2-Substituted quinazolines: Partial agonistic and antagonistic ligands of the constitutive androstane receptor (CAR)

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

(2023) Ivana Mejdrová et al.   Journal of Medicinal Chemistry

Steatosis and Metabolic Disorders Associated with Synergistic Activation of the CAR/RXR Heterodimer by Pesticides

(2023) Yannick Dauwe et al.   Cells

Searching for CAR modulators

(2022) Paavo Honkakoski   DRUG METABOLISM AND DISPOSITION

Nuclear Receptor PXR in Drug-Induced Hypercholesterolemia

(2022) Mikko Karpale et al.   Cells

Clinical relevance of the constitutive androstane receptor

(2022) Sydney Stern et al.   DRUG METABOLISM AND DISPOSITION

Highly accurate protein structure prediction with AlphaFold

(2021) John Jumper et al.   NATURE

Nuclear receptor phosphorylation in xenobiotic signal transduction

(2020) Masahiko Negishi et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Synthesis of Quinazoline and Quinazolinone Derivatives via Ligand-Promoted Ruthenium-Catalyzed Dehydrogenative and Deaminative Coupling Reaction of 2-Aminophenyl Ketones and 2-Aminobenzamides with Amines

(2019) Pandula T. Kirinde Arachchige et al.   ORGANIC LETTERS

Metal–Ligand Cooperative Approach To Achieve Dehydrogenative Functionalization of Alcohols to Quinolines and Quinazolin-4(3H)-ones under Mild Aerobic Conditions

(2019) Siuli Das et al.   JOURNAL OF ORGANIC CHEMISTRY

Regulatory Mechanics of Constitutive Androstane Receptors: Basal and Ligand-Directed Actions

(2019) Bill Pham et al.   Journal of Chemical Information and Modeling

The 3ʹ-untranslated region contributes to the pregnane X receptor (PXR) expression down-regulation by PXR ligands and up-regulation by glucocorticoids

(2019) Tomas Smutny et al.   Acta Pharmaceutica Sinica B

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

Palladium-Catalyzed Oxidative Three-Component Coupling of Anthranilamides with Isocyanides and Arylboronic Acids: Access to 2,3-Disubstituted Quinazolinones

(2018) Chun Qian et al.   JOURNAL OF ORGANIC CHEMISTRY

Synthesis of 2-Aminobenzonitriles through Nitrosation Reaction and Sequential Iron(III)-Catalyzed C–C Bond Cleavage of 2-Arylindoles

(2018) Wei-Li Chen et al.   ORGANIC LETTERS

The role of xenobiotic receptors on hepatic glycolipid metabolism

(2018) Ke Chen et al.   CURRENT DRUG METABOLISM

Palladium-catalyzed oxidative CC bond cleavage with molecular oxygen: one-pot synthesis of quinazolinones from 2-amino benzamides and alkenes

(2018) Wei Liu et al.   Organic Chemistry Frontiers

Microwave-assisted synthesis of quinazolin-4(3H)-ones catalyzed by SbCl3

(2018) Huaiyuan Kang et al.   HETEROCYCLIC COMMUNICATIONS

Synthesis and Antimicrobial Activity of Methyl 2‐(2‐(2‐Arylquinazolin‐4‐yl)sulfanyl)acetylamino Alkanoates

(2018) M. I. Megahed et al.   JOURNAL OF HETEROCYCLIC CHEMISTRY

Teriflunomide Is an Indirect Human Constitutive Androstane Receptor (CAR) Activator Interacting With Epidermal Growth Factor (EGF) Signaling

(2018) Alejandro Carazo et al.   Frontiers in Pharmacology

Iron-catalyzed one-pot sequential transformations: Synthesis of quinazolinones via oxidative Csp3H bond activation using a new metal-organic framework as catalyst

(2018) Tuong A. To et al.   JOURNAL OF CATALYSIS

Synthesis and biological investigation of 2,4-substituted quinazolines as highly potent inhibitors of breast cancer resistance protein (ABCG2)

