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Small-molecule modulators of the constitutive androstane receptor.

ABSTRACT: The constitutive androstane receptor (CAR) induces drug-metabolizing enzymes for xenobiotic metabolism.This review covers recent advances in elucidating the biological functions of CAR and its modulation by a growing number of agonists and inhibitors.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.

SUBMITTER: Cherian MT 

PROVIDER: S-EPMC4469626 | biostudies-literature | 2015 Jul

REPOSITORIES: biostudies-literature

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Small-molecule modulators of the constitutive androstane receptor.

Cherian Milu T MT   Chai Sergio C SC   Chen Taosheng T  

Expert opinion on drug metabolism & toxicology 20150515 7

<h4>Introduction</h4>The constitutive androstane receptor (CAR) induces drug-metabolizing enzymes for xenobiotic metabolism.<h4>Areas covered</h4>This review covers recent advances in elucidating the biological functions of CAR and its modulation by a growing number of agonists and inhibitors.<h4>Expert opinion</h4>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 propert  ...[more]

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