

(2016) Sergio C. Chai et al.   Biochimica et Biophysica Acta-Gene Regulatory Mechanisms

The pregnane X receptor down-regulates organic cation transporter 1 (SLC22A1) in human hepatocytes by competing for (“squelching”) SRC-1 coactivator

(2016) Lucie Hyrsova et al.   BRITISH JOURNAL OF PHARMACOLOGY

Constitutive androstane receptor (Car)-driven regeneration protects liver from failure following tissue loss

(2016) Christoph Tschuor et al.   JOURNAL OF HEPATOLOGY

2-(3-Methoxyphenyl)quinazoline Derivatives: A New Class of Direct Constitutive Androstane Receptor (CAR) Agonists

(2016) Tomas Smutny et al.   JOURNAL OF MEDICINAL CHEMISTRY

Activation of the Constitutive Androstane Receptor induces hepatic lipogenesis and regulates Pnpla3 gene expression in a LXR-independent way

(2016) Alice Marmugi et al.   TOXICOLOGY AND APPLIED PHARMACOLOGY

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

(2015) Alejandro Carazo et al.   SENSORS

Role of the constitutive androstane receptor in obesity and type 2 diabetes: a case study of the endobiotic function of a xenobiotic receptor

(2013) Mengxi Jiang et al.   DRUG METABOLISM REVIEWS

Differential effects of clinically used derivatives and metabolites of artemisinin in the activation of constitutive androstane receptor isoforms

(2012) O Burk et al.   BRITISH JOURNAL OF PHARMACOLOGY

Novel Cell-based Reporter Assay System Using Epitope-tagged Protein for the Identification of Agonistic Ligands of Constitutive Androstane Receptor (CAR)

(2012) Jun Imai et al.   Drug Metabolism and Pharmacokinetics

Identification of Novel Activators of Constitutive Androstane Receptor from FDA-Approved Drugs by Integrated Computational and Biological Approaches

(2012) Caitlin Lynch et al.   PHARMACEUTICAL RESEARCH

Targeting xenobiotic receptors PXR and CAR for metabolic diseases

(2012) Jie Gao et al.   TRENDS IN PHARMACOLOGICAL SCIENCES

Use of comprehensive screening methods to detect selective human CAR activators

(2011) Jenni Küblbeck et al.   BIOCHEMICAL PHARMACOLOGY

Newin VitroTools to Study Human Constitutive Androstane Receptor (CAR) Biology: Discovery and Comparison of Human CAR Inverse Agonists

(2011) Jenni Küblbeck et al.   MOLECULAR PHARMACEUTICS

Rational quantitative structure–activity relationship (RQSAR) screen for PXR and CAR isoform-specific nuclear receptor ligands

(2010) Ann M. Dring et al.   CHEMICO-BIOLOGICAL INTERACTIONS

Hepatic Expression of Thyroid Hormone-Responsive Spot 14 Protein Is Regulated by Constitutive Androstane Receptor (NR1I3)

(2010) Cyril Breuker et al.   ENDOCRINOLOGY

Human Constitutive Androstane Receptor (CAR) and Pregnane X Receptor (PXR) Support the Hypertrophic but not the Hyperplastic Response to the Murine Nongenotoxic Hepatocarcinogens Phenobarbital and Chlordane In Vivo

(2010) Jillian Ross et al.   TOXICOLOGICAL SCIENCES

Intestinal cell-specific vitamin D receptor (VDR)-mediated transcriptional regulation of CYP3A4 gene

(2009) Petr Pavek et al.   BIOCHEMICAL PHARMACOLOGY

Effect of CAR activation on selected metabolic pathways in normal and hyperlipidemic mouse livers

(2009) Tadeja Režen et al.   BMC GENOMICS

Nuclear Translocation of Adenoviral-Enhanced Yellow Fluorescent Protein-Tagged-Human Constitutive Androstane Receptor (hCAR): A Novel Tool for Screening hCAR Activators in Human Primary Hepatocytes

(2009) H. Li et al.   DRUG METABOLISM AND DISPOSITION

The Constitutive Androstane Receptor Is an Anti-obesity Nuclear Receptor That Improves Insulin Sensitivity

(2009) Jie Gao et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

A Single Amino Acid Controls the Functional Switch of Human Constitutive Androstane Receptor (CAR) 1 to the Xenobiotic-Sensitive Splicing Variant CAR3

(2009) T. Chen et al.   JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS

Activation of nuclear receptor CAR ameliorates diabetes and fatty liver disease

(2009) B. Dong et al.   PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA

The nuclear receptor CAR (NR1I3) regulates serum triglyceride levels under conditions of metabolic stress

(2008) Jodi M. Maglich et al.   JOURNAL OF LIPID RESEARCH

Insights into Ligand-Elicited Activation of Human Constitutive Androstane Receptor Based on Novel Agonists and Three-Dimensional Quantitative Structure−Activity Relationship

(2008) Johanna Jyrkkärinne et al.   JOURNAL OF MEDICINAL CHEMISTRY

The Peripheral Benzodiazepine Receptor Ligand 1-(2-Chlorophenyl-methylpropyl)-3-isoquinoline-carboxamide Is a Novel Antagonist of Human Constitutive Androstane Receptor

(2008) L. Li et al.   MOLECULAR PHARMACOLOGY