2ouz

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[[Image:2ouz.gif|left|200px]]
[[Image:2ouz.gif|left|200px]]
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{{Structure
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<!--
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|PDB= 2ouz |SIZE=350|CAPTION= <scene name='initialview01'>2ouz</scene>, resolution 2.000&Aring;
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The line below this paragraph, containing "STRUCTURE_2ouz", creates the "Structure Box" on the page.
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|SITE=
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You may change the PDB parameter (which sets the PDB file loaded into the applet)
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|LIGAND= <scene name='pdbligand=C3D:(5R,6S)-6-PHENYL-5-[4-(2-PYRROLIDIN-1-YLETHOXY)PHENYL]-5,6,7,8-TETRAHYDRONAPHTHALEN-2-OL'>C3D</scene>
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or the SCENE parameter (which sets the initial scene displayed when the page is loaded),
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|ACTIVITY=
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or leave the SCENE parameter empty for the default display.
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|GENE= ESR1, ESR, NR3A1 ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])
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-->
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|DOMAIN=
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{{STRUCTURE_2ouz| PDB=2ouz | SCENE= }}
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|RELATEDENTRY=[[1err|1ERR]], [[1ere|1ERE]]
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|RESOURCES=<span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=2ouz FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=2ouz OCA], [http://www.ebi.ac.uk/pdbsum/2ouz PDBsum], [http://www.rcsb.org/pdb/explore.do?structureId=2ouz RCSB]</span>
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}}
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'''Crystal Structure of Estrogen Receptor alpha-lasofoxifene complex'''
'''Crystal Structure of Estrogen Receptor alpha-lasofoxifene complex'''
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[[Category: Pandit, J.]]
[[Category: Pandit, J.]]
[[Category: Vajdos, F F.]]
[[Category: Vajdos, F F.]]
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[[Category: estrogen]]
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[[Category: Estrogen]]
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[[Category: nuclear receptor]]
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[[Category: Nuclear receptor]]
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[[Category: serm]]
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[[Category: Serm]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun May 4 11:42:47 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Mon Mar 31 04:23:34 2008''
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Revision as of 08:42, 4 May 2008

Image:2ouz.gif

Template:STRUCTURE 2ouz

Crystal Structure of Estrogen Receptor alpha-lasofoxifene complex


Overview

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.

About this Structure

2OUZ is a Single protein structure of sequence from Homo sapiens. Full crystallographic information is available from OCA.

Reference

The 2.0 A crystal structure of the ERalpha ligand-binding domain complexed with lasofoxifene., Vajdos FF, Hoth LR, Geoghegan KF, Simons SP, LeMotte PK, Danley DE, Ammirati MJ, Pandit J, Protein Sci. 2007 May;16(5):897-905. PMID:17456742 Page seeded by OCA on Sun May 4 11:42:47 2008

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