Literature DB >> 25979168

Small-molecule modulators of the constitutive androstane receptor.

Milu T Cherian1, Sergio C Chai, Taosheng Chen.   

Abstract

INTRODUCTION: The constitutive androstane receptor (CAR) induces drug-metabolizing enzymes for xenobiotic metabolism. AREAS COVERED: This review covers recent advances in elucidating the biological functions of CAR and its modulation by a growing number of agonists and inhibitors. EXPERT OPINION: Extrapolation of animal CAR function to that of humans should be carefully scrutinized, particularly when rodents are used in evaluating the metabolic profile and carcinogenic properties of clinical drugs and environmental chemicals. Continuous efforts are needed to discover novel CAR inhibitors, with extensive understanding of their inhibitory mechanism, species selectivity, and discriminating power against other xenobiotic sensors.

Entities:  

Keywords:  constitutive androstane receptor; drug–drug interactions; small-molecule; xenobiotic metabolism

Mesh：

Substances：

Year:  2015        PMID： 25979168      PMCID： PMC4469626          DOI： 10.1517/17425255.2015.1043887

Source DB:  PubMed          Journal:  Expert Opin Drug Metab Toxicol        ISSN： 1742-5255            Impact factor:   4.481


  162 in total

1.  The nuclear xenobiotic receptor CAR: structural determinants of constitutive activation and heterodimerization.

Authors:  Kelly Suino; Li Peng; Ross Reynolds; Yong Li; Ji-Young Cha; Joyce J Repa; Steven A Kliewer; H Eric Xu
Journal:  Mol Cell       Date:  2004-12-22       Impact factor: 17.970

2.  Phenobarbital indirectly activates the constitutive active androstane receptor (CAR) by inhibition of epidermal growth factor receptor signaling.

Authors:  Shingo Mutoh; Mack Sobhany; Rick Moore; Lalith Perera; Lee Pedersen; Tatsuya Sueyoshi; Masahiko Negishi
Journal:  Sci Signal       Date:  2013-05-07       Impact factor: 8.192

3.  The commonly used antimicrobial additive triclosan is a liver tumor promoter.

Authors:  Mei-Fei Yueh; Koji Taniguchi; Shujuan Chen; Ronald M Evans; Bruce D Hammock; Michael Karin; Robert H Tukey
Journal:  Proc Natl Acad Sci U S A       Date:  2014-11-17       Impact factor: 11.205

4.  Retinoid X receptor-alpha-dependent transactivation by a naturally occurring structural variant of human constitutive androstane receptor (NR1I3).

Authors:  Scott S Auerbach; Matthew A Stoner; Shengzhong Su; Curtis J Omiecinski
Journal:  Mol Pharmacol       Date:  2005-08-11       Impact factor: 4.436

5.  New in vitro tools to study human constitutive androstane receptor (CAR) biology: discovery and comparison of human CAR inverse agonists.

Authors:  Jenni Küblbeck; Johanna Jyrkkärinne; Ferdinand Molnár; Tiina Kuningas; Jayendra Patel; Björn Windshügel; Tapio Nevalainen; Tuomo Laitinen; Wolfgang Sippl; Antti Poso; Paavo Honkakoski
Journal:  Mol Pharm       Date:  2011-11-01       Impact factor: 4.939

6.  Regulation of human hepatic hydroxysteroid sulfotransferase gene expression by the peroxisome proliferator-activated receptor alpha transcription factor.

Authors:  Hai-Lin Fang; Stephen C Strom; Hongbo Cai; Charles N Falany; Thomas A Kocarek; Melissa Runge-Morris
Journal:  Mol Pharmacol       Date:  2005-01-05       Impact factor: 4.436

7.  Association of a single nucleotide polymorphism in the constitutive androstane receptor gene with bone mineral density.

