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

Journal Article · Sun Jul 10 00:00:00 EDT 1983 · J. Biol. Chem.; (United States)

OSTI ID:6414178

Sasson, S; Notides, A C

Experiments were performed to study the calf uterine estrogen receptor's interaction with (/sup 3/H)estril and (/sup 3/H)estrone and found that the receptor's cooperative binding is markedly dependent upon temperature and receptor concentration. With increasing temperature, the intensity of the estrogen receptor's cooperativity decreases: at 0/sup 0/C the Scatchard plot was convex and the Hill coefficient was 1.03 +/- 0.02 (n = 3) for the binding of (/sup 3/H)estriol with a receptor concentration of 10 to 12 nM. With increasing receptor concentration, the receptor's cooperativity gradually increased. At a receptor concentration of 1 nM, at 25/sup 0/C, with (/sup 3/H)estriol the Hill coefficient was low, 1.03 +/- 0.02 (n = 3), while at approximately intracellular receptor concentration (20 nM) the Hill coefficient increased to 1.20 +/- 0.04 (n = 4). Similar results were observed with (/sup 3/H)estrone. The cooperative interaction of the estrogen receptor with (/sup 3/H)estriol or (/sup 3/H)estrone is reversible and dependent upon temperature. The van't Hoff analysis of the apparent dissociation constant of the )/sup 3/H)estrone- and (/sup 3/H)estriol-receptor complexes indicates that a transition in the receptor's binding mechanism occurs at 15/sup 0/C. Therefore, measurement of ligand interactions with the estrogen receptor at 0 to 15/sup 0/C, may not reflect the binding mechanism of the receptor at more biologically relevant temperatures.

• Research Organization: Univ. of Rochester School of Medicine and Dentistry, NY
• DOE Contract Number: AC02-76EV03490
• OSTI ID: 6414178
• 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

Related Subjects

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