title: Targeting xenobiotic receptors PXR and CAR in human diseases.
abstract: Nuclear receptors such as the pregnane X receptor (PXR) and constitutive androstane receptor (CAR) are xenobiotic receptors regulating not only drug metabolism and disposition but also various human diseases such as cancer, diabetes, inflammatory disease, metabolic disease and liver diseases, suggesting that PXR and CAR are promising targets for drug discovery. Consequently, there is an urgent need to discover and develop small molecules that target these PXR- and/or CAR-mediated human-disease-related pathways for relevant therapeutic applications. This review proposes approaches to target PXR and CAR, either individually or simultaneously, in the context of various human diseases, taking into consideration the structural differences between PXR and CAR.
authors.affiliation: Department of Chemical Biology and Therapeutics, St Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA.
authors.forename: Monimoy
authors.initials: M
authors.lastname: Banerjee
authors.affiliation: Department of Chemical Biology and Therapeutics, St Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA.
authors.forename: Delira
authors.initials: D
authors.lastname: Robbins
authors.affiliation: Department of Chemical Biology and Therapeutics, St Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, TN 38105, USA. Electronic address: taosheng.chen@stjude.org.
authors.forename: Taosheng
authors.initials: T
authors.lastname: Chen
mesh_terms: D001665:Binding Sites; D001711:Biotransformation; D000090702:Constitutive Androstane Receptor; D015195:Drug Design; D004347:Drug Interactions; D006801:Humans; D008024:Ligands; D058990:Molecular Targeted Therapy; D000077297:Pregnane X Receptor; D011485:Protein Binding; D011487:Protein Conformation; D020239:Receptor Cross-Talk; D018160:Receptors, Cytoplasmic and Nuclear / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D011987:Receptors, Steroid / Q000737:chemistry / Q000187:drug effects* / Q000378:metabolism; D015398:Signal Transduction / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D000090702:Constitutive Androstane Receptor; D008024:Ligands; D000077297:Pregnane X Receptor; D018160:Receptors, Cytoplasmic and Nuclear; D011987:Receptors, Steroid