PMID: 9449252Aug 1, 1997Paper

Transcriptional regulation of estrogen-responsive genes by non-steroidal estrogens: doisynolic and allenolic acids

The Journal of Steroid Biochemistry and Molecular Biology
Cal Y MeyersS Adler

Abstract

Estrogen receptor (ER), a member of the nuclear receptor superfamily, exerts prominent physiological roles in both humans and other species by acting directly as a transcription factor, altering nuclear gene expression. One peculiarity of estrogenic regulation is that it is affected by a wide variety of non-steroidal compounds in addition to the natural hormone, estradiol. Doisynolic and allenolic acid compounds are non-steroidal compounds that act as potent estrogens in animal studies, yet bind to ER extremely poorly in competitive binding assays, raising the possibility of alternative molecular mechanisms for the observed estrogenic effects. In this work we demonstrate that (+/-)-Z-bisdehydrodoisynolic acid, (+/-)-Z-bisdehydrodoisynolic acid 3-methyl ether, and (-) allenolic acid can interact directly with ER. These compounds all serve as ligands for ER in mechanism-specific tissue culture-based reporter gene assays for both positive and negative gene regulation. We have also used a novel assay based on electromobility shift by ER for directly determining relative binding affinities for ER. In addition, we show cell-type-specific activity differences for (+/-)-Z-bisdehydrodoisynolic acid 3-methyl ether, supporting clinical ob...Continue Reading

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Citations

Nov 14, 2002·The Journal of Steroid Biochemistry and Molecular Biology·Cal Y MeyersStuart Adler
May 7, 2003·The Journal of Steroid Biochemistry and Molecular Biology·Virginia PearceDon Smith
Jul 10, 2010·Menopause : the Journal of the North American Menopause Society·Erin E SundermannJeffrey R Bishop
Aug 17, 1999·The Journal of Clinical Investigation·S SrivastavaR Pacifici
Mar 10, 2009·Toxicology in Vitro : an International Journal Published in Association with BIBRA·Kazuko KitaNobuo Suzuki
Jun 8, 2004·Endocrine Reviews·S K DeyHaibin Wang

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