PMID: 2432356Nov 1, 1986Paper

Competitive binding assay for estrogen receptor in monolayer culture: measure of receptor activation potency

Journal of Steroid Biochemistry
S Stoessel, G Leclercq

Abstract

MCF-7 cells were incubated with [3H]estradiol, unlabeled estradiol and various estrogens or antiestrogens to measure their relative binding affinity (whole-cell assay). Comparison of the values with those previously established on uterine cytosol with a DCC assay revealed a good parallelism for both steroid and diphenolic diethylstilbestrol based estrogens. On the contrary, in the whole-cell assay, antiestrogens and weak estrogens of the triphenyl- and gem-diphenylethylene categories always displayed low values which were in the order of magnitude found with weak steroid estrogens. This property was not due to a reduction of binding capacity, nor to the presence in some compounds of an ethoxyaminoalkyl side-chain (source of antiestrogenicity). In view of all these data, it was concluded that the present test would provide an estimate of the ability of a given compound to transform the receptor in a form which interacts with genomic sites involved in the regulation of "estrogenic-induced products" ("activation").

References

Jan 1, 1978·Journal of Steroid Biochemistry·M M Bouton, J P Raynaud
Dec 15, 1976·International Journal of Cancer. Journal International Du Cancer·G LeclercqJ C Heuson
Aug 30, 1985·Biochemical and Biophysical Research Communications·J H Fishman, J Fishman
Jan 1, 1985·Journal of Cancer Research and Clinical Oncology·R W HartmannG Kranzfelder
Aug 1, 1985·European Journal of Cancer & Clinical Oncology·N Olea-SerranoJ C Heuson
Oct 1, 1985·Journal of Medicinal Chemistry·A B FosterN Devleeschouwer
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Aug 26, 1983·Pharmaceutisch Weekblad. Scientific Edition·A J van den BroekF J Zeelen

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Citations

Oct 1, 1988·Journal of Steroid Biochemistry·R McCagueS Stoessel
Mar 1, 1994·The Journal of Steroid Biochemistry and Molecular Biology·M BorrásG Leclercq
Feb 1, 1996·The Journal of Steroid Biochemistry and Molecular Biology·M BorrásG Leclercq
Jul 1, 1997·The Journal of Steroid Biochemistry and Molecular Biology·A El KhissiinG Leclercq
Feb 12, 1998·The Journal of Steroid Biochemistry and Molecular Biology·P C RuenitzC S Bourne
Jul 13, 2016·Journal of Receptor and Signal Transduction Research·Guy LeclercqYves Jacquot
Mar 10, 2007·Bioorganic & Medicinal Chemistry Letters·Isamu ShiinaYoshimune Hasome
Aug 2, 2007·Journal of Cardiovascular Pharmacology·Viktoriya P EkshyyanTammy R Dugas
Jan 1, 1993·Breast Cancer Research and Treatment·P T JainR A Magarian
Oct 1, 2005·Alternatives to Laboratory Animals : ATLA·Susanne BremerHorst Spielmann

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