THE INTERACTION OF HUMAN ENDOMETRIAL AND MYOMETRIAL STEROID RECEPTORS WITH DANAZOL

G Jenkin, Graham Jenkin, C I Cookson, G D Thorburn
Clinical endocrinology · 1983 · vol. 19(3) , pp. 377–388 · doi:10.1111/j.1365-2265.1983.tb00011.x · PMID:6627694 · W2103230058
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This study determined danazol's affinity for human endometrial and myometrial steroid receptors, finding it binds to progesterone and androgen receptors but poorly to estrogen receptors.

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Abstract

The affinity of danazol for oestrogen, androgen and progesterone receptors in human endometrium and myometrium was determined, to study the mechanism of action of this drug in the treatment of endometriosis. The ability of danazol to combine with each of the three types of receptor was similar in both endometrium and myometrium. The capacity of danazol to compete with oestradiol-17 beta for the oestrogen receptor was very low (1.72 +/- 0.48 X 10(-3%) cross reaction, mean +/- SEM) and danazol, at the maximum concentration used, was unable to saturate the receptor; but danazol's ability to compete with progesterone for its receptor was considerably higher (8.41 +/- 1.65% using progesterone, 1.95 +/- 0.41% using R5020) and was saturable. Danazol was also able to displace dihydrotestosterone from the cytosol androgen receptor (6.29 +/- 1.82% cross reaction). The association constant of oestradiol for the endometrial and myometrial oestrogen receptors was 2.19 X 10(9)M-1 and 7.45 X 10(9)M-1 respectively, while that of progesterone and dihydrotestosterone for their receptors was similar in endometrium and myometrium (mean 0.25 +/- 0.06 X 10(9) M-1 and 3.62 +/- 1.67 X 10(9) M-1 respectively). Using R5020, the association constant for the myometrial progesterone receptor was 2.50 +/- 0.73 X 10(9) M-1. We conclude that, in view of the high circulating levels of danazol present in patients being treated for endometriosis, it is possible that danazol may bind to, and partly saturate, endometrial and myometrial oestrogen, progesterone and androgen receptors during treatment. An explanation may thus be provided for some of the diverse actions of this drug.

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Condition tags

endometriosis

MeSH descriptors

Danazol Endometrium Myometrium Pregnadienes Receptors, Steroid Binding, Competitive Cross Reactions Cytosol Cytosol Danazol Endometrium Female Humans In Vitro Techniques Myometrium Pregnadienes Receptors, Androgen Receptors, Androgen Receptors, Estrogen Receptors, Estrogen

Citation neighborhood

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References (37)

Cited by (9)

SciLite annotations

organisms 2
human human
chemicals 17
danazol danazol estrogen androgen danazol danazol danazol progesterone danazol delta(1)-dihydrotestosterone estradiol progesterone delta(1)-dihydrotestosterone danazol danazol estrogen progesterone

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