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Studies with the high-affinity antiestrogen, (/sup 3/H)HI285

Thesis/Dissertation ·
OSTI ID:7170916

Antiestrogens are compounds that inhibit some of the actions of estrogens. Certain antiestrogens, notably the triphenylethylene, tamoxifen, are useful in the treatment of female breast cancer. The triphenylethylene antiestrogen, HI285, was labelled with radioactive hydrogen ((/sup 3/H)) for use as a probe of antiestrogen action. Radioactive HI285 ((/sup 3/H)HI285) bound to the cytosolic estrogen receptor from both rat and calf uterus and competed with estradiol for the estrogen specific binding site. In both animals (/sup 3/H)HI285 displayed a higher affinity for the estrogen receptor and a slower dissociation rate from the receptor than did estradiol. (/sup 3/H)HI285, as well as estradiol, appeared to trigger receptor activation. Studies using the activation blocker, sodium molybdate, indicated that (/sup 3/H)HI285 triggered activation in a manner different from estradiol. The non-activated estrogen receptor from calf uterus, when occupied by (/sup 3/H)estradiol, existed as two discrete forms that could be separated by ion-exchange chromatography. In contrast, the (/sup 3/H)HI285-occupied receptor existed as a single form.

Research Organization:
Saint Louis Univ., MO (USA)
OSTI ID:
7170916
Country of Publication:
United States
Language:
English

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Related Subjects

550201* -- Biochemistry-- Tracer Techniques
560300 -- Chemicals Metabolism & Toxicology
59 BASIC BIOLOGICAL SCIENCES
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ANIMALS
BIOCHEMICAL REACTION KINETICS
BODY
CATTLE
CHEMICAL ACTIVATION
DATA
DOMESTIC ANIMALS
ESTRADIOL
ESTRANES
ESTROGENS
EXPERIMENTAL DATA
FEMALE GENITALS
HORMONES
HYDROXY COMPOUNDS
INFORMATION
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MAMMALS
MEMBRANE PROTEINS
NUMERICAL DATA
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PROTEINS
RATS
REACTION KINETICS
RECEPTORS
RODENTS
RUMINANTS
STEROID HORMONES
STEROIDS
TAMOXIFEN
TRACER TECHNIQUES
TRITIUM COMPOUNDS
UTERUS
VERTEBRATES