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Biochem Soc Trans. 2000;28(4):396-400.

Structural aspects of agonism and antagonism in the oestrogen receptor.

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  • 1Structural Biology Laboratory, Chemistry Department, University of York, York YO10 5DD, U.K.


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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