1qku

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[[Image:1qku.gif|left|200px]]
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[[Image:1qku.png|left|200px]]
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==Overview==
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{{ABSTRACT_11278577}}
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The crystal structure of a triple cysteine to serine mutant ERalpha ligand-binding domain (LBD), complexed with estradiol, shows that despite the presence of a tightly bound agonist ligand, the protein exhibits an antagonist-like conformation, similar to that observed in raloxifen and 4-hydroxytamoxifen-bound structures. This mutated receptor binds estradiol with wild type affinity and displays transcriptional activity upon estradiol stimulation, but with limited potency (about 50%). This partial activity is efficiently repressed in antagonist competition assays. The comparison with available LBD structures reveals key features governing the positioning of helix H12 and highlights the importance of cysteine residues in promoting an active conformation. Furthermore the present study reveals a hydrogen bond network connecting ligand binding to protein trans conformation. These observations support a dynamic view of H12 positioning, where the control of the equilibrium between two stable locations determines the partial agonist character of a given ligand.
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==About this Structure==
==About this Structure==
1QKU is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. The following page contains interesting information on the relation of 1QKU with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb45_1.html Estrogen Receptor]]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QKU OCA].
1QKU is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. The following page contains interesting information on the relation of 1QKU with [[http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/pdb45_1.html Estrogen Receptor]]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=1QKU OCA].
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==Reference==
 
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Crystal structure of a mutant hERalpha ligand-binding domain reveals key structural features for the mechanism of partial agonism., Gangloff M, Ruff M, Eiler S, Duclaud S, Wurtz JM, Moras D, J Biol Chem. 2001 May 4;276(18):15059-65. Epub 2001 Feb 6. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/11278577 11278577]
 
[[Category: Estrogen Receptor]]
[[Category: Estrogen Receptor]]
[[Category: Homo sapiens]]
[[Category: Homo sapiens]]
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[[Category: Structural genomic]]
[[Category: Structural genomic]]
[[Category: Structural proteomics in europe]]
[[Category: Structural proteomics in europe]]
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Sun Apr 13 08:10:11 2008''
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''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Jun 26 17:52:02 2008''

Revision as of 14:52, 26 June 2008

Image:1qku.png

Template:STRUCTURE 1qku

WILD TYPE ESTROGEN NUCLEAR RECEPTOR LIGAND BINDING DOMAIN COMPLEXED WITH ESTRADIOL


Template:ABSTRACT 11278577

About this Structure

1QKU is a Single protein structure of sequence from Homo sapiens. The following page contains interesting information on the relation of 1QKU with [Estrogen Receptor]. Full crystallographic information is available from OCA.

Page seeded by OCA on Thu Jun 26 17:52:02 2008

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