Authors:  Tomohiko Urano; Takahiko Usui; Masataka Shiraki; Yasuyoshi Ouchi; Satoshi Inoue
Journal:  Geriatr Gerontol Int       Date:  2009-09       Impact factor: 2.730

8.  The orphan nuclear receptor HNF4alpha determines PXR- and CAR-mediated xenobiotic induction of CYP3A4.

Authors:  Rommel G Tirona; Wooin Lee; Brenda F Leake; Lu-Bin Lan; Cynthia Brimer Cline; Vishal Lamba; Fereshteh Parviz; Stephen A Duncan; Yusuke Inoue; Frank J Gonzalez; Erin G Schuetz; Richard B Kim
Journal:  Nat Med       Date:  2003-01-06       Impact factor: 53.440

9.  Endocrine disruptors induce cytochrome P450 by affecting transcriptional regulation via pregnane X receptor.

Authors:  Eriko Mikamo; Shingo Harada; Jun-ichi Nishikawa; Tsutomu Nishihara
Journal:  Toxicol Appl Pharmacol       Date:  2003-11-15       Impact factor: 4.219

10.  A PXR reporter gene assay in a stable cell culture system: CYP3A4 and CYP2B6 induction by pesticides.

Authors:  Géraldine Lemaire; Georges de Sousa; Roger Rahmani
Journal:  Biochem Pharmacol       Date:  2004-12-15       Impact factor: 5.858
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  11 in total

1.  Lack of CAR impacts neuronal function and cerebrovascular integrity in vivo.

Authors:  Baddreddine Boussadia; Giuseppe Gangarossa; Laila Mselli-Lakhal; Marie-Claude Rousset; Frederic de Bock; Frederic Lassere; Chaitali Ghosh; Jean-Marc Pascussi; Damir Janigro; Nicola Marchi
Journal:  Exp Neurol       Date:  2016-05-27       Impact factor: 5.330

2.  Occurrence and assessment of the risk of ultraviolet filters and light stabilizers in Victorian estuaries.

Authors:  Mayumi Allinson; Yutaka Kameda; Kumiko Kimura; Graeme Allinson
Journal:  Environ Sci Pollut Res Int       Date:  2018-02-16       Impact factor: 4.223

3.  DL5050, a Selective Agonist for the Human Constitutive Androstane Receptor.

Authors:  Dongdong Liang; Linhao Li; Caitlin Lynch; Benjamin Diethelm-Varela; Menghang Xia; Fengtian Xue; Hongbing Wang
Journal:  ACS Med Chem Lett       Date:  2019-06-12       Impact factor: 4.345

4.  How similar is similar enough? A sufficient similarity case study with Ginkgo biloba extract.

Authors:  Natasha R Catlin; Bradley J Collins; Scott S Auerbach; Stephen S Ferguson; James M Harnly; Chris Gennings; Suramya Waidyanatha; Glenn E Rice; Stephanie L Smith-Roe; Kristine L Witt; Cynthia V Rider
Journal:  Food Chem Toxicol       Date:  2018-05-09       Impact factor: 6.023

Review 5.  A current structural perspective on PXR and CAR in drug metabolism.

Authors:  Cameron D Buchman; Sergio C Chai; Taosheng Chen
Journal:  Expert Opin Drug Metab Toxicol       Date:  2018-05-30       Impact factor: 4.481

6.  Sex-Differential Responses of Tumor Promotion-Associated Genes and Dysregulation of Novel Long Noncoding RNAs in Constitutive Androstane Receptor-Activated Mouse Liver.

Authors:  Nicholas J Lodato; Tisha Melia; Andy Rampersaud; David J Waxman
Journal:  Toxicol Sci       Date:  2017-09-01       Impact factor: 4.849

7.  Identification and Characterization of CINPA1 Metabolites Facilitates Structure-Activity Studies of the Constitutive Androstane Receptor.

Authors:  Milu T Cherian; Lei Yang; Sergio C Chai; Wenwei Lin; Taosheng Chen
Journal:  Drug Metab Dispos       Date:  2016-08-12       Impact factor: 3.922

Review 8.  Hepatotoxicity of Herbal Supplements Mediated by Modulation of Cytochrome P450.

Authors:  Christopher Trent Brewer; Taosheng Chen
Journal:  Int J Mol Sci       Date:  2017-11-08       Impact factor: 5.923

Review 9.  The Role of PPAR and Its Cross-Talk with CAR and LXR in Obesity and Atherosclerosis.

Authors:  Pengfei Xu; Yonggong Zhai; Jing Wang
Journal:  Int J Mol Sci       Date:  2018-04-23       Impact factor: 5.923

Review 10.  Nuclear Receptor Metabolism of Bile Acids and Xenobiotics: A Coordinated Detoxification System with Impact on Health and Diseases.

Authors:  Manon Garcia; Laura Thirouard; Lauriane Sedès; Mélusine Monrose; Hélène Holota; Françoise Caira; David H Volle; Claude Beaudoin
Journal:  Int J Mol Sci       Date:  2018-11-17       Impact factor: 5.923
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