The PXR crystal structure: The end of the beginning

Trends in Pharmacological Sciences

Volumn 23, Issue 2, 2002, Pages 49-50

  Ekins, Sean ^a   Schuetz, Erin ^b  

^a ELI LILLY AND COMPANY   (United States)

^b ST JUDE CHILDREN S RESEARCH HOSPITAL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

CYTOCHROME P450 3A4; LIGAND; PREGNANE X RECEPTOR;

ALLELE; ARTICLE; CRYSTAL STRUCTURE; DRUG METABOLISM; DRUG TRANSPORT; GENE EXPRESSION; GENE INDUCTION; GENETIC VARIABILITY; HUMAN; LIGAND BINDING; MOLECULAR MODEL; NONHUMAN; PRIORITY JOURNAL; PROTEIN BINDING; PROTEIN DOMAIN; PROTON TRANSPORT;

EID: 0036468860     PISSN: 01656147     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0165-6147(02)01977-6     Document Type: Review

References (20)

1. The human orphan nuclear receptor PXR is activated by compounds that regulate CYP3A4 gene expression and cause drug interactions
2. SXR, a novel steroid and xenobiotic sensing nuclear receptor
3. Identification of a human nuclear receptor defines a new signaling pathway for CYP3A induction
4. An orphan nuclear receptor activated by pregnanes defines a novel steroid signaling pathway
5. St. John's wort induces hepatic drug metabolism through activation of the pregnane X receptor
6. The nuclear receptor PXR is a lithocholic acid sensor that protects against liver toxicity
7. An essential role for nuclear receptors SXR/PXR in detoxification of cholestatic bile acids
8. The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux
9. The pregnane X receptor: A promiscuous xenobiotic receptor that has diverged during evolution
10. The human nuclear xenobiotic receptor PXR: Structural determinants of directed promiscuity
11. Humanized xenobiotic response in mice expressing nuclear receptor SXR
12. Comparative analysis of cytochrome P4503A induction in primary cultures of rat, rabbit and human hepatocytes
13. Disrupted bile acid homeostasis reveals an unexpected interaction among nuclear hormone receptors, transporters and cytochrome P450
14. -/- mice but not in cerebrotendinous xanthomatosis
15. A pharmacophore for human pregnane X receptor ligands
16. Evaluation of atypical cytochrome P450 kinetics with two-substrate models: Evidence that multiple substrates can simultaneously bind to cytochrome P450 active sites
17. Three dimensional quantitative structure activity relationship (3D-QSAR) analysis of CYP3A4 substrates
18. Sequence diversity in CYP3A promoters and characterization of the genetic basis of polymorphic CYP3A5 expression
19. Natural protein variants of pregnane X receptor with altered transactivation activity toward CYP3A4
20. Pharmacophore and three dimensional quantitative structure activity relationship methods for modeling cytochrome P450 active sites