title: Interaction of the antioestrogen ICI 164,384 with the oestrogen receptor.
abstract: The use of partially purified preparations of the human uterine oestrogen receptor has enabled, for the first time, a study of the binding of the steroidal, pure antioestrogen ICI 164,384 [N-n-butyl-11-(3,17 beta-dihydroxy-oestra-1,3,5(10)-trien-7 alpha-yl)N-methyl-undecamide] to the oestrogen receptor. Scatchard analyses of the binding of [3H]oestradiol and [3H]ICI 164,384 to the receptor show that the equilibrium dissociation constants for the interactions of these ligands with the receptor at 0 degrees C are 0.44 and 0.69 nM respectively. The concentration of receptor binding sites for the agonist was 1986 fmol/mg protein whilst that for the antagonist was 1400 fmol/mg protein. The affinity of the antioestrogen-receptor complex for DNA-cellulose does not increase following exposure to conditions that transform the oestrogen-receptor complex.
authors.affiliation: Tenovus Institute for Cancer Research, University of Wales College of Medicine, Heath Park, Cardiff.
authors.forename: P J
authors.initials: PJ
authors.lastname: Weatherill
authors.forename: A P
authors.initials: AP
authors.lastname: Wilson
authors.forename: R I
authors.initials: RI
authors.lastname: Nicholson
authors.forename: P
authors.initials: P
authors.lastname: Davies
authors.forename: A E
authors.initials: AE
authors.lastname: Wakeling
mesh_terms: D004958:Estradiol / Q000031:analogs & derivatives* / Q000378:metabolism; D004965:Estrogen Antagonists / Q000378:metabolism*; D005260:Female; D006801:Humans; D007700:Kinetics; D053284:Polyunsaturated Alkamides; D011960:Receptors, Estrogen / Q000378:metabolism*; D014599:Uterus / Q000378:metabolism*
chemical_list: D004965:Estrogen Antagonists; D053284:Polyunsaturated Alkamides; D011960:Receptors, Estrogen; D004958:Estradiol; C051781:ICI 164384