title: Synthetic peptides derived from the steroid binding domain block modulator and molybdate action toward the rat glucocorticoid receptor.
abstract: Modulators are endogenous low-mol-wt inhibitors of glucocorticoid receptor activation, and are mimicked by exogenous sodium molybdate. Activation involves the dissociation of the 90-kDa heat-shock protein from the receptor. The heat-shock protein is thought to bind to a conserved 20-amino-acid region in the steroid-binding domain of the receptor (595-614 of the rat protein). Synthetic peptides corresponding to this amino acid sequence prevented the modulators and sodium molybdate from inhibiting receptor activation. These results imply that the region 595-614 of the rat glucocorticoid receptor is also a modulator/molybdate binding site.
authors.affiliation: Women's Health Research Institute, Wyeth-Ayerst Laboratories, Radnor, PA 19087, USA.
authors.forename: P V
authors.initials: PV
authors.lastname: Bodine
authors.forename: E S
authors.initials: ES
authors.lastname: Alnemri
authors.forename: G
authors.initials: G
authors.lastname: Litwack
mesh_terms: D000595:Amino Acid Sequence; D000818:Animals; D001665:Binding Sites; D004305:Dose-Response Relationship, Drug; D008969:Molecular Sequence Data; D008982:Molybdenum / Q000494:pharmacology*; D010446:Peptide Fragments / Q000138:chemical synthesis / Q000494:pharmacology*; D010742:Phospholipid Ethers / Q000494:pharmacology*; D051381:Rats; D011965:Receptors, Glucocorticoid / Q000037:antagonists & inhibitors*; D014222:Triamcinolone Acetonide / Q000378:metabolism
chemical_list: D010446:Peptide Fragments; D010742:Phospholipid Ethers; D011965:Receptors, Glucocorticoid; C055044:glucocorticoid receptor complex modulator; D008982:Molybdenum; C024687:sodium molybdate(VI); D014222:Triamcinolone Acetonide