Structural aspects of agonism and antagonism in the oestrogen receptor.

Structural aspects of agonism and antagonism in the oestrogen receptor.

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 distinc...

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Bibliographic Details
Main Authors: Pike, A, Brzozowski, A, Walton, J, Hubbard, R, Bonn, T, Gustafsson, J, Carlquist, M
Format: Journal article
Language:English
Published: 2000
Description
Summary: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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