Summary: Cell, Vol. 95, 927­937, December 23, 1998, Copyright ©1998 by Cell Press
The Structural Basis of Estrogen
Receptor/Coactivator Recognition and the
Antagonism of This Interaction by Tamoxifen
endogenous estrogen 17 -estradiol (E2) and the syn-
thetic nonsteroidal estrogen diethylstilbestrol (DES),
function as pure agonists, whereas others, such as ICI-
164,384, function as pure antagonists. Synthetic ligands
such as tamoxifen and raloxifene (RAL) belong to a
Andrew K. Shiau,* Danielle Barstad, Paula M. Loria,
Lin Cheng, Peter J. Kushner, David A. Agard,*§
and Geoffrey L. Greene§
*Howard Hughes Medical Institute
and the Department of Biochemistry and Biophysics
growing class of molecules known as selective estrogenUniversity of California at San Francisco
receptor modulators (SERMs), which function as antag-San Francisco, California 94143-0448
onists in specific tissue and promoter contexts (Grese The Ben May Institute for Cancer Research
et al., 1997). The remarkable tissue-specific behavior ofand Department of Biochemistry and Molecular Biology
tamoxifen was recently demonstrated in the NationalUniversity of Chicago
Surgical Adjuvant Breast and Bowel Project­sponsoredChicago, Illinois 60637

Source: Agard, David - Department of Biochemistry and Biophysics, University of California at San Francisco

Collections: Biotechnology; Biology and Medicine