Small-molecule Modulators of the Constitutive Androstane Receptor

Overview

Journal Expert Opin Drug Metab Toxicol

Publisher Informa Healthcare

Specialties Endocrinology
Pharmacology
Toxicology

Date 2015 May 17

PMID 25979168

Citations 15

Authors

Milu T Cherian

Sergio C Chai

Taosheng Chen

Affiliations

Soon will be listed here.

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.

Citing Articles

Gut microbiota trigger host liver immune responses that affect drug-metabolising enzymes.

Rao J, Qiu P, Zhang Y, Wang X Front Immunol. 2024; 15:1511229.

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Constitutive Androstane Receptor Regulates Germ Cell Homeostasis, Sperm Quality, and Male Fertility via Akt-Foxo1 Pathway.

Monrose M, Holota H, Martinez G, Damon-Soubeyrand C, Thirouard L, Martinot E Adv Sci (Weinh). 2024; 11(43):e2402082.

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Diindoles produced from commensal microbiota metabolites function as endogenous CAR/Nr1i3 ligands.

Liu J, Malekoltojari A, Asokakumar A, Chow V, Li L, Li H Nat Commun. 2024; 15(1):2563.

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

Dauwe Y, Mary L, Oliviero F, Grimaldi M, Balaguer P, Gayrard V Cells. 2023; 12(8).

PMID: 37190111 PMC: 10137125. DOI: 10.3390/cells12081201.

Prediction Model with High-Performance Constitutive Androstane Receptor (CAR) Using DeepSnap-Deep Learning Approach from the Tox21 10K Compound Library.

Matsuzaka Y, Uesawa Y Int J Mol Sci. 2019; 20(19).

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