PMID: 7106368Jun 1, 1982Paper

The dissociation rate of estrogen receptor-ligand complexes is increased by high concentrations of steroids and antiestrogens

Molecular and Cellular Endocrinology
J L Borgna, S Ladrech

Abstract

The first-order dissociation rate constant, k-, of estradiol from uterine estrogen receptor, measured kin the presence of micromolar concentrations of diethylstilbestrol, increased linearly over a large concentration range (0-300 microM) of diethylstilbestrol. The experimental K- measured appears to be the sum of a basal dissociation rate constant corresponding to the spontaneous dissociation in the absence of diethylstilbestrol, and a diethylstilbestrol-induced dissociation rate constant, which is proportional to both the diethylstilbestrol concentration and the inverse of the cytosol concentration. Diethylstilbestrol induced the dissociation of estradiol in all species studied (lamb, calf and rat) and of estrone and 2 antiestrogens in lamb uterus. Various steroids and triphenylethylene antiestrogens also efficiently induced the dissociation of estradiol from the estrogen receptor. However, the potency of these inducers, which varied greatly, was not correlated with the binding affinity for the estrogen receptor. Structural characteristics and the hydrophobicity of the inducers, however, did appear to be important parameters. The relative efficiency of inducers varied depending on the ligand that was bound to the receptor. Thi...Continue Reading

References

Mar 1, 1979·European Journal of Cancer : Official Journal for European Organization for Research and Treatment of Cancer (EORTC) [and] European Association for Cancer Research (EACR)·R I NicholsonK Griffiths
May 28, 1979·Biochemical and Biophysical Research Communications·H RochefortJ L Borgna
Nov 1, 1977·The Journal of Endocrinology·V C JordanG Prestwich
Oct 9, 1973·Biochemistry·J A KatzenellenbogenH N Myers
Oct 1, 1980·Molecular and Cellular Endocrinology·J L Borgna, H Rochefort

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