title: Small-molecule modulators of the constitutive androstane receptor.
abstract: BACKGROUND
  The constitutive androstane receptor (CAR) induces drug-metabolizing enzymes for xenobiotic metabolism.
  
  
  METHODS
  This review covers recent advances in elucidating the biological functions of CAR and its modulation by a growing number of agonists and inhibitors.
  
  
  CONCLUSIONS
  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.
authors.affiliation: Postdoctoral fellow, St. Jude Children's Research Hospital, Department of Chemical Biology and Therapeutics , 262 Danny Thomas Place, Memphis, TN 38105 , USA.
authors.forename: Milu T
authors.initials: MT
authors.lastname: Cherian
authors.forename: Sergio C
authors.initials: SC
authors.lastname: Chai
authors.forename: Taosheng
authors.initials: T
authors.lastname: Chen
mesh_terms: D000818:Animals; D000090702:Constitutive Androstane Receptor; D015195:Drug Design; D006801:Humans; D018160:Receptors, Cytoplasmic and Nuclear / Q000819:agonists / Q000037:antagonists & inhibitors / Q000378:metabolism*; D012377:Rodentia; D013045:Species Specificity; D015262:Xenobiotics / Q000378:metabolism*
chemical_list: D000090702:Constitutive Androstane Receptor; D018160:Receptors, Cytoplasmic and Nuclear; D015262:Xenobiotics
keywords: constitutive androstane receptor; drug–drug interactions; small-molecule; xenobiotic metabolism