PMID: 7543683Aug 1, 1995Paper

An antiestrogen: a phosphotyrosyl peptide that blocks dimerization of the human estrogen receptor

Proceedings of the National Academy of Sciences of the United States of America
S F Arnold, A C Notides

Abstract

We have previously identified tyrosine-537 as a constitutively phosphorylated site on the human estrogen receptor (hER). A 12-amino acid phosphotyrosyl peptide containing a selected sequence surrounding tyrosine-537 was used to investigate the function of phosphotyrosine-537. The phosphotyrosyl peptide completely blocked the binding of the hER to an estrogen response element (ERE) in a gel mobility shift assay. Neither the nonphosphorylated tyrosyl peptide nor an unrelated phosphotyrosyl peptide previously shown to inhibit the signal transducers and activators of transcription factor (STAT) blocked binding of the hER to the ERE. The hER phosphotyrosyl peptide was shown by molecular sizing chromatography to dissociate the hER dimer into monomers. The hER specifically bound the 32P-labeled phosphotyrosyl peptide, indicating that the inhibition of ERE binding was caused by the phosphotyrosyl peptide binding directly to the hER and blocking dimerization. These data suggest that the phosphorylation of tyrosine-537 is a necessary step for the formation of the hER dimer. In addition, we propose that the dimerization of the hER occurs by a previously unrecognized Src homology 2 domain (SH2)-like phosphotyrosyl coupling mechanism. Conse...Continue Reading

References

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Citations

Nov 14, 2008·Environmental Science and Pollution Research International·J M Navas, H Segner
Jul 20, 2002·The Journal of Steroid Biochemistry and Molecular Biology·Makoto UsamiYasuo Ohno
Apr 25, 2003·The Journal of Steroid Biochemistry and Molecular Biology·Elisabeth Jisa, Alois Jungbauer
Mar 14, 2000·Journal of Interferon & Cytokine Research : the Official Journal of the International Society for Interferon and Cytokine Research·A P FlintP A Fisher
Feb 4, 2014·Breast Cancer Research and Treatment·Suzanne A W FuquaYassine Rechoum
Jul 20, 2002·Neuropharmacology·Hideyuki SawadaShun Shimohama
Jan 25, 2013·Medicinal Research Reviews·Laura Caboni, David G Lloyd
Jul 26, 2003·Nutrition and Cancer·Cécile Vissac-SabatierDominique J Bernard-Gallon
May 8, 2018·Hormones & Cancer·Sasha M PejerreySuzanne A W Fuqua
Feb 17, 2005·American Journal of Physiology. Endocrinology and Metabolism·Ewa Rzewuska-LechVirginia M Miller
Dec 8, 2004·Endocrine Reviews·Matthew H Herynk, Suzanne A W Fuqua
Jun 7, 1996·The Journal of Biological Chemistry·G S TakimotoK B Horwitz
Jun 2, 2000·FASEB Journal : Official Publication of the Federation of American Societies for Experimental Biology·H SawadaS Shimohama
Aug 1, 1996·Endocrine Research·L J BlokA O Brinkmann
Aug 16, 2018·Acta Pharmaceutica Sinica. B·Xiao-Mei QiGuan Chen
Dec 26, 2001·Chemical Reviews·M W Peczuh, A D Hamilton
Apr 1, 1996·Molecular and Cellular Biology·S Malik, S K Karathanasis

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