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| [[Image:2ouz.gif|left|200px]] | | {{Seed}} |
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| {{STRUCTURE_2ouz| PDB=2ouz | SCENE= }} | | {{STRUCTURE_2ouz| PDB=2ouz | SCENE= }} |
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| '''Crystal Structure of Estrogen Receptor alpha-lasofoxifene complex'''
| | ===Crystal Structure of Estrogen Receptor alpha-lasofoxifene complex=== |
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| ==Overview==
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| Lasofoxifene is a new and potent selective estrogen receptor modulator (SERM). The structural basis of its interaction with the estrogen receptor has been investigated by crystallographic analysis of its complex with the ligand-binding domain of estrogen receptor alpha at a resolution of 2.0 A. As with other SERMs, lasofoxifene diverts the receptor from its agonist-bound conformation by displacing the C-terminal AF-2 helix into the site at which the LXXLL motif of coactivator proteins would otherwise be able to bind. Lasofoxifene achieves this effect by occupying the space normally filled by residue Leu 540, as well as by modulating the conformation of residues of helix 11 (His 524, Leu 525). A well-defined salt bridge between lasofoxifene and Asp 351 suggests that charge neutralization in this region of the receptor may explain the some of the antiestrogenic effects of lasofoxifene. The results suggest general features of ERalpha/SERM recognition, and add a new dimension to efforts to rationalize differences between the biological activity profiles exhibited by these important pharmacological agents.
| | The line below this paragraph, {{ABSTRACT_PUBMED_17456742}}, adds the Publication Abstract to the page |
| | (as it appears on PubMed at http://www.pubmed.gov), where 17456742 is the PubMed ID number. |
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| | {{ABSTRACT_PUBMED_17456742}} |
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| ==About this Structure== | | ==About this Structure== |
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| [[Category: Nuclear receptor]] | | [[Category: Nuclear receptor]] |
| [[Category: Serm]] | | [[Category: Serm]] |
| ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:42:47 2008'' | | |
| | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Jul 28 18:52:13 2008'' |