Structural aspects of agonism and antagonism in the oestrogen receptor |
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Authors: | Pike A C Brzozowski A M Walton J Hubbard R E Bonn T Gustafsson J A Carlquist M |
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Affiliation: | Structural Biology Laboratory, Chemistry Department, University of York, York YO10 5DD, U.K. |
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Abstract: | We have determined the three-dimensional structures of both alpha- and beta-forms of the ligand-binding domain of the oestrogen receptor (ER) in complexes with a range of receptor agonists and antagonists. Here, we summarize how these structures provide both an understanding of the ER's distinctive pharmacophore and a rationale for its ability to bind a diverse range of chemically distinct compounds. In addition, these studies provide a unique insight into the mechanisms that underlie receptor activation, as well as providing a structural basis for the antagonist action of molecules, such as raloxifene. |
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