3ert
From Proteopedia
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| - | [[Image:3ert.gif|left|200px]] | + | [[Image:3ert.gif|left|200px]] |
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| - | '''HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH 4-HYDROXYTAMOXIFEN''' | + | {{Structure |
| + | |PDB= 3ert |SIZE=350|CAPTION= <scene name='initialview01'>3ert</scene>, resolution 1.90Å | ||
| + | |SITE= | ||
| + | |LIGAND= <scene name='pdbligand=OHT:4-HYDROXYTAMOXIFEN'>OHT</scene> | ||
| + | |ACTIVITY= | ||
| + | |GENE= ESTROGEN RECEPTOR ALPHA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens]) | ||
| + | }} | ||
| + | |||
| + | '''HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH 4-HYDROXYTAMOXIFEN''' | ||
| + | |||
==Overview== | ==Overview== | ||
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==About this Structure== | ==About this Structure== | ||
| - | 3ERT is a [ | + | 3ERT is a [[Single protein]] structure of sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. This structure supersedes the now removed PDB entry 2ERT. The following page contains interesting information on the relation of 3ERT 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=3ERT OCA]. |
==Reference== | ==Reference== | ||
| - | The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen., Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL, Cell. 1998 Dec 23;95(7):927-37. PMID:[http:// | + | The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen., Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL, Cell. 1998 Dec 23;95(7):927-37. PMID:[http://www.ncbi.nlm.nih.gov/pubmed/9875847 9875847] |
[[Category: Estrogen Receptor]] | [[Category: Estrogen Receptor]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
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[[Category: transcription factor]] | [[Category: transcription factor]] | ||
| - | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu | + | ''Page seeded by [http://oca.weizmann.ac.il/oca OCA ] on Thu Mar 20 19:04:39 2008'' |
Revision as of 17:04, 20 March 2008
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| , resolution 1.90Å | |||||||
|---|---|---|---|---|---|---|---|
| Ligands: | |||||||
| Gene: | ESTROGEN RECEPTOR ALPHA (Homo sapiens) | ||||||
| Coordinates: | save as pdb, mmCIF, xml | ||||||
HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH 4-HYDROXYTAMOXIFEN
Contents |
Overview
Ligand-dependent activation of transcription by nuclear receptors (NRs) is mediated by interactions with coactivators. Receptor agonists promote coactivator binding, and antagonists block coactivator binding. Here we report the crystal structure of the human estrogen receptor alpha (hER alpha) ligand-binding domain (LBD) bound to both the agonist diethylstilbestrol (DES) and a peptide derived from the NR box II region of the coactivator GRIP1 and the crystal structure of the hER alpha LBD bound to the selective antagonist 4-hydroxytamoxifen (OHT). In the DES-LBD-peptide complex, the peptide binds as a short alpha helix to a hydrophobic groove on the surface of the LBD. In the OHT-LBD complex, helix 12 occludes the coactivator recognition groove by mimicking the interactions of the NR box peptide with the LBD. These structures reveal the two distinct mechanisms by which structural features of OHT promote this "autoinhibitory" helix 12 conformation.
Disease
Known diseases associated with this structure: Atherosclerosis, susceptibility to OMIM:[133430], Breast cancer OMIM:[133430], Estrogen resistance OMIM:[133430], HDL response to hormone replacement, augmented OMIM:[133430], Migraine, susceptibility to OMIM:[133430], Myocardial infarction, susceptibility to OMIM:[133430]
About this Structure
3ERT is a Single protein structure of sequence from Homo sapiens. This structure supersedes the now removed PDB entry 2ERT. The following page contains interesting information on the relation of 3ERT with [Estrogen Receptor]. Full crystallographic information is available from OCA.
Reference
The structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifen., Shiau AK, Barstad D, Loria PM, Cheng L, Kushner PJ, Agard DA, Greene GL, Cell. 1998 Dec 23;95(7):927-37. PMID:9875847
Page seeded by OCA on Thu Mar 20 19:04:39 2008