(2017) Michael K. Krapf et al.   EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY

Phosphorylated Nuclear Receptor CAR Forms a Homodimer To Repress Its Constitutive Activity for Ligand Activation

(2017) Ryota Shizu et al.   MOLECULAR AND CELLULAR BIOLOGY

Metal-Free Ionic-Liquid-Mediated Synthesis of Benzimidazoles and Quinazolin-4(3H )-ones from Benzylamines

(2017) Rohit Sharma et al.   Asian Journal of Organic Chemistry

SwissADME: a free web tool to evaluate pharmacokinetics, drug-likeness and medicinal chemistry friendliness of small molecules

(2017) Antoine Daina et al.   Scientific Reports

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

2-Amino[1,2,4]triazolo[1,5-c]quinazolines and Derived Novel Heterocycles: Syntheses and Structure-Activity Relationships of Potent Adenosine Receptor Antagonists

(2016) Joachim C. Burbiel et al.   ChemMedChem

Synthesis of 2,3-Disubstituted Quinazolinone Derivatives through Copper Catalyzed C-H Amidation Reactions

(2016) Trimurtulu Kotipalli et al.   EUROPEAN JOURNAL OF ORGANIC CHEMISTRY

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

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

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

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

Quinazoline Synthesis via Rh(III)-Catalyzed Intermolecular C–H Functionalization of Benzimidates with Dioxazolones

(2016) Jie Wang et al.   ORGANIC LETTERS

Pd/Fe3O4 supported on nitrogen-doped reduced graphene oxide for room-temperature isocyanide insertion reactions

(2016) Karandeep Singh et al.   Catalysis Science & Technology

2-Alkyl(aryl)-quinazolin-4(3H)-thiones, 2-R-(quinazolin-4(3H)-ylthio)carboxylic acids and amides: synthesis, molecular docking, antimicrobial and anticancer properties

(2015) Lyudmyla Antypenko et al.   JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY

CAR Suppresses Hepatic Gluconeogenesis by Facilitating the Ubiquitination and Degradation of PGC1α

(2015) Jie Gao et al.   MOLECULAR ENDOCRINOLOGY

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

Chrysin, baicalein and galangin are indirect activators of the human constitutive androstane receptor (CAR)

(2015) Alejandro Carazo Fernández et al.   TOXICOLOGY LETTERS

Deciphering the roles of the constitutive androstane receptor in energy metabolism

(2014) Jiong Yan et al.   ACTA PHARMACOLOGICA SINICA

Synthesis and Anticonvulsant Activity Evaluation of 5-Phenyl-[1,2,4]triazolo[4,3-c]quinazolin-3-amines

(2012) Yan Zheng et al.   ARCHIV DER PHARMAZIE

The unambiguous synthesis and NMR assignment of 4-alkoxy and 3-alkylquinazolines

(2012) Marcel Špulák et al.   TETRAHEDRON

Targeting xenobiotic receptors PXR and CAR for metabolic diseases

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

Constitutive androstane receptor agonist CITCO inhibits growth and expansion of brain tumour stem cells

(2011) S Chakraborty et al.   BRITISH JOURNAL OF CANCER

Constitutive androstane receptor activation stimulates faecal bile acid excretion and reverse cholesterol transport in mice

(2010) Anne Laure Sberna et al.   JOURNAL OF HEPATOLOGY

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

(2009) Tadeja Režen et al.   BMC GENOMICS

Dephosphorylation of Threonine 38 Is Required for Nuclear Translocation and Activation of Human Xenobiotic Receptor CAR (NR1I3)

(2009) Shingo Mutoh et al.   JOURNAL OF BIOLOGICAL CHEMISTRY

Nuclear receptors CAR and PXR: Molecular, functional, and biomedical aspects

(2009) Alessandra di Masi et al.   MOLECULAR ASPECTS OF MEDICINE

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 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