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Updated: Apr 12, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Small-molecule modulators of the constitutive androstane receptor
Milu T Cherian1, Sergio C Chai, Taosheng Chen
1Postdoctoral fellow, St. Jude Children's Research Hospital, Department of Chemical Biology and Therapeutics , 262 Danny Thomas Place, Memphis, TN 38105 , USA.
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.
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