3ert
From Proteopedia
(Difference between revisions)
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| - | + | ==HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH 4-HYDROXYTAMOXIFEN== | |
| - | + | <StructureSection load='3ert' size='340' side='right' caption='[[3ert]], [[Resolution|resolution]] 1.90Å' scene=''> | |
| - | + | == Structural highlights == | |
| + | <table><tr><td colspan='2'>[[3ert]] is a 1 chain structure with sequence from [http://en.wikipedia.org/wiki/Homo_sapiens Homo sapiens]. This structure supersedes the now removed PDB entry [http://oca.weizmann.ac.il/oca-bin/send-pdb?obs=1&id=2ert 2ert]. The September 2003 RCSB PDB [http://pdb.rcsb.org/pdb/static.do?p=education_discussion/molecule_of_the_month/index.html Molecule of the Month] feature on ''Estrogen Receptor'' by David S. Goodsell is [http://dx.doi.org/10.2210/rcsb_pdb/mom_2003_9 10.2210/rcsb_pdb/mom_2003_9]. Full crystallographic information is available from [http://oca.weizmann.ac.il/oca-bin/ocashort?id=3ERT OCA]. For a <b>guided tour on the structure components</b> use [http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ERT FirstGlance]. <br> | ||
| + | </td></tr><tr id='ligand'><td class="sblockLbl"><b>[[Ligand|Ligands:]]</b></td><td class="sblockDat"><scene name='pdbligand=OHT:4-HYDROXYTAMOXIFEN'>OHT</scene></td></tr> | ||
| + | <tr id='gene'><td class="sblockLbl"><b>[[Gene|Gene:]]</b></td><td class="sblockDat">ESTROGEN RECEPTOR ALPHA ([http://www.ncbi.nlm.nih.gov/Taxonomy/Browser/wwwtax.cgi?mode=Info&srchmode=5&id=9606 Homo sapiens])</td></tr> | ||
| + | <tr id='resources'><td class="sblockLbl"><b>Resources:</b></td><td class="sblockDat"><span class='plainlinks'>[http://oca.weizmann.ac.il/oca-docs/fgij/fg.htm?mol=3ert FirstGlance], [http://oca.weizmann.ac.il/oca-bin/ocaids?id=3ert OCA], [http://www.rcsb.org/pdb/explore.do?structureId=3ert RCSB], [http://www.ebi.ac.uk/pdbsum/3ert PDBsum]</span></td></tr> | ||
| + | </table> | ||
| + | == Evolutionary Conservation == | ||
| + | [[Image:Consurf_key_small.gif|200px|right]] | ||
| + | Check<jmol> | ||
| + | <jmolCheckbox> | ||
| + | <scriptWhenChecked>select protein; define ~consurf_to_do selected; consurf_initial_scene = true; script "/wiki/ConSurf/er/3ert_consurf.spt"</scriptWhenChecked> | ||
| + | <scriptWhenUnchecked>script /wiki/extensions/Proteopedia/spt/initialview01.spt</scriptWhenUnchecked> | ||
| + | <text>to colour the structure by Evolutionary Conservation</text> | ||
| + | </jmolCheckbox> | ||
| + | </jmol>, as determined by [http://consurfdb.tau.ac.il/ ConSurfDB]. You may read the [[Conservation%2C_Evolutionary|explanation]] of the method and the full data available from [http://bental.tau.ac.il/new_ConSurfDB/chain_selection.php?pdb_ID=2ata ConSurf]. | ||
| + | <div style="clear:both"></div> | ||
| + | <div style="background-color:#fffaf0;"> | ||
| + | == Publication Abstract from PubMed == | ||
| + | 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. | ||
| - | + | 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<ref>PMID:9875847</ref> | |
| - | + | ||
| + | From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.<br> | ||
| + | </div> | ||
==See Also== | ==See Also== | ||
*[[Estrogen receptor|Estrogen receptor]] | *[[Estrogen receptor|Estrogen receptor]] | ||
*[[Journal:JMedChem:1|Journal:JMedChem:1]] | *[[Journal:JMedChem:1|Journal:JMedChem:1]] | ||
| - | + | == References == | |
| - | == | + | <references/> |
| - | < | + | __TOC__ |
| + | </StructureSection> | ||
[[Category: Estrogen Receptor]] | [[Category: Estrogen Receptor]] | ||
[[Category: Homo sapiens]] | [[Category: Homo sapiens]] | ||
[[Category: RCSB PDB Molecule of the Month]] | [[Category: RCSB PDB Molecule of the Month]] | ||
| - | [[Category: Agard, D A | + | [[Category: Agard, D A]] |
| - | [[Category: Barstad, D | + | [[Category: Barstad, D]] |
| - | [[Category: Cheng, L | + | [[Category: Cheng, L]] |
| - | [[Category: Greene, G L | + | [[Category: Greene, G L]] |
| - | [[Category: Kushner, P J | + | [[Category: Kushner, P J]] |
| - | [[Category: Loria, P M | + | [[Category: Loria, P M]] |
| - | [[Category: Shiau, A K | + | [[Category: Shiau, A K]] |
[[Category: Antagonist]] | [[Category: Antagonist]] | ||
[[Category: Estrogen]] | [[Category: Estrogen]] | ||
[[Category: Nuclear receptor]] | [[Category: Nuclear receptor]] | ||
[[Category: Transcription factor]] | [[Category: Transcription factor]] | ||
Revision as of 14:15, 17 December 2014
HUMAN ESTROGEN RECEPTOR ALPHA LIGAND-BINDING DOMAIN IN COMPLEX WITH 4-HYDROXYTAMOXIFEN
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