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Estriol and estrone interaction with the estrogen receptor: estriol and estrone-induced inhibition of the cooperative binding of (/sup 3/H)estradiol to the estrogen receptor

Journal Article · · J. Biol. Chem.; (United States)
OSTI ID:6472827
;

The effects of estriol and estone on the positive cooperativity of (/sup 3/H)estradiol binding to the partially purified, calf uterine estrogen receptor were studied. The receptor was titrated with variable concentrations of (/sup 3/H)estradiol in combination with estriol or estrone, while maintaining a constant molar ratio of the estriol or estrone to the (/sup 3/H)estradiol. With either a 4-fold molar excess of estriol or a 25-fold molar excess of estrone above the (/sup 3/H)estradiol concentrations, the receptor's positive cooperative (/sup 3/H)estradiol binding was inhibited. The Scatchard plot showed a transition from a convex to a linear curve and a decrease in the Hill coefficient value from 1.61 +/- 0.02 (n = 7) in the absence of estriol or estrone to 1.04 +/- 0.04 (n = 4) in the presence of estriol and 0.99 +/- 0.03 (n = 4) in the presence of estrone. The inhibition of the positive cooperativity of (/sup 3/H) estradiol binding by estriol or estrone was shown not to be due to isotope dilution of the specifically bound (/sup 3/H)estradiol by the unlabeled estriol or estrone. These kinetic analyses demonstrate that the positively cooperative equilibrium binding of (/sup 3/H)estradiol by the receptor, which is characteristic of the receptor's activation process, is eliminated by estriol and estrone and consistent with their partial agonist-antagonist activities observed in vivo.

Research Organization:
Univ. of Rochester School of Medicine and Dentistry, NY
DOE Contract Number:
AC02-76EV03490
OSTI ID:
6472827
Journal Information:
J. Biol. Chem.; (United States), Journal Name: J. Biol. Chem.; (United States) Vol. 258:13; ISSN JBCHA
Country of Publication:
United States
Language:
English

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Related Subjects

550200* -- Biochemistry
59 BASIC BIOLOGICAL SCIENCES
ANIMALS
BINDING ENERGY
BIOCHEMICAL REACTION KINETICS
BODY
CALVES
CATTLE
CPB
DOMESTIC ANIMALS
ENERGY
ESTRADIOL
ESTRANES
ESTRIOL
ESTROGENS
ESTRONE
FEMALE GENITALS
HORMONES
HYDROXY COMPOUNDS
IN VIVO
INHIBITION
ISOTOPE APPLICATIONS
KETONES
KINETICS
LABELLED COMPOUNDS
MAMMALS
ORGANIC COMPOUNDS
ORGANS
RADIORECEPTOR ASSAY
REACTION KINETICS
RECEPTORS
RUMINANTS
STEROID HORMONES
STEROIDS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
UTERUS
VERTEBRATES