title: Crystallographic analysis of murine constitutive androstane receptor ligand-binding domain complexed with 5alpha-androst-16-en-3alpha-ol.
abstract: The constitutive androstane receptor (CAR) is a member of the nuclear receptor superfamily. In contrast to classical nuclear receptors, which possess small-molecule ligand-inducible activity, CAR exhibits constitutive transcriptional activity in the apparent absence of ligand. CAR is among the most important transcription factors; it coordinately regulates the expression of microsomal cytochrome P450 genes and other drug-metabolizing enzymes. The murine CAR ligand-binding domain (LBD) was coexpressed with the steroid receptor coactivator protein (SRC-1) receptor-interacting domain (RID) in Escherichia coli. The mCAR LBD subunit was purified away from SRC-1 by affinity, anion-exchange and size-exclusion chromatography, crystallized with androstenol and the structure of the complex determined by molecular replacement.
authors.affiliation: Department of Biochemistry, Cellular and Molecular Biology, University of Tennessee, Knoxville, Tennessee 37996, USA.
authors.forename: Jeremy
authors.initials: J
authors.lastname: Vincent
authors.forename: Li
authors.initials: L
authors.lastname: Shan
authors.forename: Ming
authors.initials: M
authors.lastname: Fan
authors.forename: Joseph S
authors.initials: JS
authors.lastname: Brunzelle
authors.forename: Barry M
authors.initials: BM
authors.lastname: Forman
authors.forename: Elias J
authors.initials: EJ
authors.lastname: Fernandez
mesh_terms: D000737:Androstenols / Q000378:metabolism*; D000818:Animals; D001665:Binding Sites; D018360:Crystallography, X-Ray; D008024:Ligands; D051379:Mice; D011487:Protein Conformation; D011944:Receptors, Androgen / Q000737:chemistry* / Q000302:isolation & purification / Q000378:metabolism*; D011994:Recombinant Proteins / Q000737:chemistry / Q000302:isolation & purification / Q000378:metabolism
chemical_list: D000737:Androstenols; D008024:Ligands; D011944:Receptors, Androgen; D011994:Recombinant Proteins; C026828:5 alpha-androst-16-en-3 beta-ol